A TRPV1 antagonist; inhibits capsaicin-induced calcium uptake in CHO cells expressing rat TRPV1 (EC50 = 9.2 nM); inhibits capsaicin-induced release of somatostatin

JYL1421 – 10 mg

Brand:
Cayman
CAS:
401907-26-4
Storage:
-20
UN-No:
Non-Hazardous - /

JYL1421 is an antagonist of transient receptor potential vanilloid 1 (TRPV1).{48180} It inhibits calcium uptake induced by capsaicin (Item Nos. 92350 | 10010743) in CHO cells expressing rat TRPV1 (EC50 = 9.2 nM). JYL1421 inhibits capsaicin-induced release of the neuropeptides somatostatin, substance P (Item No. 24035), and calcitonin gene-related peptide (CGRP) from isolated rat trachea (IC50s = 227-491 nM).{48181} It inhibits capsaicin-induced hypothermia and hypotension in rats when administered at doses of 2 and 0.4 mg/kg, respectively. JYL1421 (2 mg/kg) also reduces the number of wiping movements induced by ocular administration of capsaicin in rats. Unlike several other TRPV1 antagonists, JYL1421 does not induce hyperthermia in rats when administered at doses ranging from 1.02 to 32.77 μmol/kg.{48182}  

 

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Description

A TRPV1 antagonist; inhibits capsaicin-induced calcium uptake in CHO cells expressing rat TRPV1 (EC50 = 9.2 nM); inhibits capsaicin-induced release of somatostatin, substance P, and CGRP from isolated rat trachea (IC50s = 227-491 nM); inhibits capsaicin-induced hypothermia and hypotension in rats at 2 and 0.4 mg/kg, respectively; reduces the number of wiping movements induced by ocular administration of capsaicin in rats at 2 mg/kg

Formal name: N-[4-[[[[[[4-(1,1-dimethylethyl)phenyl]methyl]amino]thioxomethyl]amino]methyl]-2-fluorophenyl]-methanesulfonamide

Synonyms: 

Molecular weight: 423.6

CAS: 401907-26-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cell Biology|Cell Signaling|Calcium Mobilization||Research Area|Neuroscience|Neuroendocrinology||Research Area|Neuroscience|Pain Research

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