JYL 1421

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JYL 1421 是 TRPV1 受体拮抗剂 (IC50 = 8 nM)。

JYL 1421 is an antagonist of TRPV1 receptor (IC50 = 8 nM).(In Vitro):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.(In Vivo):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).

Incubation with JYL 1421 for 5 min concentration-dependently inhibits the capsaicin (330 nM)-evoked Ca2+ accumulation. 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. The IC50 value is 8 nM for JYL 1421. Meanwhile, the effect of capsazepine is markedly smaller, it induces 41.7% inhibition in 1 μM concentration, but this inhibitory effect does not increase further in 10 μM and does not reach 50%.

Instillation of 50 μL capsaicin solution (10 μg/mL) into the left eye of the rat evokes 12.9±1.3 wiping movements within 3 min. Pretreating the rats with 0.4 or 1 mg/kg i.p. JYL 1421 does not influence significantly the wiping behavior, but 2-5 mg/kg dose-dependently reduces the number of wiping movements. The ID50 value is 4.6 mg/kg. The mean arterial pressure of untreated rats is 109.9±4.2 Hgmm (n=6). One 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 dose-dependently inhibits the capsaicin-induced fall in blood pressure 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.

SC 0030

Membrane Transporter/Ion Channel

TRP/TRPV Channel

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401907-26-4

423.57

C20H26FN3O2S2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (236.09 mM)

CC(C)(C)c1ccc(CNC(=S)NCc2ccc(NS(C)(=O)=O)c(F)c2)cc1

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(-20℃)

With Ice Pack

≥ 2 years