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JYL 1421
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。
JYL 1421图片
CAS NO:401907-26-4
包装:10 mg
市场价:9450元

产品名称
SC 0030
产品介绍
JYL 1421 是 TRPV1 的拮抗剂 (IC50 = 8 nM)。

产品描述

JYL 1421 is an antagonist of TRPV1 receptor (IC50 = 8 nM).

体外活性

JYL 1421(5 min) inhibits the capsaicin (330 nM)-evoked Ca2+ accumulation in a concentration-dependent manner. The inhibitory effect of the lowest concentration (5 nM) of JYL 1421 reaches the level of significance and 1 μM almost abolishes the response, only 3.1±0.65% of the first capsaicin-induced Ca2+ influx could be observed[1].

体内活性

1 and 2 μg/kg capsaicin i.v. injection evokes a transient drop of blood pressure by 47.4±4.7 and 59.6±4.2 Hgmm (n=6), respectively. Both applied doses of JYL 1421 (0.4 and 1.6 mg/kg) fail to evoke hypotension. JYL 1421 inhibits the capsaicin-induced fall in blood pressure in a dose-dependent manner as shown by the need for higher capsaicin doses to elicit the reflex hypotension after JYL 1421 administration than before treatment. Capsazepine fails to induce a significant inhibition of the capsaicin-evoked hypotension up to a dose of 2 mg/kg. Instillation of capsaicin solution (50 μL, 10 μg/mL) into the left eye of the rat evokes 12.9±1.3 wiping movements within 3 min. Pretreating the rats with JYL 1421(0.4 or 1 mg/kg i.p.) does not influence significantly the wiping behavior, but 2-5 mg/kg JYL 1421 reduces the number of wiping movements in a dose-dependent manner with an ID50 value of 4.6 mg/kg. The mean arterial pressure of untreated rats is 109.9±4.2 Hgmm (n=6)[1].

Cas No.

401907-26-4

分子式

C20H26FN3O2S2

分子量

423.57

别名

SC 0030

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years