WIN 64338 hydrochloride is a potent and competitive antagonist of bradykinin B2 receptor . Bradykinin B2 receptor is a G-protein coupled receptor for bradykinin. Bradykinin is an inflammatory nonapeptide and plays a critical role in edema, vasodilation, pain fiber stimulation and smooth muscle spasm. WIN 64338 hydrochloride is a potent and competitive bradykinin B2 receptor antagonist. In human IMR-90 cells, WIN 64338 inhibited bradykinin binding to the bradykinin B2 receptor with Ki value of 64 nM and inhibited Ca2+ efflux stimulated by bradykinin with pA2 value of 7.1 in a competitive way. WIN 64338 inhibited guinea pig ileum contractility induced by bradykinin with pA2 value of 8.2 and also inhibited acetyicholine-induced contractility . In iris sphincter isolated from rabbit, WIN 64338 (1-10 μM) inhibited contractile responses evoked by bradykinin with pKB value of 6.6 . In guinea-pig tracheal smooth muscle cells, WIN 64338 inhibited inositol phosphate formation induced by bradykinin . In guinea-pigs, WIN 64338 (30 nM) significantly inhibited the increases in plasma extravasation induced by bradykinin via the release of tachykinins from the trigeminal nerve .

Product information

CAS Number: 163727-74-0

Molecular Weight: 783.94

Formula: C45H69Cl2N4OP

Chemical Name: tributyl({4-[(2S)-2-{[(E)-N,N'-dicyclohexylcarbamimidoyl]azanidyl}-3-(naphthalen-2-yl)propanamido]phenyl}methyl)phosphanium dihydrochloride

Smiles: Cl.Cl.CCCC[P+](CC1C=CC(=CC=1)NC(=O)[C@H](CC1=CC2=CC=CC=C2C=C1)[N-]/C(/NC1CCCCC1)=N\C1CCCCC1)(CCCC)CCCC

InChiKey: YYJGBEZPVOUBMJ-KRFCICRISA-N

InChi: InChI=1S/C45H67N4OP.2ClH/c1-4-7-30-51(31-8-5-2,32-9-6-3)35-36-25-28-42(29-26-36)46-44(50)43(34-37-24-27-38-18-16-17-19-39(38)33-37)49-45(47-40-20-12-10-13-21-40)48-41-22-14-11-15-23-41;;/h16-19,24-29,33,40-41,43H,4-15,20-23,30-32,34-35H2,1-3H3,(H2-,46,47,48,49,50);2*1H/t43-;;/m0../s1

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

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