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Evocarpine, a quinolone alkaloid that could be isolated from Evodiae fructus, inhibitss Ca 2+influx through voltage-dependent calcium channels. Antimycobacterial activity .
Bay K 8644 ((±)-Bay K 8644) is a racemate consisting of two isomers (R)-(+)-Bay-K-8644 and (S)-(-)-Bay-K-8644 . Bay K 8644 is a L-type Ca 2+ channel agonist with an EC50 of 17.3 nM. Bay K 8644 increases Ca 2+influx through sarcolemmal Ca 2+ channels by increasing the open time of the channel. Bay K 8644 has vasoconstrictive effects .
Farnesyl pyrophosphate ammonium salt, a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. Farnesyl pyrophosphate ammonium salt is a TRPM2 (TRP Channel) agonist, and activates TRPM2 opening for ion influx. Farnesyl pyrophosphate ammonium salt is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity .
Calcium influx inducer compound 634 is a calcium influx inducer. Calcium influx inducer compound 634 (10 µM) enhances the release of extracellular vesicles (EVs) from mouse bone marrow-derived dendritic cells (mBMDCs). Calcium influx inducer compound 634 (10 µM) also increases the levels of CD86 and CD80 on the surface of mBMDCs, an effect that can be blocked by the calcium release-activated calcium channel inhibitor YM-58483 (HY-100831) .
H052 is a selective Staphylococcus aureus α-hemolysin (Hla) inhibitor. H052 binds to Hla monomers, disrupts the interaction with host cell membranes to block pore formation, inhibiting calcium ion influx, cytotoxicity, and inflammatory responses. H052 exhibits potency (EC50=30 nM in U937 cells) against Hla-induced calcium influx. H052 is promising for research of lung infections caused by S. aureus .
LY320954 is a selective 5-HT2A receptor antagonist, with a Ki of 96 nM. LY320954 potently inhibits Ca 2+influx in the functional assay (EC50 of 35.5 nM). LY320954 inhibits 5-HT-induced paw swelling in rats, with ED50 of 4.8 mg/kg .
PRO20 is a specific and competitive (pro)renin receptor (PRR) antagonist. PRO20 inhibits Prorenin-induced calcium influx with an IC50 value of 81 nmol/L. PRO20 exerts antihypertensive activity by blocking the binding of prorenin to the PRR, inhibiting the activation of the renin-angiotensin system (RAS), and reducing the production of angiotensin II (Ang II). PRO20 is promising for research of antihypertensive agents .
Bay K 8644 (Standard) is the analytical standard of Bay K 8644. This product is intended for research and analytical applications. Bay K 8644 ((±)-Bay K 8644) is a racemate consisting of two isomers (R)-(+)-Bay-K-8644 and (S)-(-)-Bay-K-8644 . Bay K 8644 is a L-type Ca2+ channel agonist with an EC50 of 17.3 nM. Bay K 8644 increases Ca2+ influx through sarcolemmal Ca2+ channels by increasing the open time of the channel. Bay K 8644 has vasoconstrictive effects .
CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity .
Nothofagin, a dihydrochalcone, is isolated from rooibos (Aspalathus linearis) . Nothofagin downregulates NF-κB translocation through blocking calciuminflux. Nothofagin has antioxidant activity and ameliorates various inflammatory responses such as the septic response and vascular inflammation .
Conantokin-T is a γ-carboxyglutamate-containing, N-methyl-D-aspartate (NMDA) antagonist peptidewith an IC50 value of 2 μM. Conantokin-T inhibits NMDA receptor-mediated calcium influx in central nervous system neurons. Conantokin-T can be purified from the venom of the fish-hunting cone snail, Conus tulipa .
YM928 is an orally active and noncompetitive α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist. YM928 inhibits AMPA receptor-mediated toxicity in primary rat hippocampal cultures with an IC50 value of 2 μM. YM928 blocks AMPA-induced intracellular calcium influx with an IC50 value of 3 μM and antagonizes AMPA-induced inward currents with an IC50 value of 1 μM. YM928 is promising for research of neurological disorders .
Palmitoylglycine (N-palmitoyl glycine), an endogenous lipid that acts as a modulator of calcium influx and nitric oxide () production in sensory neurons. Palmitoylglycine is linked to an increased risk of Background Brugada syndrome (BrS) and interacts with BrS-associated proteins, demonstrating moderate binding affinities for DCC, CR1, CTSB, NAAA, DEFB1, EPHA1, IGF1/IGFBP3/ALS, and LTA .
ω-Agatoxin IVA is a potent, selective P/Q type Ca 2+ (Cav2.1) channel blocker with IC50s of 2 nM and 90 nM for P-type and Q-type Ca 2+ channels, respectively. ω-Agatoxin IVA (IC50, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA has no effect on L-type or N-type calcium channels .
Palmitoylglycine (Standard) is the analytical standard of Palmitoylglycine. This product is intended for research and analytical applications. Palmitoylglycine (N-palmitoyl glycine), an endogenous lipid that acts as a modulator of calcium influx and nitric oxide () production in sensory neurons. Palmitoylglycine is linked to an increased risk of Background Brugada syndrome (BrS) and interacts with BrS-associated proteins, demonstrating moderate binding affinities for DCC, CR1, CTSB, NAAA, DEFB1, EPHA1, IGF1/IGFBP3/ALS, and LTA[1][2][3].
ω-Agatoxin IVA TFA is a potent, selective P/Q type Ca 2+ (Cav2.1) channel blocker with IC50s of 2 nM and 90 nM for P-type and Q-type Ca 2+ channels, respectively. ω-Agatoxin IVA TFA (IC50, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA TFA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA TFA has no effect on L-type or N-type calcium channels .
2-Chloroadenosine is an adenosine analog, a transporter permeabilizer of nucleoside transporters, and a competitive uridine influx inhibitor (apparent Ki=33 μM). 2-Chloroadenosine binds to nitrobenzylthioinosine with high affinity (apparent Ki=0.18 mM). 2-Chloroadenosine promotes Apoptosis and increases cerebral blood flow. 2-Chloroadenosine has anticonvulsant properties. 2-Chloroadenosine is used to study infection, inflammatory diseases, cancer, blood-related diseases, lung injury, epilepsy, and kidney disease .
(-)-Praeruptorin A is a nature product that could be isolated from the roots of Peucedanum praeruptorum Dunn. (-)-Praeruptorin A relaxes ileum and tracheal smooth muscles by activating NO/cGMP signaling pathway. (-)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca 2+-influx blocker .
Mepivacaine hydrochloride binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization .
Diltiazem-d3 (hydrochloride) is the deuterium labeled Diltiazem hydrochloride. Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist)[1][2].
Riparin is a nonspecific smooth muscle relaxant. Riparin exerts spasmolytic effect by inhibiting Ca 2+influx and inhibiting the release of intracellular calcium ion stores .
Diltiazem (hydrochloride) (Standard) is the analytical standard of Diltiazem (hydrochloride). This product is intended for research and analytical applications. Diltiazem hydrochloride is a Ca 2+influx inhibitor (slow channel blocker or calcium antagonist).
Diltiazem-(acetoxy-d3) (hydrochloride) is the deuterium labeled Diltiazem hydrochloride. Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist)[1][2].
ITH12575, a CGP37157 derivative, is a potent and selective mNCX blocker. ITH12575 reduces Ca 2+influx through CALHM1 at low micromolar concentrations .
(S)-AMG-628 (Compound 16q) is the S-isomer of AMG-628 (HY-123374). (S)-AMG-628 is the orally active antagonist for TRPV1, that inhibits the Capsaicin (HY-10448)- and acid-induced Ca 2+-influx with IC50 of 7 nM and 5 nM in CHO cell. (S)-AMG-628 ameliorates Capsaicin-induced rats flinching, and reverses the thermal hypersensitivity in CFA-(HY-153808) induced inflammatory pain models .
Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization .
Diltiazem-d6 (hydrochloride) (CRD-401-d6 (hydrochloride)) is deuterium labeled Diltiazem (hydrochloride). Diltiazem hydrochloride is a Ca 2+influx inhibitor (slow channel blocker or calcium antagonist).
Palmitoylcarnitine chloride is a fatty acid-derived mitochondrial substrate, and selectively decreases cell survival in colorectal and prostate cancer cells by affecting on pro-inflammatory pathways, Ca 2+influx, and DHT-like effects .
OBAA is a potent phospholipase A2 (PLA2) inhibitor with an IC50 of 70 nM. OBAA blocks Melittin-induced Ca 2+influx in Trypanosoma brucei with an IC50 of 0.4 μM .
Celangulin is an insecticidal component isolated from Celastrus angulatus. Celangulin activates the calcium channel on the plasma membrane with increasing the intracellular Ca 2+ after influx from the external. Celangulin activates the calcium channel in the ER .
Aminopterin N-hydroxysuccinimide ester(NHS-methotrexate) is an irreversible
Methotrexate (HY-14519) influx carrier inhibitor. Aminopterin N-hydroxysuccinimide ester can be used for the research of rheumatoid arthritis and a number of cancers (such as acute lymphoblastic leukemia) .
GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca 2+influx and elevate intracellular Ca 2+ in HEK cells .
Imperatoxin A, a peptide toxin derived from the venom of the African scorpion Pandinus imperator, activator of Ca 2+-release channels/ryanodine receptors (RyRs) enhances the influx of Ca 2+ from the sarcoplasmatic reticulum into the cell .
Mepivacaine (hydrochloride) (Standard) is the analytical standard of Mepivacaine (hydrochloride). This product is intended for research and analytical applications. Mepivacaine hydrochloride binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization .
HC-030031 is a potent and selective TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.
Bekanamycin (Kanamycin B) is an aminoglycoside antibiotic produced by Streptomyces kanamyceticus, against an array of Gram-positive and Gram-negative bacterial strain .
Bekanamycin (Standard) is the analytical standard of Bekanamycin. This product is intended for research and analytical applications. Bekanamycin (Kanamycin B) is an aminoglycoside antibiotic produced by Streptomyces kanamyceticus, against an array of Gram-positive and Gram-negative bacterial strain .
(-)-Denudatin B is an antiplatelet agent. (-)-Denudatin B relaxed vascular smooth muscle by inhibiting the Ca2+ influx through voltage-gated and receptor-operated Ca2+ channels . And (-)-Denudatin B has nonspecific antiplatelet action
MLN3126 is an orally active and potent CCR9 antagonist. MLN3126 inhibits CCL25-induced calcium mobilization and chemotaxis of mouse primary thymocytes, wiht an IC50 value of 6.3 nM for calcium influx .
Gabapentin is a potent, orally active P/Q type Ca 2+ channel blocker. Gabapentin inhibits neuronal Ca 2+influx and reduction of neurotransmitter release. Gabapentin is a GABA analog that can be used to relieve neuropathic pain .
Gabapentin hydrochloride is a potent, orally active P/Q type Ca 2+ channel blocker. Gabapentin hydrochloride inhibits neuronal Ca 2+influx and reduction of neurotransmitter release. Gabapentin hydrochloride is a GABA analog that can be used to relieve neuropathic pain .
Mepivacaine-d3 is the deuterium labeled Mepivacaine. Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization .
Propiverine is a potent antimuscarinic agent. Propiverine inhibits cellular calcium influx, thereby diminishing muscle spasm. Propiverine has neurotropic and musculotropic effects on the urinary bladder smooth muscle. Propiverine can used for overactive bladder (OAB) research .
13(S)-HODE is the lipoxygenase metabolite of Linoleic acid (HY-N0729). 13(S)-HODE modulates the platelet-activating factor, leukotriene B4, and formyl-Met-Leu-Phe-induced calcium influx in human polymorphonuclear leukocytes.
KS-133 is a selective and potent antagonist of vasoactive intestinal peptide receptor 2 (VIPR2), with the IC50 values of 24.8 nM and 500 nM in Ca influx assay and cAMP assay. KS-133 plays an important role in schizophrenia research .
Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasma membrane. Syringomycin E causes K + efflux, Ca 2+influx, and changes in membrane potential, and is related to channel formation .
Imperatoxin A TFA is a peptide toxin derived from the venom of the African scorpion Pandinus imperator. Imperatoxin A TFA is a Ca 2+-release channels/ryanodine receptors (RyRs) activator. Imperatoxin A TFA enhances the influx of Ca 2+ from the sarcoplasmatic reticulum into the cell .
Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
Amlodipine mesylate, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine mesylate can be used for the research of high blood pressure and cancer .
Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca 2+influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects .
1,4-Dihydropyridine is an inhibitor for calcium channel, that blocks the L-type calcium channels, reduces the influx of calcium ions into cardiac and vascular smooth muscle cells, and thus reduces the contractility and heart rate of the heart, dilates blood vessels, and lowers blood pressure .
Mepivacaine (Standard) is the analytical standard of Mepivacaine. This product is intended for research and analytical applications. Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization .
Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
KS-133 TFA is a selective and potent antagonist of vasoactive intestinal peptide receptor 2 (VIPR2), with the IC50 values of 24.8 nM and 500 nM in Ca influx assay and cAMP assay. KS-133 TFA plays an important role in schizophrenia research .
Losigamone (AO-33) is an orally active antiepileptic compound. Losigamone blocks sodium channel. Losigamone stimulates the neuronal chloride channel and enhance chloride influx. Losigamone potentiates GABA-mediated responses and reduces epileptiform activity induced by chloride channel antagonists. Losigamone can be used for epilepsy research .
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+influx and Ca 2+ cell overload .
Etripamil (MSP-2017) hydrochloride is a short-acting, L-type calcium channel antagonist that can be used in the study of paroxysmal supraventricular tachycardia (PSVT). Etripamil hydrochloride inhibits calcium influx through slow calcium channels, thereby slowing atrioventricular node conduction and prolonging the atrioventricular node refractory period.
7ACC2 is a potent monocarboxylate transporter (MCT) inhibitor with an IC50 of 11 nM for inhibition of [ 14C]-lactate influx. 7ACC2 is also a potent inhibitor of mitochondrial pyruvate transport. 7ACC2 is an anticancer agent through inhibition of lactate flux .
Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer .
(+)-Mepivacaine is a racemic isomer of Mepivacaine (HY-B0517), which has analgesic and vasoconstrictive activity. Mepivacaine is an amide type agent that temporarily causes local loss of consciousness. Mepivacaine binds to specific voltage-gated sodium channels on neuronal cell membranes, inhibiting sodium influx and membrane depolarization .
CCR6 antagonist 2 (Compound 20c) is the antagonist for CCR6 with a Ki of 1.1 nM. CCR6 antagonist 2 inhibits CCL20-induced calcium ion influx (IC50 = 4.9 nM), inhibits the chemotactic migration of CCR6+ T cells (IC50 = 190 nM) .
(R)-(+)-Bupivacaine hydrochloride is a voltage-gated sodium channel inhibitor. (R)-(+)-Bupivacaine hydrochloride can selectively block the voltage-gated sodium channels on nerve cell membranes, inhibit the influx of sodium ions, and thus prevent the generation and conduction of nerve impulses, exerting local anesthetic activity. (R)-(+)-Bupivacaine hydrochloride can be used in research of acute pains .
Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
U-44069 serinol amide is a derivative of U-44069 (HY-121825). U-44069 serinol amide is a stable analog of the endoperoxide prostaglandin H2 (HY-136500). U-44069 serinol amide is a vasoconstrictor that can induce preglomerular Ca 2+influx .
Gabapentin (Standard) is the analytical standard of Gabapentin. This product is intended for research and analytical applications. Gabapentin is a potent, orally active P/Q type Ca2+ channel blocker. Gabapentin inhibits neuronal Ca2+ influx and reduction of neurotransmitter release. Gabapentin is a GABA analog that can be used to relieve neuropathic pain .
Phaseic acid is a Abscisic acid terpenoid catabolite that can able to activate a subset of Abscisic acid repectors. Phaseic acid is a plant hormone associated with photosynthesis arrest and abscission. Phaseic acid is the antagonist for NMDA-type glutamate receptor (NMDAR) that inhibits NMDAR currents with an IC50 of 34.37 μM. Phaseic acid reduces intracellular calcium influx, and exhibits neuroprotective effect .
Urolithin C, a gut-microbial metabolite of Ellagic acid, is a glucose-dependent activator of insulin secretion. Urolithin C is a L-type Ca 2+ channel opener and enhances Ca 2+influx. Urolithin C induces cell apoptosis through a mitochondria-mediated pathway and also stimulates reactive oxygen species (ROS) formation .
Cyclic ADP-ribose (cADPR) is a potent second messenger for calcium mobilization that is synthesized from NAD + by an ADP-ribosyl cyclase. Cyclic ADP-ribose increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels .
Amlodipine-d4 (maleate) is the deuterium labeled Amlodipine maleate. Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
(2E)-OBAA is a potent phospholipase A2 (PLA2) inhibitor, with an IC50 of 70 nM. (2E)-OBAA induces apoptosis of HUVEC cells. (2E)-OBAA blocks Melittin-induced Ca 2+influx in Trypanosoma brucei, with an IC50 of 0.4 μM .
Anisodine (Daturamine) is a neuroprotective compound that reduces exacerbated M1, M2, M4, and M5 receptor expression in brain tissues under hypoxia/reoxygenation conditions. Anisodine inhibits calcium ion influx and reactive oxygen species (ROS)levels. Anisodine leads to decreased aspartate levels during hypoxia .
Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca 2+influx .
Amlodipine (Standard) is the analytical standard of Amlodipine. This product is intended for research and analytical applications. Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
Calcium Channel antagonist 6 (Compound 328) is a highly selective antagonist of voltage-gated calcium channel CaV2.2 with an IC50 value of 0.37 μM. Calcium Channel antagonist 6 inhibits of neuron depolarization-induced Ca 2+influx. Calcium Channel antagonist 6 is promising for research of neuropathic pain .
Anisodine (Daturamine) hydrobromide is a neuroprotective compound that reduces exacerbated M1, M2, M4, and M5 receptor expression in brain tissues under hypoxia/reoxygenation conditions. Anisodine hydrobromide inhibits calcium ion influx and reactive oxygen species (ROS)levels. Anisodine hydrobromide leads to decreased aspartate levels during hypoxia .
Gabapentin-d4 hydrochloride is the deuterium labeled Gabapentin hydrochloride (HY-A0057A). Gabapentin hydrochloride is a potent, orally active P/Q type Ca 2+ channel blocker. Gabapentin hydrochloride inhibits neuronal Ca 2+influx and reduction of neurotransmitter release. Gabapentin hydrochloride is a GABA analog that can be used to relieve neuropathic pain .
NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.
Cyclic ADP-ribose ammonium (cADPR ammonium) is a potent second messenger for calcium mobilization that is synthesized from NAD + by an ADP-ribosyl cyclase. Cyclic ADP-ribose ammonium increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels .
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease .
Amlodipine (maleate) (Standard) is the analytical standard of Amlodipine (maleate). This product is intended for research and analytical applications. Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
M3/PDE4 modulator-1 (compound 10f) is a bifunctional molecule that is an M3 mAChR antagonist and a PDE4 inhibitor. M3/PDE4 modulator-1 (10-1000 nM/kg; iv) reduces cysteine eosinophil influx in the OVA rat model .
Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca 2+influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders .
Lys-Bradykinin, a kind of kallidin and bradykinin receptor ligand, can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin, also a vasodilator, can widen blood vessels and increase blood flow. ys-Bradykinin stimulates net Na+ influx, and also the DNA synthesis. Lys-Bradykinin involves in vascular regulation, inflammation and pain sensation .
Englerin A (Standard) is the analytical standard of Englerin A. This product is intended for research and analytical applications. Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca2+ influx and Ca2+ cell overload .
Amlodipine-d9 maleate is deuterated labeled Amlodipine maleate (HY-B0317A). Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
Amlodipine-d4 (besylate) is the deuterium labeled Amlodipine besylate. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer .
Amlodipine (maleate) (Standard) is the analytical standard of Amlodipine (maleate). This product is intended for research and analytical applications. Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
Amlodipine-d4 is a deuterium labeled Amlodipine (HY-B0317). Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
Procyanidin A1 (Standard) is the analytical standard of Procyanidin A1. This product is intended for research and analytical applications. Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects .
Amlodipine-1,1,2,2-d4 (maleate) is the deuterium labeled Amlodipine. Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca 2+influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation .
ISX-9 (Isoxazole 9) is a potent inducer of adult neural stem cell differentiation. ISX-9 activates Ca 2+influx through both voltage-gated Ca 2+ channels and NMDA receptors and increases neuroD expression. ISX-9 also induces cardiomyogenic differentiation of Notch-activated epicardium-derived cells (NECs) .
(±)-1,2-Diolein- 13C3 (1,2-Dioleoyl-rac-glycerol- 13C3) is 13C labeled (±)-1,2-Diolein. (±)-1,2-Diolein (1,2-Dioleoyl-rac-glycerol) is a PKC activator. (±)-1,2-Diolein increases myotubes Ca 2+influx .
Phaseic acid-d4 is the deuterium labeled Phaseic acid. Phaseic acid is a Abscisic acid terpenoid catabolite that can able to activate a subset of Abscisic acid repectors. Phaseic acid is a plant hormone associated with photosynthesis arrest and abscission. Phaseic acid is the antagonist for NMDA-type glutamate receptor (NMDAR) that inhibits NMDAR currents with an IC50 of 34.37 μM. Phaseic acid reduces intracellular calcium influx, and exhibits neuroprotective effect .
Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain management in vivo .
Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is used for the research of neuropathic pain management .
BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
Amlodipine (besylate) (Standard) is the analytical standard of Amlodipine (besylate). This product is intended for research and analytical applications. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer .
Obexelimab (XmAb5871) is a humanized anti-CD19 antibody. Obexelimab works by inhibiting B cell receptor (BCR) mediated calcium influx and promoting the phosphorylation of Fc γ receptor IIb (FcγRIIb), which reduces B cell activation and function, leading to B cell apoptosis. Obexelimab can be used in research for rheumatoid arthritis and systemic lupus erythematosus .
Etripamil (MSP-2017) is a short-acting, L-type calcium-channel antagonist. Etripamil inhibits calcium influx through slow calcium channels, thereby slowing AV node conduction and prolonging the AV node refractory period. Etripamil increases heart rate and decreases systolic blood pressure. Etripamil can be used in the study of paroxysmal supraventricular tachycardia (PSVT) .
A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta .
Ropivacaine hydrochloride monohydrate is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for regional anesthesia and neuropathic pain management in vivo .
BAPTA tetrapotassium is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrapotassium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
Nisoldipine (BAY-k 5552; Sular) is an orally active and blood-brain barrier-penetrating dihydropyridine calcium antagonist, with greater vascular selectivity than other calcium channel antagonists. Nisoldipine inhibits calcium influx and blocks voltage-gated calcium channels. Nisoldipine dilates coronary and systemic arteries. Nisoldipine has antihypertensive and anti-anginal activity. Nisoldipine also displays neuroprotective and antiviral activity .
iJak-381 is a JAK1/2 inhibitor with anti-inflammatory activity. iJak-381 blocks IL-13 signaling and also inhibits IL-4 and IL-6 signaling pathways. iJak-381 also reduced p-STAT6 levels and inhibited the influx of inflammatory cells into the lungs of mice. iJak-381 inhibits airway hyperresponsiveness (AHR) .
(E/Z)-Farnesyl pyrophosphate ((E/Z)-Farnesyl diphosphate), a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. (E/Z)-Farnesyl pyrophosphate is a TRPM2 (TRP Channel) agonist, activates TRPM2 opening for ion influx. (E/Z)-Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
AMG-628 is an orally active inhibitor for TRPV1, that inhibits Capsaicin (HY-10448) or acid (pH 5)-induced Ca 2+influx into TRPV1- expressing CHO cell with IC50 of 4.9 and 3.1 nM. AMG-628 exhibits analgesic activity in Capsaicin (HY-10448)-induced rat model, and exhibits a half-life of 2.4 h in rats .
Ropivacaine-d7 is deuterium labeled Ropivacaine. Ropivacain is a potent?sodium channel?blocker. Ropivacain blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is used for the research of neuropathic pain?management .
Ropivacaine mesylate is a long-acting amide local anaesthetic agent for a spinal block and effectively blocks neuropathic pain. Ropivacaine blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibressup>[1] . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel)?TREK-1?with an IC50?of 402.7 μM in COS-7 cell's membrane .
BAPTA tetrasodium is a selective chelator for calcium. BAPTA tetrasodium, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrasodium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA tetrasodium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
Lys-Bradykinin (Kallidin (380-389) (human, porcine, bovine)) tetraacetate, a kind of kallidin and bradykinin receptor ligand, can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin tetraacetate, also a vasodilator, can widen blood vessels and increase blood flow. ys-Bradykinin stimulates net Na+ influx, and also the DNA synthesis. Lys-Bradykinin tetraacetate involves in vascular regulation, inflammation and pain sensation .
TRPV2-selective blocker 1 (compound IV2-1) is a selective TRPV2 channel blocker with an IC50 of 6.3 μM. TRPV2-selective blocker 1 does not affect TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 also inhibits TRPV2-mediated Ca 2+influx in macrophages, and inhibits macrophage phagocytosis .
D-AP4 (D-APB; D-2-Amino-4-phosphonobutyric acid), a phosphono analogue of glutamate, is an NMDA broad spectrum excitatory amino acid receptor antagonist. D-AP4 also is an agonist for a quisqualate-sensitized AP6 site in hippocampus. D-AP4 inhibits AMPA receptor-stimulated 57Co 2+influx in cultured cerebellar granule cells (IC50 ≥ 100 μM) .
Lys-Bradykinin TFA is the TFA salt form of Lys-Bradykinin (HY-103293). Lys-Bradykinin TFA is a ligand for kallidin and bradykinin receptor, which can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin TFA serves as a vasodilator, which widens blood vessels and increases blood flow. Lys-Bradykinin TFA stimulates net Na+ influx, and contributes to DNA synthesis. Lys-Bradykinin TFA involves in vascular regulation, inflammation and pain sensation .
Israpafant (Y-24180) is a potent, selective and long-acting platelet activation factor (PAF) receptor antagonist with IC50s of 0.84 nM and 3.84 nM against PAF-induced human and rabbit platelet aggregation, respectively. Israpafant stimulates both extracellular Ca 2+influx and intracellular Ca 2+ release in prostate cancer cells. Israpafant suppresses the allergic cutaneous reactions including eosinophilia, cytokine production, edema and erythema in mice .
DL-Menthol (Racementhol) is an orally active, GABAaR positive allosteric modulator and UDP-glucuronosyltransferase (UGT) inhibitor that can cross the blood-brain barrier. DL-Menthol binds to GABAAR and exhibits an allosteric activation effect, enhancing GABA-mediated chloride influx and inhibiting neuronal excitability. DL-Menthol can induce surgical anesthesia in fish and inhibit the metabolic detoxification of tobacco carcinogens by human liver and intestinal UGT enzymes, resulting in reduced NNAL-N-Gluc production .
Perindopril-d5 (S-9490-d5) is deuterium labeled Perindopril. Perindopril (S-9490) is an orally available, long-acting angiotensin-converting enzyme (ACE) inhibitor. Perindopril inhibits inflammatory cell influx and intimal thickening, preserving elastin on the inside of the aorta. Perindopril effectively inhibits experimental abdominal aortic aneurysm (AAA) formation in a rat model and reduces pulmonary vasoconstriction in rats with pulmonary hypertension .
Ropivacaine (Standard) is the analytical standard of Ropivacaine. This product is intended for research and analytical applications. Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is used for the research of neuropathic pain management .
FLY26 is a selective partial GluN2B antagonist with an IC50 value of 0.64 μM. FLY26 partially inhibits the GluN2B subunit of NMDA receptors, reduces calcium ion influx and reactive oxygen species (ROS) production and activates the BDNF/TrkB/CREB neuroprotective signaling pathway to alleviate neuronal excitotoxicity and mitochondrial dysfunction. FLY26 is promising for research of neurological deficits caused by cerebral ischemia-reperfusion injury .
PDDHV is a calcium absorption inducer and may achieve 45Ca 2+influx by stimulating vanillic acid receptor VR1. PDDHV induces 45Ca 2+ uptake (EC50: 70 nM) in rat dorsal root ganglion neurons (expressing native vanilloid receptors) and calcium mobilization (EC50: 125 nM) in VR1-transfected CHO cells. PDDHV also inhibits [3H]-resiniferatoxin (RTX) binding to the dorsal root ganglion membrane in rats .
Mavatrep-d6 (JNJ-39439335-d6) is a deuterated labeled Mavatrep (HY-16935). Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
JNJ-41443532 (CCR2 antagonist 5) is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). JNJ-41443532 displays a Ki of 9.6 µM for mCCR2 binding. JNJ-41443532 can be used in the research of inflammatory disease .
Ropivacaine (hydrochloride monohydrate) (Standard) is the analytical standard of Ropivacaine (hydrochloride monohydrate). This product is intended for research and analytical applications. Ropivacaine hydrochloride monohydrate is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for regional anesthesia and neuropathic pain management in vivo .
Mrgx2 antagonist-3 (Compound B-40) is a highly selective antagonist of MrgX2 receptor with an IC50 value of 0.042-2.5 nM. Mrgx2 antagonist-3 blocks downstream G protein signaling and β-Arrestin recruitment, thereby inhibiting MrgX2 receptor-mediated calcium influx and cellular degranulation. Mrgx2 antagonist-3 is promising for research of inflammation-related diseases and pruritus, such as chronic urticaria, allergic asthma .
BAPTA (Standard) is the analytical standard of BAPTA. This product is intended for research and analytical applications. BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca2+ release from intracellular stores or influx via Ca2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca2+ chelators .
Ropivacaine-d7 hydrochloride is a deuterium labeled Ropivacaine (hydrochloride) (HY-B0563B) . Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain management in vivo .
dl-Tetrandrine is an orally active and brain-penetrant calcium channel blocker that inhibits voltage-dependent calcium channels. dl-Tetrandrine selectively blocks Ca 2+influx with an IC50 value of approximately 1-10 μM. dl-Tetrandrine exerts anti-inflammatory, immunosuppressive, and anti-arrhythmic activities by inhibiting intracellular calcium overload, and can reverse multidrug resistance in tumor cells. dl-Tetrandrine is promising for research of autoimmune diseases (such as rheumatoid arthritis), cardiovascular diseases, and tumor drug resistance reversal .
MRS4719 is a potent P2X4 receptor antagonist with an IC50 value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca 2+]iinflux in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke .
Leukadherin-1, a specific agonist of the leukocyte surface integrin CD11b/CD18, increases CD11b/CD18-dependent cell adhesion to fibrinogen with an EC50 of 4 μM. Leukadherin-1 enhances leukocyte adhesion to ligands (such as ICAM-1) and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites. Leukadherin-1 suppresses innate inflammatory signaling .
β-Amyloid (1-40) (rat) is a rat form of the amyloid β-peptide, which accumulates as an insoluble extracellular deposit around neurons, giving rise to the senile plaques associated with Alzheimer's disease (AD). β-Amyloid (1-40) (rat) increases 45Ca 2+influx, induces neurodegeneration in the rat hippocampal neurons of the CA1 subfield. β-Amyloid (1-40) (rat) induces apoptosis. β-Amyloid (1-40) (rat) can be used for the research of Alzheimer's disease .
YM-355179 fumarate is a newly synthesized selective CCR3 antagonist with the potential to inhibit eosinophil-related allergic inflammatory diseases. YM-355179 can effectively inhibit the binding of CCL11 and CCL5 to CCR3-expressing cells, with IC50 values of 7.6 nM and 24 nM respectively. In functional experiments, YM-355179 can inhibit CCL11-induced intracellular Ca(2+) influx, chemotaxis and eosinophil degranulation, IC50 The values are 8.0 nM, 24 nM and 29 nM respectively .
(+)-Niguldipine hydrochloride is an antagonist for calcium channel. (+)-Niguldipine hydrochloride produces vasodilation by blocking calcium channels and reducing the transmembrane influx of calcium ions. (+)-Niguldipine hydrochloride inhibits U-46619 (HY-108566)-induced coronary vasoconstriction in guinea pig Langendorff heart with pID50 of 11.37, binds to calcium channel on guinea pig skeletal muscle membrane with Ki of 9.75, and lowers the blood pressure in spontaneously hypertensive rat with pED30 of 7.1. (+)-Niguldipine hydrochloride ameliorates cardiovascular diseases such as hypertension, angina pectoris and arrhythmias .
BAPTA (tetrasodium) (Standard) is the analytical standard of BAPTA (tetrasodium). This product is intended for research and analytical applications. BAPTA tetrasodium is a selective chelator for calcium. BAPTA tetrasodium, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrasodium is widely used as an intracellular buffer for investigating the effects of Ca2+ release from intracellular stores or influx via Ca2+-permeable channels in the plasma membrane. BAPTA tetrasodium can also inhibit phospholipase C activity independently of their role as Ca2+ chelators .
Candidalysin is a cytolytic peptide toxin secreted by the fungus Candida albicans. Candidalysin drives epithelial immune responses by activating the EGFR-MAPK signaling pathway, inducing MMP expression and calcium influx, and regulating the c-Fos transcription factor and MKP1 via p38 MAPK and ERK1/2 respectively. Candidalysin is essential for mucosal and systemic infections, activating NLRP3 to promote inflammatory responses, neutrophil recruitment, and Th17 immunity. Candidalysin activates LDH causing membrane damage and exhibiting cytotoxicity
SKP-451 is an ATP-sensitive potassium (K +) channel agonist. SKP-451 activates the ATP-sensitive K + channels, promotes the efflux of K +, causes membrane hyperpolarization, and inhibits the influx of Ca 2+, thereby relaxing the vascular smooth muscle. SKP-451 relaxs the canine coronary artery, rabbit basilar artery, and vertebral artery. SKP-451 also reduces the mean arterial blood pressure of conscious spontaneously hypertensive rats (SHR). SKP-451 is promising for research of cardiovascular diseases .
8-Br-7-CH-ADPR (8-Bromo-7-deazaadenosine-5'-O-diphosphoribose) is a specific TRPM2 antagonist that inhibits TRPM2 activation by binding to the NUDT9 homology domain of the TRPM2 channel, thereby controlling the influx of cations through the cell membrane channel. 8-Br-7-CH-ADPR can be used to study the role of TRPM2 in pathological processes such as cell death, neurodegenerative diseases, myocardial infarction, and diabetes .
Guanidinoethyl sulfonate (Taurocyamine) is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .
Cinnarizine is an orally active, effective and selective inhibitor of L-type calcium channel Cav1.3 with an IC50 of 1.5 μM (in vestibular hair cells). Cinnarizine can cross the blood-brain barrier and regulate calcium homeostasis and dopamine neurotransmission. Cinnarizine inhibits the influx of calcium ions into smooth muscle cells by blocking L-type calcium channels, thereby relaxing vascular smooth muscle, improving cerebral circulation and reducing blood viscosity, while antagonizing dopamine receptors. Cinnarizine can be used in the study of vestibular vertigo, Meniere's disease and cerebrovascular diseases .
Diphyllin is an orally active V-ATPase inhibitor (IC50=17 nM) and HIV-1 inhibitor (IC50=0.38 μM). Diphyllin blocks the acidification of osteoclast lysosomes and bone resorption lacunas (IC50=0.6 nM for acid influx inhibition)， thereby inhibiting bone resorption. Diphyllin can effectively inhibit osteoclast-mediated bone resorption and has no effect on osteoblastic bone formation. Diphyllin can be used in the research of bone metabolism-related diseases and has the potential to inhibit diseases related to excessive bone resorption .
Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca 2+influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca 2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels .
Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca 2+influx through voltage-gated Ca 2+ channels, leading to the reduction in [Ca 2+]i in vascular smooth muscle cells and consequent peripheral vasodilation . Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM .
(-)-Niguldipine ((R)-Niguldipine) hydrochloride is a calcium channel antagonist. (-)-Niguldipine hydrochloride exerts a vasodilatory effect by blocking calcium channels and reducing the transmembrane influx of calcium ions. (-)-Niguldipine can inhibit U-46619 (HY-108566)-induced coronary artery contraction in guinea pig Langendorff hearts (pID50 of 9.93), has high affinity for calcium channel binding sites on guinea pig skeletal muscle membranes (Ki of 8.10), and lowers blood pressure in spontaneously hypertensive rats (pED30 of 5.55). (-)-Niguldipine hydrochloride can improve cardiovascular diseases such as hypertension, angina pectoris, and arrhythmias .
QNZ46 is a highly selective noncompetitive NMDA receptor antagonist targeting GluN2C/D (IC50=3.9 μM), GluN1/GluN2C (IC50=7.1 μM), and GluN1/GluN2D (IC50=182 μM) subunits. QNZ46 inhibits glutamate-mediated calcium influx, thereby blocking excitotoxicity. QNZ46 is membrane permeable and can cross the blood-brain barrier, where it inhibits myelin damage and axonal degeneration .
GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel Kir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of Kir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, Kir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome .
Deoxypheganomycin D is a specific antimycobacterial inhibitor with no cross-resistance to other antibiotics such as Paromomycin (HY-B0956), Capreomycin (HY-P3270), Viomycin (HY-A0155), Streptothricin (HY-129065), Kanamycin (HY-16566), and Streptomycin (HY-B1906). Deoxypheganomycin D (28 μM) partially inhibits the growth of Mycobacterium 607, with no significant inhibitory effects on DNA, RNA, or protein synthesis. Deoxypheganomycin D (7 μM) affects leucine influx, not thymidine, and has the opposite effect on efflux. The effects of Deoxypheganomycin D may be related to cell membrane and specific mycobacterial lipid components.
Guanidinoethyl sulfonate (Standard) is the analytical standard of Guanidinoethyl sulfonate. This product is intended for research and analytical applications. Guanidinoethyl sulfonate is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .
Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
Ginsenoside Rd (Standard) is the analytical standard of Ginsenoside Rd. This product is intended for research and analytical applications. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium salt can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium salt participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .
Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
(2R,3R)-Butane-2,3-diol is a non-covalent, reversible agonist targeting lanthanum (La 3+)-sensitive calcium channels in bacteria (e.g., Escherichia coli) with an EC50 of approximately 25 mM. (2R,3R)-Butane-2,3-diol binds to calcium channel proteins or related complexes, induces channel opening, promotes extracellular calcium influx, and triggers intracellular calcium transients, which may regulate bacterial physiological activities such as growth, metabolism, and signal transduction. (2R,3R)-Butane-2,3-diol mediates bacterial-host cell signaling interactions and affects the metabolic balance of intestinal microorganisms, and can be used to study lactose intolerance and other related diseases .
Trimebutine-d3 hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Trimebutine-d5 fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Zandatrigine (NBI-921352; XEN901) is a selective, orally active, voltage-gated sodium channel NaV1.6/SCN8A inhibitor that can penetrate the blood-brain barrier. Zandatrigine inhibits sodium influx by non-covalently binding to the VSD4 structure of NaV1.6, blocking the persistent and resuscitative currents under pathological conditions. Zandatrigine can reduce neuronal hyperexcitability and reduce epileptic seizures. Zandatrigine is 134-756-fold selective for other isoforms such as NaV1.1 and NaV1.2, and has minimal effect on NaV1.1 expressed by inhibitory interneurons. Zandatrigine can be used to study NaV1.6-mediated neuroexcitability diseases such as SCN8A-related developmental epileptic encephalopathy (SCN8A-DEE) and adult focal epilepsy .
Trimebutine maleate (Standard) is the analytical standard of Trimebutine maleate (HY-B0380A). This product is intended for research and analytical applications. Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Dehydroepiandrosterone sulfate sodium dihydrate-d6 sodium dihydrate is the deuterium labeled Dehydroepiandrosterone sulfate sodium dihydrate. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium dihydrate is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium dihydrate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium dihydrate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium dihydrate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium dihydrate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .
PPZ2 is a diacylglycerol (DAG)-activated TRPC3/TRPC6/TRPC7 channel activator with activity in promoting neuronal development and survival. PPZ2 activates recombinant TRPC3/TRPC6/TRPC7 channels in a dose-dependent manner without affecting other TRPC channels. PPZ2 elicits cation currents and calcium ion (Ca(2+)) influx in cultured central neurons. PPZ2 is able to induce BDNF-like neurite outgrowth and neuroprotection, an effect that disappears after TRPC3/TRPC6/TRPC7 knockdown or inhibition. PPZ2 also increases the activation of the calcium-dependent transcription factor cAMP response element binding protein. The effects of PPZ2 suggest that calcium signaling mediated by activation of DAG-activated TRPC channels plays an important role in its neurotrophic effects .
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) (Standard) is the analytical standard of Dehydroepiandrosterone sulfate (HY-113416). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .
Trimebutine (Standard) is the analytical standard of Trimebutine (HY-B0380). This product is intended for research and analytical applications. Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Dehydroepiandrosterone sulfate sodium salt-d6 (DHEA sulfate sodium salt-d6; Prasterone sulfate sodium salt-d6) is the deuterium labeled Dehydroepiandrosterone sulfate sodium salt (HY-B0765). Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium salt can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium salt participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt (Standard) is the analytical standard of Dehydroepiandrosterone sulfate sodium salt (HY-B0765). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .
Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
Pheniramine (maleate) (Standard) is the analytical standard of Pheniramine (maleate). This product is intended for research and analytical applications. Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
Pheniramine (Standard) is the analytical standard of Pheniramine. This product is intended for research and analytical applications. Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
(2R,3R)-Butane-2,3-diol (Standard) is the analytical standard of (2R,3R)-Butane-2,3-diol (HY-W015954). This product is intended for research and analytical applications. (2R,3R)-Butane-2,3-diol is a non-covalent, reversible agonist targeting lanthanum (La 3+)-sensitive calcium channels in bacteria (e.g., Escherichia coli) with an EC50 of approximately 25 mM. (2R,3R)-Butane-2,3-diol binds to calcium channel proteins or related complexes, induces channel opening, promotes extracellular calcium influx, and triggers intracellular calcium transients, which may regulate bacterial physiological activities such as growth, metabolism, and signal transduction. (2R,3R)-Butane-2,3-diol mediates bacterial-host cell signaling interactions and affects the metabolic balance of intestinal microorganisms, and can be used to study lactose intolerance and other related diseases .
BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
BAPTA tetrapotassium is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrapotassium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
BAPTA (Standard) is the analytical standard of BAPTA. This product is intended for research and analytical applications. BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca2+ release from intracellular stores or influx via Ca2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca2+ chelators .
CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity .
CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity .
ω-Agatoxin IVA TFA is a potent, selective P/Q type Ca 2+ (Cav2.1) channel blocker with IC50s of 2 nM and 90 nM for P-type and Q-type Ca 2+ channels, respectively. ω-Agatoxin IVA TFA (IC50, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA TFA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA TFA has no effect on L-type or N-type calcium channels .
PRO20 is a specific and competitive (pro)renin receptor (PRR) antagonist. PRO20 inhibits Prorenin-induced calcium influx with an IC50 value of 81 nmol/L. PRO20 exerts antihypertensive activity by blocking the binding of prorenin to the PRR, inhibiting the activation of the renin-angiotensin system (RAS), and reducing the production of angiotensin II (Ang II). PRO20 is promising for research of antihypertensive agents .
Conantokin-T is a γ-carboxyglutamate-containing, N-methyl-D-aspartate (NMDA) antagonist peptidewith an IC50 value of 2 μM. Conantokin-T inhibits NMDA receptor-mediated calcium influx in central nervous system neurons. Conantokin-T can be purified from the venom of the fish-hunting cone snail, Conus tulipa .
ω-Agatoxin IVA is a potent, selective P/Q type Ca 2+ (Cav2.1) channel blocker with IC50s of 2 nM and 90 nM for P-type and Q-type Ca 2+ channels, respectively. ω-Agatoxin IVA (IC50, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA has no effect on L-type or N-type calcium channels .
Imperatoxin A, a peptide toxin derived from the venom of the African scorpion Pandinus imperator, activator of Ca 2+-release channels/ryanodine receptors (RyRs) enhances the influx of Ca 2+ from the sarcoplasmatic reticulum into the cell .
KS-133 is a selective and potent antagonist of vasoactive intestinal peptide receptor 2 (VIPR2), with the IC50 values of 24.8 nM and 500 nM in Ca influx assay and cAMP assay. KS-133 plays an important role in schizophrenia research .
Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasma membrane. Syringomycin E causes K + efflux, Ca 2+influx, and changes in membrane potential, and is related to channel formation .
Imperatoxin A TFA is a peptide toxin derived from the venom of the African scorpion Pandinus imperator. Imperatoxin A TFA is a Ca 2+-release channels/ryanodine receptors (RyRs) activator. Imperatoxin A TFA enhances the influx of Ca 2+ from the sarcoplasmatic reticulum into the cell .
KS-133 TFA is a selective and potent antagonist of vasoactive intestinal peptide receptor 2 (VIPR2), with the IC50 values of 24.8 nM and 500 nM in Ca influx assay and cAMP assay. KS-133 TFA plays an important role in schizophrenia research .
Lys-Bradykinin, a kind of kallidin and bradykinin receptor ligand, can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin, also a vasodilator, can widen blood vessels and increase blood flow. ys-Bradykinin stimulates net Na+ influx, and also the DNA synthesis. Lys-Bradykinin involves in vascular regulation, inflammation and pain sensation .
Lys-Bradykinin (Kallidin (380-389) (human, porcine, bovine)) tetraacetate, a kind of kallidin and bradykinin receptor ligand, can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin tetraacetate, also a vasodilator, can widen blood vessels and increase blood flow. ys-Bradykinin stimulates net Na+ influx, and also the DNA synthesis. Lys-Bradykinin tetraacetate involves in vascular regulation, inflammation and pain sensation .
Lys-Bradykinin TFA is the TFA salt form of Lys-Bradykinin (HY-103293). Lys-Bradykinin TFA is a ligand for kallidin and bradykinin receptor, which can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin TFA serves as a vasodilator, which widens blood vessels and increases blood flow. Lys-Bradykinin TFA stimulates net Na+ influx, and contributes to DNA synthesis. Lys-Bradykinin TFA involves in vascular regulation, inflammation and pain sensation .
β-Amyloid (1-40) (rat) is a rat form of the amyloid β-peptide, which accumulates as an insoluble extracellular deposit around neurons, giving rise to the senile plaques associated with Alzheimer's disease (AD). β-Amyloid (1-40) (rat) increases 45Ca 2+influx, induces neurodegeneration in the rat hippocampal neurons of the CA1 subfield. β-Amyloid (1-40) (rat) induces apoptosis. β-Amyloid (1-40) (rat) can be used for the research of Alzheimer's disease .
Candidalysin is a cytolytic peptide toxin secreted by the fungus Candida albicans. Candidalysin drives epithelial immune responses by activating the EGFR-MAPK signaling pathway, inducing MMP expression and calcium influx, and regulating the c-Fos transcription factor and MKP1 via p38 MAPK and ERK1/2 respectively. Candidalysin is essential for mucosal and systemic infections, activating NLRP3 to promote inflammatory responses, neutrophil recruitment, and Th17 immunity. Candidalysin activates LDH causing membrane damage and exhibiting cytotoxicity
Obexelimab (XmAb5871) is a humanized anti-CD19 antibody. Obexelimab works by inhibiting B cell receptor (BCR) mediated calcium influx and promoting the phosphorylation of Fc γ receptor IIb (FcγRIIb), which reduces B cell activation and function, leading to B cell apoptosis. Obexelimab can be used in research for rheumatoid arthritis and systemic lupus erythematosus .
Evocarpine, a quinolone alkaloid that could be isolated from Evodiae fructus, inhibitss Ca 2+influx through voltage-dependent calcium channels. Antimycobacterial activity .
Farnesyl pyrophosphate ammonium salt, a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. Farnesyl pyrophosphate ammonium salt is a TRPM2 (TRP Channel) agonist, and activates TRPM2 opening for ion influx. Farnesyl pyrophosphate ammonium salt is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
Palmitoylglycine (N-palmitoyl glycine), an endogenous lipid that acts as a modulator of calcium influx and nitric oxide () production in sensory neurons. Palmitoylglycine is linked to an increased risk of Background Brugada syndrome (BrS) and interacts with BrS-associated proteins, demonstrating moderate binding affinities for DCC, CR1, CTSB, NAAA, DEFB1, EPHA1, IGF1/IGFBP3/ALS, and LTA .
Palmitoylcarnitine chloride is a fatty acid-derived mitochondrial substrate, and selectively decreases cell survival in colorectal and prostate cancer cells by affecting on pro-inflammatory pathways, Ca 2+influx, and DHT-like effects .
Bekanamycin (Kanamycin B) is an aminoglycoside antibiotic produced by Streptomyces kanamyceticus, against an array of Gram-positive and Gram-negative bacterial strain .
Nothofagin, a dihydrochalcone, is isolated from rooibos (Aspalathus linearis) . Nothofagin downregulates NF-κB translocation through blocking calciuminflux. Nothofagin has antioxidant activity and ameliorates various inflammatory responses such as the septic response and vascular inflammation .
Palmitoylglycine (Standard) is the analytical standard of Palmitoylglycine. This product is intended for research and analytical applications. Palmitoylglycine (N-palmitoyl glycine), an endogenous lipid that acts as a modulator of calcium influx and nitric oxide () production in sensory neurons. Palmitoylglycine is linked to an increased risk of Background Brugada syndrome (BrS) and interacts with BrS-associated proteins, demonstrating moderate binding affinities for DCC, CR1, CTSB, NAAA, DEFB1, EPHA1, IGF1/IGFBP3/ALS, and LTA[1][2][3].
(-)-Praeruptorin A is a nature product that could be isolated from the roots of Peucedanum praeruptorum Dunn. (-)-Praeruptorin A relaxes ileum and tracheal smooth muscles by activating NO/cGMP signaling pathway. (-)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca 2+-influx blocker .
Celangulin is an insecticidal component isolated from Celastrus angulatus. Celangulin activates the calcium channel on the plasma membrane with increasing the intracellular Ca 2+ after influx from the external. Celangulin activates the calcium channel in the ER .
Bekanamycin (Standard) is the analytical standard of Bekanamycin. This product is intended for research and analytical applications. Bekanamycin (Kanamycin B) is an aminoglycoside antibiotic produced by Streptomyces kanamyceticus, against an array of Gram-positive and Gram-negative bacterial strain .
(-)-Denudatin B is an antiplatelet agent. (-)-Denudatin B relaxed vascular smooth muscle by inhibiting the Ca2+ influx through voltage-gated and receptor-operated Ca2+ channels . And (-)-Denudatin B has nonspecific antiplatelet action
Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca 2+influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects .
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+influx and Ca 2+ cell overload .
Urolithin C, a gut-microbial metabolite of Ellagic acid, is a glucose-dependent activator of insulin secretion. Urolithin C is a L-type Ca 2+ channel opener and enhances Ca 2+influx. Urolithin C induces cell apoptosis through a mitochondria-mediated pathway and also stimulates reactive oxygen species (ROS) formation .
Cyclic ADP-ribose (cADPR) is a potent second messenger for calcium mobilization that is synthesized from NAD + by an ADP-ribosyl cyclase. Cyclic ADP-ribose increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels .
Anisodine (Daturamine) is a neuroprotective compound that reduces exacerbated M1, M2, M4, and M5 receptor expression in brain tissues under hypoxia/reoxygenation conditions. Anisodine inhibits calcium ion influx and reactive oxygen species (ROS)levels. Anisodine leads to decreased aspartate levels during hypoxia .
Cyclic ADP-ribose ammonium (cADPR ammonium) is a potent second messenger for calcium mobilization that is synthesized from NAD + by an ADP-ribosyl cyclase. Cyclic ADP-ribose ammonium increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels .
Englerin A (Standard) is the analytical standard of Englerin A. This product is intended for research and analytical applications. Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca2+ influx and Ca2+ cell overload .
Procyanidin A1 (Standard) is the analytical standard of Procyanidin A1. This product is intended for research and analytical applications. Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects .
(E/Z)-Farnesyl pyrophosphate ((E/Z)-Farnesyl diphosphate), a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. (E/Z)-Farnesyl pyrophosphate is a TRPM2 (TRP Channel) agonist, activates TRPM2 opening for ion influx. (E/Z)-Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis .
DL-Menthol (Racementhol) is an orally active, GABAaR positive allosteric modulator and UDP-glucuronosyltransferase (UGT) inhibitor that can cross the blood-brain barrier. DL-Menthol binds to GABAAR and exhibits an allosteric activation effect, enhancing GABA-mediated chloride influx and inhibiting neuronal excitability. DL-Menthol can induce surgical anesthesia in fish and inhibit the metabolic detoxification of tobacco carcinogens by human liver and intestinal UGT enzymes, resulting in reduced NNAL-N-Gluc production .
dl-Tetrandrine is an orally active and brain-penetrant calcium channel blocker that inhibits voltage-dependent calcium channels. dl-Tetrandrine selectively blocks Ca 2+influx with an IC50 value of approximately 1-10 μM. dl-Tetrandrine exerts anti-inflammatory, immunosuppressive, and anti-arrhythmic activities by inhibiting intracellular calcium overload, and can reverse multidrug resistance in tumor cells. dl-Tetrandrine is promising for research of autoimmune diseases (such as rheumatoid arthritis), cardiovascular diseases, and tumor drug resistance reversal .
Guanidinoethyl sulfonate (Taurocyamine) is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .
Diphyllin is an orally active V-ATPase inhibitor (IC50=17 nM) and HIV-1 inhibitor (IC50=0.38 μM). Diphyllin blocks the acidification of osteoclast lysosomes and bone resorption lacunas (IC50=0.6 nM for acid influx inhibition)， thereby inhibiting bone resorption. Diphyllin can effectively inhibit osteoclast-mediated bone resorption and has no effect on osteoblastic bone formation. Diphyllin can be used in the research of bone metabolism-related diseases and has the potential to inhibit diseases related to excessive bone resorption .
Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca 2+influx through voltage-gated Ca 2+ channels, leading to the reduction in [Ca 2+]i in vascular smooth muscle cells and consequent peripheral vasodilation . Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM .
Guanidinoethyl sulfonate (Standard) is the analytical standard of Guanidinoethyl sulfonate. This product is intended for research and analytical applications. Guanidinoethyl sulfonate is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .
Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
Ginsenoside Rd (Standard) is the analytical standard of Ginsenoside Rd. This product is intended for research and analytical applications. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium salt can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium salt participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .
(2R,3R)-Butane-2,3-diol is a non-covalent, reversible agonist targeting lanthanum (La 3+)-sensitive calcium channels in bacteria (e.g., Escherichia coli) with an EC50 of approximately 25 mM. (2R,3R)-Butane-2,3-diol binds to calcium channel proteins or related complexes, induces channel opening, promotes extracellular calcium influx, and triggers intracellular calcium transients, which may regulate bacterial physiological activities such as growth, metabolism, and signal transduction. (2R,3R)-Butane-2,3-diol mediates bacterial-host cell signaling interactions and affects the metabolic balance of intestinal microorganisms, and can be used to study lactose intolerance and other related diseases .
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) (Standard) is the analytical standard of Dehydroepiandrosterone sulfate (HY-113416). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .
Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt (Standard) is the analytical standard of Dehydroepiandrosterone sulfate sodium salt (HY-B0765). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .
(2R,3R)-Butane-2,3-diol (Standard) is the analytical standard of (2R,3R)-Butane-2,3-diol (HY-W015954). This product is intended for research and analytical applications. (2R,3R)-Butane-2,3-diol is a non-covalent, reversible agonist targeting lanthanum (La 3+)-sensitive calcium channels in bacteria (e.g., Escherichia coli) with an EC50 of approximately 25 mM. (2R,3R)-Butane-2,3-diol binds to calcium channel proteins or related complexes, induces channel opening, promotes extracellular calcium influx, and triggers intracellular calcium transients, which may regulate bacterial physiological activities such as growth, metabolism, and signal transduction. (2R,3R)-Butane-2,3-diol mediates bacterial-host cell signaling interactions and affects the metabolic balance of intestinal microorganisms, and can be used to study lactose intolerance and other related diseases .
FYN Protein, Human (Biotinylated, sf9, His, Flag, Avi) is the recombinant human-derived FYN, expressed by Sf9 insect cells , with Avi, His, Flag labeled tag.
Diltiazem-d3 (hydrochloride) is the deuterium labeled Diltiazem hydrochloride. Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist)[1][2].
Mepivacaine-d3 is the deuterium labeled Mepivacaine. Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization .
Amlodipine-d4 (maleate) is the deuterium labeled Amlodipine maleate. Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
Amlodipine-d4 is a deuterium labeled Amlodipine (HY-B0317). Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
Amlodipine-1,1,2,2-d4 (maleate) is the deuterium labeled Amlodipine. Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer .
Diltiazem-(acetoxy-d3) (hydrochloride) is the deuterium labeled Diltiazem hydrochloride. Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist)[1][2].
Diltiazem-d6 (hydrochloride) (CRD-401-d6 (hydrochloride)) is deuterium labeled Diltiazem (hydrochloride). Diltiazem hydrochloride is a Ca 2+influx inhibitor (slow channel blocker or calcium antagonist).
Gabapentin-d4 hydrochloride is the deuterium labeled Gabapentin hydrochloride (HY-A0057A). Gabapentin hydrochloride is a potent, orally active P/Q type Ca 2+ channel blocker. Gabapentin hydrochloride inhibits neuronal Ca 2+influx and reduction of neurotransmitter release. Gabapentin hydrochloride is a GABA analog that can be used to relieve neuropathic pain .
Amlodipine-d9 maleate is deuterated labeled Amlodipine maleate (HY-B0317A). Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer .
Amlodipine-d4 (besylate) is the deuterium labeled Amlodipine besylate. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer .
(±)-1,2-Diolein- 13C3 (1,2-Dioleoyl-rac-glycerol- 13C3) is 13C labeled (±)-1,2-Diolein. (±)-1,2-Diolein (1,2-Dioleoyl-rac-glycerol) is a PKC activator. (±)-1,2-Diolein increases myotubes Ca 2+influx .
Phaseic acid-d4 is the deuterium labeled Phaseic acid. Phaseic acid is a Abscisic acid terpenoid catabolite that can able to activate a subset of Abscisic acid repectors. Phaseic acid is a plant hormone associated with photosynthesis arrest and abscission. Phaseic acid is the antagonist for NMDA-type glutamate receptor (NMDAR) that inhibits NMDAR currents with an IC50 of 34.37 μM. Phaseic acid reduces intracellular calcium influx, and exhibits neuroprotective effect .
Ropivacaine-d7 is deuterium labeled Ropivacaine. Ropivacain is a potent?sodium channel?blocker. Ropivacain blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is used for the research of neuropathic pain?management .
Perindopril-d5 (S-9490-d5) is deuterium labeled Perindopril. Perindopril (S-9490) is an orally available, long-acting angiotensin-converting enzyme (ACE) inhibitor. Perindopril inhibits inflammatory cell influx and intimal thickening, preserving elastin on the inside of the aorta. Perindopril effectively inhibits experimental abdominal aortic aneurysm (AAA) formation in a rat model and reduces pulmonary vasoconstriction in rats with pulmonary hypertension .
Mavatrep-d6 (JNJ-39439335-d6) is a deuterated labeled Mavatrep (HY-16935). Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
Ropivacaine-d7 hydrochloride is a deuterium labeled Ropivacaine (hydrochloride) (HY-B0563B) . Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain management in vivo .
Trimebutine-d3 hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Trimebutine-d5 fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Dehydroepiandrosterone sulfate sodium dihydrate-d6 sodium dihydrate is the deuterium labeled Dehydroepiandrosterone sulfate sodium dihydrate. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium dihydrate is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium dihydrate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium dihydrate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium dihydrate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium dihydrate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .
Dehydroepiandrosterone sulfate sodium salt-d6 (DHEA sulfate sodium salt-d6; Prasterone sulfate sodium salt-d6) is the deuterium labeled Dehydroepiandrosterone sulfate sodium salt (HY-B0765). Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium salt can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium salt participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality .
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