A 784168


Catalog No. Size PriceQuantity
M22493-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

A 784168 is a potent antagonist of TRPV1 receptor with pKi value of 7.15 . The transient receptor potential cation channel subfamily V member 1 (TrpV1) receptor is a nonselective cation channel and distributes throughout the nervous system. TrpV1 receptor is activated by a wide variety of physical and chemical stimuli . A 784168 is a potent TRPV1 receptor antagonist with pKi value of 7.15 for recombinant hTRPV1 receptor. In the Ca2+ flux assay, A 784168 inhibited 50 nM CAP-induced calcium flux with pIC50 value of 7.13 of the recombinant hTRPV1 receptor . A 784168 inhibited TRPV1 activation by 50 nM capsaicin, pH 5.5, 3 μM NADA and 10 μM anandamide with IC50 values of 25, 14, 33.7, 35.1 nM, respectively. In rat dorsal root ganglion neurons, A 784168 inhibited 1 μM capsaicin-induced currents with IC50 value of 10 nM . In CFA-induced thermal hyperalgesia, A-784168 (30 μM/kg) reduced capsaicin-induced nocifensive behaviors with ED50 value of 10 μM/kg . In rats, A 784168 inhibited 1% formalin-induced secondary mechanical hyperalgesia and allodynia in the contralateral and ipsilateral paws .

Product information

CAS Number: 824982-41-4

Molecular Weight: 479.40

Formula: C19H15F6N3O3S

Chemical Name: N-(4-trifluoromethanesulfonylphenyl)-3'-(trifluoromethyl)-3,6-dihydro-2H-[1,2'-bipyridine]-4-carboxamide

Smiles: O=C(NC1=CC=C(C=C1)S(=O)(=O)C(F)(F)F)C1CCN(CC=1)C1=NC=CC=C1C(F)(F)F

InChiKey: SDUAWRFBHRAFBM-UHFFFAOYSA-N

InChi: InChI=1S/C19H15F6N3O3S/c20-18(21,22)15-2-1-9-26-16(15)28-10-7-12(8-11-28)17(29)27-13-3-5-14(6-4-13)32(30,31)19(23,24)25/h1-7,9H,8,10-11H2,(H,27,29)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.

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