Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TRPV1 antagonist 3 (Compound 7q) is a highly potent antagonist of the TRPV1 receptor with an IC50 of 2.66 nM against capsaicin. It exhibits selectivity towards its mode of action and is orally bioavailable (with a bioavailability of 60%). Additionally, it can penetrate the central nervous system [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 10-14 weeks | $ 987.00 | |
50 mg | 10-14 weeks | $ 1,360.00 | |
100 mg | 10-14 weeks | $ 2,190.00 |
Description | TRPV1 antagonist 3 (Compound 7q) is a highly potent antagonist of the TRPV1 receptor with an IC50 of 2.66 nM against capsaicin. It exhibits selectivity towards its mode of action and is orally bioavailable (with a bioavailability of 60%). Additionally, it can penetrate the central nervous system [1]. |
In vitro | TRPV1 antagonist 3 (Compound 7q) exhibits high selectivity toward the TRPV1 receptor compared to other TRP channels [1]. It demonstrates acceptable aqueous solubility, with a solubility of 26 μg/mL at pH 7.4 [1]. |
In vivo | TRPV1 antagonist 3 (Compound 7q), administered intraperitoneally (0-30 mg/kg; 30 min before testing), exhibits significant anti-nociceptive effects primarily by inhibiting the capsaicin (CAP)-activated channel, with no evident thermal impact when given orally (0-100 mg/kg). A notable concentration of 2311 ng/g was observed in the brain 0.5 hours after intravenous administration (10 mg/kg), indicating effective central nervous system (CNS) penetration, evidenced by a brain/plasma ratio of 1.66. In experiments involving KM male mice (18-22 g) subjected to capsaicin, acetic acid, and thermal pain models, results showed a dose-dependent decrease in licking time in capsaicin-induced pain and an increase in latency time for thermal-induced nociceptive responses at doses of 10 and 30 mg/kg. However, no significant anti-nociceptive activity was observed in acid-induced pain compared to controls. Pharmacokinetic analysis in Sprague-Dawley male rats (220-250 g) following either intravenous (10 mg/kg) or oral (20 mg/kg) administration revealed various absorption and elimination parameters, demonstrating the compound's favorable pharmacokinetics, including a half-life suggesting rapid clearance from the body. |
Molecular Weight | 391.53 |
Formula | C23H25N3OS |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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TRPV1 antagonist 3 inhibitor inhibit