Cloperastine Fendizoate

Cloperastine fendizoate inhibits the hERG K+ currents in a concentration-dependent manner with an IC50 value of 27 nM.

Product information

CAS Number: 85187-37-7

Molecular Weight: 648.19

Formula: C40H38ClNO5

Chemical Name: o-((2'-Hydroxy(1,1'-biphenyl)-4-yl)carbonyl)benzoic acid, compoundwith 1-(2-(4-chlorobenzhydryloxy)ethyl)piperidine (1:1)

Smiles: OC(=O)C1=CC=CC=C1C(=O)C1=CC(C2C=CC=CC=2)=C(O)C=C1.ClC1C=CC(=CC=1)C(OCCN1CCCCC1)C1C=CC=CC=1

InChiKey: PXZFKAKWSHBDCP-UHFFFAOYSA-N

InChi: InChI=1S/C20H24ClNO.C20H14O4/c21-19-11-9-18(10-12-19)20(17-7-3-1-4-8-17)23-16-15-22-13-5-2-6-14-22;21-18-11-10-14(12-17(18)13-6-2-1-3-7-13)19(22)15-8-4-5-9-16(15)20(23)24/h1,3-4,7-12,20H,2,5-6,13-16H2;1-12,21H,(H,23,24)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 10 mg/mL (15.43 mM; Need ultrasonic)

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

How to use

In Vitro:

Cloperastine inhibits the hERG K+ currents in a concentrationdependent manner with IC50 value of 27±3 nM. Among the antitussive agents, Cloperastine, which possesses antitussive and antiedemic activity, also relaxes the bronchial musculature. Cloperastine is a drug with a central antitussive effect, and is also endowed with an antihistaminic and papaverine-like activity similar to codeine but without its narcotic effects.

In Vivo:

In the anesthetized guinea pigs, Cloperastine at a therapeutic dose of 1 mg/kg prolonged the QT interval and monophasic action potential (MAP) duration without affecting PR interval or QRS width. Cloperastine hydrochloride shows relatively low acute toxicity when administered by the intraperitoneal route in rats and mice, and shows minor toxicity by the oral route when administered as Cloperastine fendizoate, the LD50 in rats and mice for the two administration routes exceeds 1000 and 2000 mg/kg, respectively.

References:

1. Takahara A, et al. Effects of the antitussive drug cloperastine on ventricular repolarization in halothane-anesthetized guinea pigs. J Pharmacol Sci. 2012;120(3):165-75.
2. Catania MA, et al. Pharmacological and clinical overview of cloperastine in treatment of cough. Ther Clin Risk Manag. 2011;7:83-92.

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