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JYL 1421

Catalog No. T15634   CAS 401907-26-4
Synonyms: SC 0030

JYL 1421 (SC 0030) is an antagonist of TRPV1 receptor (IC50 = 8 nM).

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JYL 1421 Chemical Structure
JYL 1421, CAS 401907-26-4
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25 mg 6-8 weeks $ 767.00
50 mg 6-8 weeks $ 997.00
100 mg 6-8 weeks $ 1,570.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description JYL 1421 (SC 0030) is an antagonist of TRPV1 receptor (IC50 = 8 nM).
Targets&IC50 TRPV1:8 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[1].
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)[1].
Synonyms SC 0030
Molecular Weight 423.57
Formula C20H26FN3O2S2
CAS No. 401907-26-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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.

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Keywords

JYL 1421 401907-26-4 Membrane transporter/Ion channel TRP/TRPV Channel JYL-1421 inhibit Inhibitor SC0030 JYL1421 SC 0030 TRP Channel Transient receptor potential channels SC-0030 inhibitor

 

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