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AMG 21629 is a potent and selective TRPV1 antagonist. Blocks Ca2+ uptake by CHO cells expressing TRPV1 receptors (IC50 values are 0.6 and 0.8 nM for capsaicin and acid-induced Ca2+ uptake, respectively). Exhibits >4000-fold selectivity for TRPV1 over other TRP channels. Blocks capsaicin-induced flinch response and causes hyperthermia in rats. Orally available and non-CNS penetrant.
| Molecular Weight | 472.42 |
| Formula | C22H19F3N6O3 |
| CAS Number | 939040-79-6 |
| Solubility (25°C) | DMSO 23.62 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related TRP Channel Products |
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SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1. |
| HC-030031
HC-030031 is a selective TRPA1 blocker, antagonizing TRPA1-mediated calcium influx induced by AITC and formalin (IC50 = 6.2 and 5.3 μM, respectively). |
| AMG-517
AMG 517 is a potent and selective TRPV1 antagonist, antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM. |
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| Phenazopyridine hydrochloride
Phenazopyridine HCl is a competitive SARM1 inhibitor as well as a TRPM8 antagonist with an IC50 for SARM1 inhibition of 145 μM. It has local anesthetic/analgesic activity and can be used in studies related to traumatic brain injury, peripheral neuropathy, and neurodegenerative diseases. |
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