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TRPV1 antagonist 3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TRPV1 antagonist 3图片

TRPV1 antagonist 3 (Compound 7q) 是一种有效的TRPV1拮抗剂,对 capsaicin 的IC50值为 2.66 nM。 TRPV1 antagonist 3 具有模式选择性和良好的口服生物利用度 (F = 60%),可透过血脑屏障。
生物活性

TRPV1 antagonist 3 (Compound 7q) is a potentTRPV1antagonist with anIC50of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant[1].

IC50& Target

hTRPV1

2.66 nM (IC50)

TRPM8

7.45 μM (IC50)

体外研究
(In Vitro)

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].

体内研究
(In Vivo)

TRPV1 antagonist 3 (Compound 7q) (0-30 mg/kg; i.p.; 30 min) shows anti-nociceptive effect mainly mediated by blocking CAP-activated channel[1].
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].

Animal Model:KM male mice (18-22 g), capsaicin, acetic acid, and thermal induced pain model[1]
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.).
Administration:Intraperitoneally administration; 30 min
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.
Animal Model:Spragur-Dawley male rats (220-250 g)[1]
Dosage:10 mg/kg or 20 mg/kg
Administration:Intravenous injection of 10 mg/kg or oral dose of 20 mg/kg (Pharmacokinetic Analysis)
Result:In vivo pharmacokinetic parameters of TRPV1 antagonist 3 in rats (n=3)[1]
ParametersIVPO
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 ± 2.3371.133 ± 0.358
V (L/kg)0.003 ± 0.0010.016 ± 0.006
CL (L/h/kg)0.024 ± 0.0130.022 ± 0.01
Tmax(h)0.711 ± 0.144
Cmax(ng/mL)311.377 ± 108.017
AUC0-inf(ng/mL*h)495.955 ± 214.634598.873 ± 212.319
MRT (h)
分子量

391.53

Formula

C23H25N3OS

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

 
 
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