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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related TRP Channel Products |
|---|
| N-Oleoyl glutamine
N-oleoyl-glutamine is a PM20D1-regulated N-acyl amino acids (NAAs). |
| N-Oleoyl valine
N-Oleoyl valine is a N-acyl valine compound that acts as a TRPV3 receptor antagonist. |
| TAT-M2NX
TAT-M2NX (tatM2NX) is a TRPM2 inhibitor with specific neuroprotective activity in male mice. |
| SOR-C13
SOR-C13, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. |
| GsMTx4 TFA
GsMTx4 TFA is a spider venom peptide that selectively inhibits cation permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. In addition, GsMTx4 TFA blocks cation-selective stretch-activated channels (SACs) and attenuates lysophosphatidylcholine (LPC)-induced astrocytotoxicity and microglial cell reactivity. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
