1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. Cloperastine fendizoate

Cloperastine fendizoate 

Cat. No.: HY-B2179 Purity: 99.38%
Handling Instructions

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

For research use only. We do not sell to patients.

Cloperastine fendizoate Chemical Structure

Cloperastine fendizoate Chemical Structure

CAS No. : 85187-37-7

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
100 mg USD 60 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

27 nM (K+ currents)[1]

In Vitro

Cloperastine inhibits the hERG K+ currents in a concentrationdependent manner with IC50 value of 27±3 nM[1]. 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[2].

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[1]. 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[2].

Molecular Weight

648.19

Formula

C₄₀H₃₈ClNO₅

CAS No.

85187-37-7

SMILES

O=C(O)C1=CC=CC=C1C(C2=CC(C3=CC=CC=C3)=C(O)C=C2)=O.ClC4=CC=C(C(C5=CC=CC=C5)OCCN6CCCCC6)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (46.28 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5428 mL 7.7138 mL 15.4276 mL
5 mM 0.3086 mL 1.5428 mL 3.0855 mL
10 mM 0.1543 mL 0.7714 mL 1.5428 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

Cloperastine fendizoatePotassium ChannelKcsAInhibitorinhibitorinhibit

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Cloperastine fendizoate
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