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Results for "

Desensitization

" in MedChemExpress (MCE) Product Catalog:

34

Inhibitors & Agonists

6

Peptides

11

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101165
    Cyclothiazide

    		iGluR Neurological Disease
    Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current .
    Cyclothiazide
  • HY-121027
    Anagyrine

    (-)-Anagyrine; Monolupine; Rhombinine

    		 mAChR nAChR Neurological Disease
    Anagyrine ((-)-Anagyrine) is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine is a potent and effective desensitizer of nAChR, and Anagyrine can directly, without metabolism, desensitize nAChR .
    Anagyrine
  • HY-103229
    Cl-HIBO

    		iGluR Neurological Disease
    Cl-HIBO is a highly subtype-selective GluR1/2 agonist (EC50=4.7 and 1.7 μM, respectively). Cl-HIBO is a potent AMPA receptor agonist (IC50=0.22 μM). Cl-HIBO has desensitizing properties .
    Cl-HIBO
  • HY-121027A
    Anagyrine hydrochloride

    (-)-Anagyrine hydrochloride; Monolupine hydrochloride; Rhombinine hydrochloride

    		 mAChR nAChR Neurological Disease
    Anagyrine ((-)-Anagyrine) hydrochloride is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine hydrochloride binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine hydrochloride is a potent and effective desensitizer of nAChR, and Anagyrine hydrochloride can directly, without metabolism, desensitize nAChR .
    Anagyrine hydrochloride
  • HY-101165R
    Cyclothiazide (Standard)

    		Reference Standards iGluR Neurological Disease
    Cyclothiazide (Standard) is the analytical standard of Cyclothiazide. This product is intended for research and analytical applications. Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current .
    Cyclothiazide (Standard)
  • HY-124906
    JAMI1001A

    		iGluR Neurological Disease
    JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms .
    JAMI1001A
  • HY-P3785
    PKI(5-22)amide

    		PKA Neurological Disease
    PKI(5-22)amide is the active inhibitory fragment of the inhibitor of the cyclic AMP-dependent protein kinase (PKA). PKI(5-22)amide inhibits PKA activation, but fails to attenuate homologous desensitization of CRF1 receptors .
    PKI(5-22)amide
  • HY-P10594
    Myr-Arf1(2–17)

    		Ras Endocrinology
    Myr-Arf1(2–17) is a sarcosinated peptide that mimics the localization and function of Arf1 protein on the cell membrane. Myr-Arf1(2–17) can be used to study the desensitization mechanism of luteinizing hormone/chorionic gonadotropin receptor (LH/CGR) .
    Myr-Arf1(2–17)
  • HY-137988
    Palvanil

    		TRP Channel Neurological Disease Inflammation/Immunology
    Palvanil is a Capsaicin (HY-10448) analogue, shows strong desensitizing capability against the TRPV1 receptor. Palvanil shows anti-nociceptive and anti-inflammation effects .
    Palvanil
  • HY-P5876
    Proadrenomedullin (N-20) (bovine, porcine)

    ProADM N20(bovine, porcine); PAMP-20(bovine, porcine)

    		 nAChR Neurological Disease
    Proadrenomedullin (N-20) (ProADM N20) (bovine, porcine) is a potent and noncompetitive hypotensive and catecholamine release-inhibitory peptide released from chromaffin cells. Proadrenomedullin (N-20) (bovine, porcine) inhibits catecholamine secretion with an IC50 of 350 nM in PC12 pheochromocytoma cells. Proadrenomedullin (N-20) (bovine, porcine) also blocks (EC50≈270 nM) nicotinic cholinergic agonist desensitization of catecholamine release, as well as desensitization of nicotinic signal transduction ( 22Na + uptake) .
    Proadrenomedullin (N-20) (bovine, porcine)
  • HY-103045
    CMPD101
    4 Publications Verification

    		 PKC ROCK Cardiovascular Disease
    CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure .
    CMPD101
  • HY-120946
    VMY-2-95

    		nAChR Neurological Disease
    VMY-2-95 is an oral active and blood-brain barrier (BBB) penetrant α4β2 nicotinic acetylcholine receptor desensitizer. VMY-2-95 can be used for study of depression or addiction .
    VMY-2-95
  • HY-119943B
    (R)-PF-06256142

    		Dopamine Receptor Neurological Disease
    (R)-PF-06256142 is the R enantiomer of PF-06256142 with low active. PF-06256142 is a potent and selective orthosteric D1 receptor agonist that can reduce receptor desensitization relative to dopamine and other catechol-containing agonists .
    (R)-PF-06256142
  • HY-B0822S1
    Fipronil-13C6

    		GABA Receptor Cytochrome P450 Inflammation/Immunology
    Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
    Fipronil-13C6
  • HY-161118
    MB327

    		Others Neurological Disease
    MB327 is a bipyridine nonoxime compound that restores neuromuscular function. MB327 restores the activity of nicotinamide acetylcholine receptors (nAChRs) for carbachol desensitization in a typical type II PAM manner. MB327 can neutralize nerve agent poisoning .
    MB327
  • HY-172588
    GABAA receptor modulator-7

    		GABA Receptor Neurological Disease
    GABAA receptor modulator-7 (compound 1m), a spiro-Barbiturate, is a GABAA receptor modulator. GABAA receptor modulator-7 reverses the action of anesthetics without affecting GABA-induced desensitization and can be used for study of antiepileptics and anxiolytics .
    GABAA receptor modulator-7
  • HY-P3041
    Chromostatin (bovine)

    		Calcium Channel Endocrinology
    Chromostatin bovine is a chromogranin A (CGA) derivative peptide, which inhibits postassium or carbamoylcholine induced catecholamine release with an ID50 of 5 nM. Chromostatin bovine reduces calcium flux, enhances the desensitization process of the cholinergic-evoked secretory response and modulates the endocrine response associated with catecholamine .
    Chromostatin (bovine)
  • HY-W004049
    3-Hydroxybenzoic acid

    		Endogenous Metabolite Hydroxycarboxylic Acid Receptor (HCAR) Neurological Disease Metabolic Disease Inflammation/Immunology
    3-Hydroxybenzoic acid is an orally active endogenous metabolite. 3-Hydroxybenzoic acid is an agonist for GPR81 and GPR109A. 3-Hydroxybenzoic acid acts as stress response desensitizers. 3-Hydroxybenzoic acid can be used for anti-inflammatory and analgesic study .
    3-Hydroxybenzoic acid
  • HY-173471
    TRPA1 agonist-1

    		TRP Channel Neurological Disease
    TRPA1 agonist-1 (compound 21) is a potent and selective TAAR1 agonist with an EC50 of 25.47 μM. TRPA1 agonist-1 shows effective analgesic properties without irritation in mice .
    TRPA1 agonist-1
  • HY-12509
    PEPA

    		iGluR Neurological Disease
    PEPA is an AMPA receptor allosteric potentiator. PEPA shows preferential action of PEPA on the flop form of AMPA receptors. PEPA is a more potent suppressor of desensitization of receptors containing GluR3 and GluR4 as opposed to those containing GluR1. PEPA has antianxiety effects .
    PEPA
  • HY-N4323
    14-Deoxyandrographolide

    		Calcium Channel Apoptosis Caspase Neurological Disease Metabolic Disease
    14-Deoxyandrographolide is a diterpene with calcium channel blocking activity and acts as a uterine smooth muscle relaxant. 14-Deoxyandrographolide stimulates the release of nitric oxide (NO) in endothelial cells. 14-Deoxyandrographolide gradually desensitizes liver cells to TNF-α mediated apoptosis by inducing the release of TNFRSF1A .
    14-Deoxyandrographolide
  • HY-W004049R
    3-Hydroxybenzoic acid (Standard)

    		Endogenous Metabolite Hydroxycarboxylic Acid Receptor (HCAR) Neurological Disease Metabolic Disease Inflammation/Immunology
    3-Hydroxybenzoic acid (Standard) is the analytical standard of 3-Hydroxybenzoic acid. This product is intended for research and analytical applications. 3-Hydroxybenzoic acid is an orally active endogenous metabolite. 3-Hydroxybenzoic acid is an agonist for GPR81 and GPR109A. 3-Hydroxybenzoic acid acts as stress response desensitizers. 3-Hydroxybenzoic acid can be used for anti-inflammatory and analgesic study.
    3-Hydroxybenzoic acid (Standard)
  • HY-100939
    4-Chlorophenylguanidine hydrochloride

    		Sodium Channel Neurological Disease
    4-Chlorophenylguanidine hydrochloride is a potent ASIC3 positive allosteric modulator and reverses the effects of ASIC3 desensitization. 4-Chlorophenylguanidine hydrochloride influences ASIC3 activity through directly activating the channel and increasing proton sensitivity. 4-Chlorophenylguanidine hydrochloride offers a chemical backbone for the design of new ASIC3 ligands to study ASIC3 in vivo .
    4-Chlorophenylguanidine hydrochloride
  • HY-N4323R
    14-Deoxyandrographolide (Standard)

    		Calcium Channel Apoptosis Caspase Neurological Disease Metabolic Disease
    14-Deoxyandrographolide (Standard) is the analytical standard of 14-Deoxyandrographolide. 14-Deoxyandrographolide is a diterpene with calcium channel blocking activity and acts as a uterine smooth muscle relaxant. 14-Deoxyandrographolide stimulates the release of nitric oxide (NO) in endothelial cells. 14-Deoxyandrographolide gradually desensitizes liver cells to TNF-α mediated apoptosis by inducing the release of TNFRSF1A .
    14-Deoxyandrographolide (Standard)
  • HY-121082
    (-)-Dihydroalprenolol

    L-Dihydroalprenolol

    		 Adrenergic Receptor Endocrinology
    (-)-Dihydroalprenolol (L-Dihydroalprenolol) is a β-adrenergic antagonist that inhibits the activity of β-adrenergic receptors. (-)-Dihydroalprenolol can cause desensitization of approximately 60% of β-adrenergic receptor binding sites. (-)-Dihydroalprenolol has also been shown to reduce the binding capacity of specific β-adrenergic ligands. (-)-Dihydroalprenolol may affect the ability to stimulate membrane-bound adenylate acylase .
    (-)-Dihydroalprenolol
  • HY-P2307
    Tat-NR2Baa

    		iGluR NO Synthase Neurological Disease
    Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 .
    Tat-NR2Baa
  • HY-P2307A
    Tat-NR2Baa TFA

    		iGluR NO Synthase Neurological Disease
    Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95 .
    Tat-NR2Baa TFA
  • HY-130176
    UFP-512

    		Opioid Receptor ERK Adenylate Cyclase Neurological Disease
    UFP-512 is a selective and potent σ-opioid receptor (DOP receptor) peptidic agonist with antidepressant- and anxiolytic-like effects. UFP-512 exhibits as a potent agonist on adenylyl cyclase inhibition and Erk1/2 activation. UFP-512 induces phosphorylation of DOP receptors on Ser 363 with a low desensitization of the cAMP pathway. UFP-512 is promising for research of mood disorders .
    UFP-512
  • HY-N2071
    Cedrol
    1 Publications Verification

    (+)-Cedrol; α-Cedrol

    		 Cytochrome P450 Fungal Apoptosis Caspase Platelet-activating Factor Receptor (PAFR) Infection Neurological Disease Inflammation/Immunology Cancer
    Cedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties .
    Cedrol
  • HY-N2071R
    Cedrol (Standard)

    		Cytochrome P450 Fungal Apoptosis Caspase Infection Neurological Disease Inflammation/Immunology Cancer
    Cedrol (Standard) is the analytical standard of Cedrol. This product is intended for research and analytical applications. Cedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties.
    Cedrol (Standard)
  • HY-W001160
    5-Hydroxyindole

    		Endogenous Metabolite Calcium Channel nAChR Neurological Disease Endocrinology Cancer
    5-Hydroxyindole is an orally active hydroxylated indole and tryptophan metabolite. 5-Hydroxyindole activates α7 nicotinic acetylcholine receptors and acts on intestinal L-type calcium channels. 5-Hydroxyindole slows down the desensitization of 5-HT3 receptor-mediated ion currents in cells. 5-Hydroxyindole causes convulsions and loss of consciousness. 5-Hydroxyindole is used in the study of neuroblastoma, schizophrenia, and diseases related to intestinal motility disorders .
    5-Hydroxyindole
  • HY-W001160R
    5-Hydroxyindole (Standard)

    		Endogenous Metabolite nAChR Calcium Channel Neurological Disease Endocrinology Cancer
    5-Hydroxyindole (Standard) is the analytical standard of 5-Hydroxyindole (HY-W001160). This product is intended for research and analytical applications. 5-Hydroxyindole is an orally active hydroxylated indole and tryptophan metabolite. 5-Hydroxyindole activates α7 nicotinic acetylcholine receptors and acts on intestinal L-type calcium channels. 5-Hydroxyindole slows down the desensitization of 5-HT3 receptor-mediated ion currents in cells. 5-Hydroxyindole causes convulsions and loss of consciousness. 5-Hydroxyindole is used in the study of neuroblastoma, schizophrenia, and diseases related to intestinal motility disorders .
    5-Hydroxyindole (Standard)
  • HY-121143
    Bis-Q

    		Cholinesterase (ChE) Neurological Disease
    Bis-Q is an acetylcholine (ACh) agonist that targets voltage-clamped muscle fibers of the fish Xenomystus nigris. Bis-Q exists in two forms: cis-Bis-Q (non-agonist) and trans-Bis-Q (agonist). Photoisomerization converts cis-Bis-Q to trans-Bis-Q, which induces agonist-induced currents. Channels activated by trans-Bis-Q and ACh have similar conductances and open times. Flashes increase the ratio of trans-Bis-Q to cis-Bis-Q until light equilibrium is reached. Further flashes transiently increase agonist-induced currents, indicating binding of trans-Bis-Q to desensitized receptors. Higher concentrations of cis-Bis-Q produce larger agonist-induced currents that decay exponentially. .
    Bis-Q
  • HY-150057
    CB1R Allosteric modulator 4

    		Cannabinoid Receptor Others
    CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment .
    CB1R Allosteric modulator 4

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