Identification | Back Directory | [Name]
JYL1421 | [CAS]
401907-26-4 | [Synonyms]
JYL1421 SC 0030 JYL-1421
(SC-0030) inhibit,JYL-1421,Inhibitor,JYL 1421,SC-0030,TRP Channel,Transient receptor potential channels,JYL1421,SC0030 Methanesulfonamide, N-[4-[[[[[[4-(1,1-dimethylethyl)phenyl]methyl]amino]thioxomethyl]amino]methyl]-2-fluorophenyl]- | [Molecular Formula]
C20H26FN3O2S2 | [MDL Number]
MFCD29770787 | [MOL File]
401907-26-4.mol | [Molecular Weight]
423.57 |
Hazard Information | Back Directory | [Uses]
JYL 1421 is a TRPV1 receptor antagonist, with an IC50 of 8 nM. | [in vivo]
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[1]. | [References]
[1] Jakab B, et al. Pharmacological characterization of the TRPV1 receptor antagonist JYL1421 (SC0030) in vitro and in vivo in the rat. Eur J Pharmacol. 2005 Jul 4;517(1-2):35-44. DOI:10.1016/j.ejphar.2005.05.002 |
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