B6573-10mg | WIN 64338 hydrochloride [163727-74-0] Clinisciences

Background

WIN 64338 hydrochloride is a potent and competitive antagonist of bradykinin B2 receptor [1].

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 [1]. In iris sphincter isolated from rabbit, WIN 64338 (1-10 μM) inhibited contractile responses evoked by bradykinin with pKB value of 6.6 [2]. In guinea-pig tracheal smooth muscle cells, WIN 64338 inhibited inositol phosphate formation induced by bradykinin [3].

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 [2].

References:
[1]. Sawutz DG, Salvino JM, Dolle RE, et al. The nonpeptide WIN 64338 is a bradykinin B2 receptor antagonist. Proc Natl Acad Sci U S A, 1994, 91(11): 4693-4697.
[2]. Hall JM, Figini M, Butt SK, et al. Inhibition of bradykinin-evoked trigeminal nerve stimulation by the non-peptide bradykinin B2 receptor antagonist WIN 64338 in vivo and in vitro. Br J Pharmacol, 1995, 116(8): 3164-3168.
[3]. Scherrer D, Schmidlin F, Lach E, et al. Effect of WIN 64338, a B2 bradykinin receptor antagonist on guinea-pig tracheal smooth muscle cells in culture. Fundam Clin Pharmacol, 1998, 12(2): 188-193.

Chemical Properties

Physical Appearance	White solid
Storage	Store at -20°C
M.Wt	783.95
Cas No.	163727-74-0
Formula	C₄₅H₆₈ClN₄OP·HCl
Solubility	<58.8mg/ml in DMSO
Chemical Name	(S,E)-(N,N'-dicyclohexylcarbamimidoyl)(3-(naphthalen-2-yl)-1-oxo-1-((4-((tributylphosphonio)methyl)phenyl)amino)propan-2-yl)amide dihydrochloride
SDF	Download SDF
Canonical SMILES	CCCC[P+](CCCC)(CC1=CC=C(NC([C@]([N-]/C(NC2CCCCC2)=N\C3CCCCC3)(10)CC4=CC5=CC=CC=C5C=C4)=O)C=C1)CCCC.Cl.Cl
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Purity = 98.00%

COA (Certificate Of Analysis)
MSDS (Material Safety Data Sheet)

Chemical structure

WIN 64338 hydrochloride [163727-74-0]

Referência B6573-10mg

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Background

Chemical Properties

Quality Control

Chemical structure

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