Search Result
Results for "
constriction
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-107692
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Neurokinin Receptor
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Neurological Disease
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SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit .
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- HY-119304
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- HY-101952
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- HY-120380
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Autophagy
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Inflammation/Immunology
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FeTMPyP is an orally active peroxynitrite (ONOO ) scavenger. FeTMPyP reduces nitrative stress and increases autophagy. FeTMPyP reduces PARP over-activation and neuroinflammation in chronic constriction injury (CCI)-induced rats, and ameliorates functional, behavioral and biochemical deficits .
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- HY-137227
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15(R)-Pinanethromboxane A2
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Prostaglandin Receptor
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Cardiovascular Disease
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15(R)-PTA2 (15(R)-Pinanethromboxane A2) is an antithrombotic agent that inhibits platelet aggregation. 15(R)-PTA2 inhibits stable prostaglandin endoperoxide analog-induced constriction of feline coronary arteries and stabilizes hepatic lysosomes. 15(R)-PTA2 also inhibits thromboxane synthase but has no effect on prostacyclin synthase .
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- HY-159931
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AAK1
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Neurological Disease
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HW161023 (compound 5) is an orally active AP2-associated protein kinase 1 (AAK1) inhibitor with IC50 values of 5.4 nM and 11.9 μM aganist of AAK1and hERG, respectively. HW161023 inhibits the pain in chronic constriction injury of the sciatic nerve rat model .
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- HY-19202
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rac-EMA401; rac-PD-126055; EMA400
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Angiotensin Receptor
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Neurological Disease
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rac-Olodanrigan (rac-EMA401; EMA400) is a racemic mixture of the S-enantiomer (EMA401; HY-13106) and R-enantiomer (EMA402). rac-Olodanrigan is a potent and selective AT2 receptor antagonist with IC50s of 75.2 nM and 2918 nM for AT2R and AT1R, respectively. rac-Olodanrigan evokes dose-dependent relief of mechanical allodynia in the ipsilateral hind paws of rats with a chronic constriction injury (CCI) of the sciatic nerve .
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- HY-118220
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Thrombin
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Cardiovascular Disease
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EP 171 is a TP receptor agonist and human platelet activator. EP 171 can induce constriction of guinea pig trachea, and the constriction can be inhibited by the TP receptor antagonist EP 092. EP 171 binds to TP receptors on intact human platelets with an IC50 of 2.9 nM .
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- HY-124905
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- HY-W650803
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A-57219
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Adrenergic Receptor
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Cardiovascular Disease
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Nemazoline (A-57219) is selective α-adrenergic agent with α1-agonist/α2-antagonist activity, which is used as a nasal decongestant. Nemazoline produces decongestion by α1-mediated contraction of capacitance vessels, but not compromises blood flow by virtue of α2-antagonism. Nemazoline also blocks endogenous noradrenaline-mediated α 2-constriction of the resistance vessels .
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- HY-118268
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Lipoxygenase
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Cardiovascular Disease
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RG 6866 is a 5-lipoxygenase (5-LOX) inhibitor with the potential to inhibit coronary artery constriction and negative cardiac inotropic effects in cardiac inflammatory states. When the heart is stimulated by antigens, RG 6866 can block the antigen-induced reduction in coronary flow in the heart.
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- HY-N10881
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Others
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Cardiovascular Disease
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Dihydrocurcumenone is a carabrane-type sesquiterpene. Dihydrocurcumenone can be isolated from Curcuma zedoaria, and the common form is 4-dihydrocurcumenone. Curcuma zedoaria sesquiterpene has vascular relaxation activity. 4-dihydrocurcumenone can inhibit the high concentration of K + induced constriction of isolated rat aortic strips .
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- HY-P10898
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- HY-101952R
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PGE2(Standard); Dinoprostone (Standard)
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Reference Standards
Prostaglandin Receptor
Endogenous Metabolite
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Cardiovascular Disease
Endocrinology
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Prostaglandin E2 (Standard) is the analytical standard of Prostaglandin E2. This product is intended for research and analytical applications. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.
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- HY-101952S1
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- HY-101952S
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PGE2-d4; Dinoprostone-d4
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Prostaglandin Receptor
Endogenous Metabolite
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Cardiovascular Disease
Endocrinology
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Prostaglandin E2-d4 is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation .
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- HY-12598A
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DHPG
4 Publications Verification
(RS)-3,5-DHPG
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mGluR
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Neurological Disease
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DHPG is the agonist for mGluR 1/5 (EC50 for mGluR 1 is 60 nM) that activates the phospholipase C (PLC) pathway, and leads ultimately to the activation of protein kinase C (PKC) .
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- HY-12598AR
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mGluR
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Neurological Disease
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DHPG (Standard) is the analytical standard of DHPG. This product is intended for research and analytical applications. DHPG is the agonist for mGluR 1/5 (EC50 for mGluR 1 is 60 nM) that activates the phospholipase C (PLC) pathway, and leads ultimately to the activation of protein kinase C (PKC) .
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- HY-105711
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Lipoxygenase
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Inflammation/Immunology
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RBx-7796 (sodium) is a competitive, highly selective, orally active 5-LO (IC50 = 3.5 mM for human 5-LO enzyme) inhibitor. RBx-7796 (sodium) can effectively inhibit 5-LO activity and LTB4 release. RBx-7796 (sodium) can significantly inhibit airway inflammation and bronchial constriction .
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- HY-138885
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TpGc
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Tyrosinase
DNA/RNA Synthesis
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Neurological Disease
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Tryptamine guanosine carbamate (TpGc) is a selective HINT1 (histidine triad nucleotide-binding protein 1) inhibitor (Ki=34 μM, Kd=3.65 μM). Tryptamine guanosine carbamate significantly enhances morphine antinociception while preventing the development of tolerance .
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- HY-N1478
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P2X Receptor
Reactive Oxygen Species (ROS)
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Neurological Disease
Inflammation/Immunology
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Gardenoside is an orally active natural compound found in Gardenia fruits. Gardenoside reliefs chronic constriction injury (CCI)-induced neuropathic pain by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. Gardenoside reduces reactive oxygen species (ROS). Gardenoside can be used for anti-inflammatory, antinociceptive and hepatoprotective study .
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- HY-N1478R
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P2X Receptor
Reactive Oxygen Species (ROS)
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Neurological Disease
Inflammation/Immunology
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Gardenoside is an orally active natural compound found in Gardenia fruits. Gardenoside reliefs chronic constriction injury (CCI)-induced neuropathic pain by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. Gardenoside reduces reactive oxygen species (ROS). Gardenoside can be used for anti-inflammatory, antinociceptive and hepatoprotective study .
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- HY-120484
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Calcium Channel
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Neurological Disease
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A-1048400 is an orally active and selective calcium channel inhibitor with an IC50 value of 1.4 μM for N-type channels, 1.2 μM for T-type channel. A-1048400 inhibits neurotransmitter release and reduces membrane hyperexcitability, exerting potent analgesic activity. A-1048400 is promising for research of neuropathic pain (e.g., pain induced by spinal nerve ligation and chronic constriction injury) .
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- HY-161539
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Opioid Receptor
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Neurological Disease
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KOR agonist 1 (Compound 7a) is a selective agonist for opioid receptor, with EC50s of 3.4, 701.2 and 1649 nM, for KOR, MOR and DOR, respectively. KOR agonist 1 binds KOR, MOR and DOR, with Kis of 3.9, 1053 and 4196 nM, respectively. KOR agonist 1 exhibits antinociceptive effect in ICR mouse model (ED50 in hot plate test is 0.3 mg/kg, in abdominal constriction test is 0.2 mg/kg) .
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- HY-178006
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P2Y Receptor
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Neurological Disease
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MRS4917 is an orally active, potent selective P2Y14 receptor (hP2Y14R) antagonist (IC50 = 2.88 nM, Ki = 1.67 nM) that shows >18,000 fold selectivity against P2Y6R (IC50 = 54 μM). MRS4917 demonstrates oral efficacy in reversing established mechanoallodynia in the chronic constriction injury (CCI) mouse model, while having no effect on thermoregulation. MRS4917 can be used for neurological diseases research .
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- HY-W740014
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183C91; DZT
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5-HT Receptor
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Neurological Disease
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N-Desmethyl Zolmitriptan (183C91; DZT) is the active metabolite of the serotonin (5-HT) receptor subtype 5-HT1B and 5-HT1D agonist Zolmitriptan (HY-B0229). N-Desmethyl Zolmitriptan (183C91; DZT) is an agonist of 5-HT1B receptors and induces constriction in isolated human cerebral arteries (EC50=100 nM).
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- HY-135871A
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AAK1
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Neurological Disease
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BMT-124110 formic is a potent, selective AAK1 inhibitor, with an IC50 of 0.9 nM. BMT-124110 shows antinociceptive activity. BMT-124110 formic inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 17 and 99 nM, respectively .
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- HY-100571
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Prostaglandin Receptor
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Endocrinology
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Cloprostenol isopropyl ester, a prostaglandin F2α analogs, is the intermediate of (+)-Cloprostenol (HY-107381). Cloprostenol isopropyl ester is a FP receptor agonist with a Ki value of 28 nM .
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- HY-159088
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Opioid Receptor
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Neurological Disease
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KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .
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- HY-135871
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AAK1
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Neurological Disease
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BMT-124110 is a potent, selective AAK1 inhibitor with an IC50 of 0.9 nM. BMT-124110 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 17 and 99 nM, respectively .
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- HY-168214
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Potassium Channel
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Neurological Disease
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Kv7.2/Kv7.3 agonist 1 (Compound 16) is an orally active agonist for KV7.2/7.3 channel (KCNQ2/3) with an EC50 of 1.03 μM. Kv7.2/Kv7.3 agonist 1 exhibits analgesic efficacy in mice chronic constriction injury (CCI) model and mice Streptozotocin (HY-13753)-induced diabetic peripheral neuropathic pain (DPNP) model, with ED50 of 12.02 and 9.63 mg/kg .
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- HY-101317A
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SB-205607
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Opioid Receptor
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Metabolic Disease
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TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.
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- HY-108400
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R-(+)-SCH-23390 maleate
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Dopamine Receptor
5-HT Receptor
Potassium Channel
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Neurological Disease
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SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM .
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- HY-148625
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- HY-19545A
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R-(+)-SCH-23390 hydrochloride
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Dopamine Receptor
5-HT Receptor
Potassium Channel
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Neurological Disease
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SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM .
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- HY-19888
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P2X Receptor
Interleukin Related
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Neurological Disease
Inflammation/Immunology
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GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI) .
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- HY-123382
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Drug Isomer
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Neurological Disease
Inflammation/Immunology
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GSK-1482160 isomer is the isomer of GSK-1482160 (HY-19888). GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI).
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- HY-178281
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Potassium Channel
Sodium Channel
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Neurological Disease
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E0199 is a novel potent dual-target KV7/NaV modulator that activates the KV7 channel (KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels) while simultaneously blocks the NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. E0199 shows a potent analgesic effect without affecting heart and skeletal muscle ion channels critically in a chronic constriction injury (CCI) mouse model. E0199 can be used for Neuropathic pain (NP) research .
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- HY-N2071
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- HY-110036
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L768242
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Cannabinoid Receptor
Endogenous Metabolite
HIF/HIF Prolyl-Hydroxylase
TNF Receptor
Interleukin Related
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Neurological Disease
Inflammation/Immunology
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GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values of 16.1 μM and 4772 nM for CB1. GW-405833 also exhibits non-competitive CB1 antagonist, exerting its analgesic and and anti-inflammatory effect through a CB1 receptor (rather than CB2) dependent mechanism. GW-405833 can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF) .
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- HY-110036A
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L768242 hydrochloride
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Cannabinoid Receptor
Endogenous Metabolite
HIF/HIF Prolyl-Hydroxylase
TNF Receptor
Interleukin Related
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Neurological Disease
Inflammation/Immunology
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GW405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values of 16.1 μM and 4772 nM for CB1. GW405833 hydrochloride also exhibits non-competitive CB1 antagonist, exerting its analgesic effect through a CB1 receptor (rather than CB2) dependent mechanism. GW405833 hydrochloride can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 hydrochloride inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF) .
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- HY-W097625
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Toll-like Receptor (TLR)
MyD88
p38 MAPK
NF-κB
Heme Oxygenase (HO)
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Neurological Disease
Inflammation/Immunology
Cancer
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6-Methoxyflavone is an orally active methoxyflavone. 6-Methoxyflavone suppresses neuroinflammation in microglia through the inhibition of TLR4/MyD88/p38 MAPK/NF-κB dependent pathways and the activation of HO-1/NQO-1 signaling. 6-Methoxyflavone induces S-phase arrest through the CCNA2/CDK2/p21CIP1 signaling pathway in HeLa cells. 6-Methoxyflavone inhibits NFAT Translocation into the nucleus and suppresses T cell activation. 6-Methoxyflavone partially restores chronic ethanol-induced behavioral deficits in mice. 6-Methoxyflavone antagonizes chronic constriction injury and diabetes associated neuropathic nociception expression. 6-Methoxyflavone can be used for the study of cancer, inflammation and neurological diseases .
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- HY-117626
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AAK1
Cyclin G-associated Kinase (GAK)
SARS-CoV
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Infection
Neurological Disease
Inflammation/Immunology
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LP-935509 is an orally active, potent, selective, ATP-competitive and brain-penetrant inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research .
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- HY-N1181
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- HY-101290A
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Cyclin G-associated Kinase (GAK)
AAK1
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Neurological Disease
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BMT-090605 hydrochloride is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 hydrochloride shows antinociceptive activity. BMT-090605 hydrochloride inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 hydrochloride can be used for the research of neuropathic pain .
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- HY-101290
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AAK1
Cyclin G-associated Kinase (GAK)
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Neurological Disease
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BMT-090605 is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 can be used for the research of neuropathic pain .
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| Cat. No. |
Product Name |
Target |
Research Area |
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-101952S
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1 Publications Verification
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Prostaglandin E2-d4 is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation .
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- HY-101952S1
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Prostaglandin E2-d9 is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation .
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| Cat. No. |
Product Name |
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Classification |
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- HY-138885
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TpGc
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Nucleoside Analogs
Guanosine
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Tryptamine guanosine carbamate (TpGc) is a selective HINT1 (histidine triad nucleotide-binding protein 1) inhibitor (Ki=34 μM, Kd=3.65 μM). Tryptamine guanosine carbamate significantly enhances morphine antinociception while preventing the development of tolerance .
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