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AM-0902 is a potent, selective antagonist of TRPA1 with IC50s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively. AM-0902 is highly permeable (average Papp=44.5 μcm/s in MDCK cells), an unlikely substrate for P-gp (efflux ratio=1.3 in P-gp overexpressing MDCK cells), and demonstrates good solubility (PBS pH 7.4: 226 μM, SIF: 248 μM). AM-0902 shows good selectivity over other TRP channels, as no activity is observed against human TRPV1 or TRPV4, or rat TRPV1, TRPV3, or TRPM8, at concentrations up to 10 μM. AM-0902 inhibits 45Ca2+ flux upon activation of rat TRPA1 with methylglyoxal with an IC50 of 0.019 μM.
| Molecular Weight | 370.79 |
| Formula | C17H15ClN6O2 |
| CAS Number | 1883711-97-4 |
| Form | Solid |
| Solubility (25°C) | 150 mg/mL in DMSO |
| 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
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. |
| Icilin
Icilin is a synthetic super-agonist of the transient receptor potential M8 (TRPM8) ion channel. |
| 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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