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Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC 50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant.
Appearance:Solid
IC50& Target:hTRPV1 2.66 nM (IC 50 ) TRPM8 7.45 μM (IC 50 )
In Vitro:TRPV1 antagonist 3 (Compound 7q) is highly selective for the TRPV1 receptor relative to other TRP channels. TRPV1 antagonist 3 shows acceptable aqueous solubility (solubility at pH 7.4 = 26 μg/mL). MCE has not independently confirmed the accurac
In Vivo:TRPV1 antagonist 3 (Compound 7q) (0-30mg/kg; i.p.; 30 min) shows anti-nociceptive effect mainly mediated by blocking CAP-activated channel. TRPV1 antagonist 3 (0-100mg/kg; i.g.) had no obvious thermal effect in rats. TRPV1 antagonist 3 (10 mg/
Biological Activity:TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC 50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant.
| Canonical Smiles | CC(C1=CC=CC(NC(N2CCC[C@H]2C3=NC=C(S3)C4=CC=CC=C4)=O)=C1)C |
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| Molecular Weight | 391.53 |
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View spec sheet →| Solubility | DMSO : ≥ 100 mg/mL (255.41 mM) |
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