A TRPV1 antagonist
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JYL1421

Item No. 20458

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[[[[[[4-(1,1-dimethylethyl)phenyl]methyl]amino]thioxomethyl]amino]methyl]-2-fluorophenyl]-methanesulfonamide
CAS Number
401907-26-4
Molecular Formula
C20H26FN3O2S2
Formula Weight
423.6
Purity
≥95%
Formulation
A crystalline solid
λmax
225 nm
SMILES
CC(C)(C)C1=CC=C(CNC(NCC2=CC(F)=C(NS(C)(=O)=O)C=C2)=S)C=C1
InChi Code
InChI=1S/C20H26FN3O2S2/c1-20(2,3)16-8-5-14(6-9-16)12-22-19(27)23-13-15-7-10-18(17(21)11-15)24-28(4,25)26/h5-11,24H,12-13H2,1-4H3,(H2,22,23,27)
InChi Key
DUHBVFMCIJLUJX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $54

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    1 mg

    $96

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    5 mg

    $367

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    10 mg

    $470

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    Product Description

    JYL1421 is an antagonist of transient receptor potential vanilloid 1 (TRPV1).1 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).2 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.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, Y., Szabo, T., Welter, J.D., et al. High affinity antagonists of the vanilloid receptor. Mol. Pharmacol. 62(4), 947-956 (2002).

    2. Jakab, B., Helyes, Z., Varga, A., et al. Pharmacological characterization of the TRPV1 receptor antagonist JYL1421 (SC0030) in vitro and in vivo in the rat. Eur. J. Pharmacol. 517(1-2), 35-44 (2005).

    3. Garami, A., Shimansky, Y.P., Pakai, E., et al. Contributions of different modes of TRPV1 activation to TRPV1 antagonist-induced hyperthermia. J. Neurosci. 30(4), 1435-1440 (2010).