| Cat. No. |
Product Name |
CAS No. |
Information |
| H4840 |
AMG-333
|
1416799-28-4 |
AMG-333 (AMG333, AMG 333) is a novel potent, highly selective TRPM8 antagonist with IC50 of 13 nM and 20 nM for hTRPM8 and rTRPM8, respectively; displays high selectivity over other TRP channels (IC50>20 uM, TRPV1/V3/V4/A1); exhibits statistically significant and dose-dependent prevention of icilin-induced rat WDS, at 0.6, 1 and 3 mg/kg, inhibits cold-induced increase in blood pressure in the rat CPT in a dose-dependent manner with 1 and 3 mg/kg producing significant inhibition with an ED90 of 1.1 mg/kg, also fully blocks the cold pressor response at 3 mg/kg. |
| H4520 |
Tezampanel
|
150131-78-5 |
Tezampanel (LY 293558, NGX 424) is a competitive antagonist of the AMPA and kainate receptors with selectivity for the GluR5 subtype of the kainate receptor; has neuroprotective and anticonvulsant properties, also has anxiolytic effects in animal studies. |
| H4472 |
Dasolampanel
|
503294-13-1 |
Dasolampanel (NGX426) is an orally bioavailable, competitive antagonist of the AMPA-kainate receptors for the treatment of chronic pain conditions including neuropathic pain and migraine. |
| H3809 |
BGC20-1531
|
1962928-26-2 |
BGC20-1531 (PGN-1531, AP 1531) is a potent, selective prostanoid EP receptor EP antagonist, exhibits high affinity at recombinant human EP4 receptors expressed in cell lines (pKB=7.6) and native EP4 receptors in human cerebral and meningeal artery (pKB=7.6-7.8); shows no appreciable affinity at a wide range of other receptors (including other prostanoid receptors), channels, transporters and enzymes (pKi < 5); competitively antagonizes PGE(2)-induced vasodilatation of human middle cerebral (pK(B) 7.8) and meningeal (pK(B) 7.6) arteries in vitro, and PGE(2)-induced increase in canine carotid blood flow in vivo. |
| H3099 |
Ubrogepant
|
1374248-77-7 |
Ubrogepant (MK-1602) is a novel potent, selective, oral calcitonin gene-related peptide receptor (CGRP) antagonist for acute treatment of migraine. |
| H3096 |
MK-8825
|
1380887-60-4 |
MK-8825 is a highly potent, selective, orally bioavailable CGRP receptor antagonist with Ki of 17 nM for rat CGRP; blocks hCGRP-stimulated cAMP responses in HEK293 cells stably expressing the human CGRP receptor with IC50 of 0.23 nM; possesses significantly improved in vivo potency in rat pharmacodynamic models. |
| H3093 |
MK-0974
|
781649-09-0 |
A potent, selective, orally bioavailable CGRP receptor antagonist with Ki of 0.77 nM; shows >10,000-fold selectivity in a panel of assays representing over 160 receptors, transporters, and enzymes; inhibits CGRP-stimulated cAMP production in E10 cells with IC50 of 2.2 nM; inhibits the capsaicin-induced increase in dermal blood flow in monkey models. |
| H3092 |
Atogepant
|
1374248-81-3 |
A potent, selective and orally available CGRP receptor antagonist for the prevention of migraine. |
| H2865 |
Frovatriptan
|
158930-17-7 |
A potent, long lasting 5-HT(1B/1D) receptor agonist as a antimigraine agent. |
| H2859 |
Eletriptan hydrobromide
|
177834-92-3 |
Eletriptan (UK 116044) is a potent, selective, and orally active 5-HT1B/1D receptor agonist; significantly increases occluded wedge pressure and mean pulmonary artery pressure in vivo, with no significant coronary artery constriction, and obstructive coronary artery disease; displays antimigraine activity. |
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