TRPV1 antagonist 3
Based on 1 Customer Validation
TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant.
For research use only. We do not sell to patients.
- Purity: 99.30%
- CAS No.: 2765294-54-8
- Formula: C23H25N3OS
- Molecular Weight:391.53
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Biological Activity
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hTRPV1 2.66 nM (IC50) |
TRPM8 7.45 μM (IC50) |
TRPV1 antagonist 3 (Compound 7q) is highly selective for the TRPV1 receptor relative to other TRP channels[1].
TRPV1 antagonist 3 shows acceptable aqueous solubility (solubility at pH 7.4 = 26 μg/mL) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TRPV1 antagonist 3 (0-100 mg/kg; i.g.) had no obvious thermal effect in rats[1].
TRPV1 antagonist 3 (10 mg/kg; i.v.) shows a good concentration in the brain at 0.5 h, with value of 2311 ng/g, and has good CNS penetration, with a brain/plasma ratio of 1.66[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KM male mice (18-22 g), capsaicin, acetic acid, and thermal induced pain model[1]
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Dosage:3, 10, and 30 mg/kg. 20 μL of solution of capsaicin (16 mg/20 mL) was injected s.c. under the skin of the dorsal surface of the right hind paw, or injected with 0.6% acetic acid (0.1 mL/10 g/mouse i.p.).
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Administration:Intraperitoneally administration; 30 min
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Result:In capsaicin-induced nociception, licking time decreased significantly in a dose-dependent manner. In acid-induced nociception, no significant anti-nociceptive activities were found compared with the control (SB-705498 and BCTC) at all dosage. In thermal-induced nociception, the latency time of nociceptive responses was increased at the doses of 10 and 30 mg/kg.
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Animal Model:Spragur-Dawley male rats (220-250 g)[1]
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Dosage:10 mg/kg or 20 mg/kg
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Administration:Intravenous injection of 10 mg/kg or oral dose of 20 mg/kg (Pharmacokinetic Analysis)
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Result:In vivo pharmacokinetic parameters of TRPV1 antagonist 3 in rats (n=3)[1]
Parameters IV PO t1/2 (h) 0.106 ± 0.076 t1/2, ka (h) 0.462 ± 0.096 t1/2, k10 (h) 0.527 ± 0.106 ka (1/h) 1.65 ± 0.364 k10 (1/h) 12.076 ± 2.337 1.133 ± 0.358 V (L/kg) 0.003 ± 0.001 0.016 ± 0.006 CL (L/h/kg) 0.024 ± 0.013 0.022 ± 0.01 Tmax (h) 0.711 ± 0.144 Cmax (ng/mL) 311.377 ± 108.017 AUC 0-inf (ng/mL*h) 495.955 ± 214.634 598.873 ± 212.319