CXCR4 Antagonist II-CAS 1258011-83-4-Calbiochem

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一般描述

A thiopseudourea compound that acts as a selective and highly potent CXCR4/Fusin antagonist (IC₅₀= 1.1 nM against SDF-1/CXCL12-induced Ca²⁺mobilization in CEM cells) and effectively targets CXCR4-mediated binding of both CXCL12 (IC₅₀= 8 and 11 nM in competitive binding assays using human CEM and rat IR983F membrane, respectively) and HIV gp120 (IC₅₀= 7 nM in HIV attachment assays). Shown to be orally available in rat with goodin vivopharmacokinetics (32% availability, t_max= 0.5 h, C_max= 18 ng/ml, t_1/2= 7.6 h, based on an oral dose of 1 mg/kg). Comparing to AMD3100 (Cat. No. 239820), CXCR4 Antagonist II is ~30-times more potent as a CXCR4-CXCL12 interaction blocker, while being ~2-fold less potent in blocking gp120-mediated HIV attachment.
A thiopseudourea compound that acts as a selective and highly potent CXCR4/Fusin antagonist (IC₅₀= 1.1 nM against SDF-1/CXCL12-induced Ca²⁺mobilization in CEM cells) and effectively targets CXCR4-mediated binding of both CXCL12 (IC₅₀= 8 and 11 nM in competitive binding assays using human CEM and rat IR983F membrane, respectively) and HIV gp120 (IC₅₀= 7 nM in HIV attachment assays). Shown to be orally available in rat with goodin vivopharmacokinetics (32% availability, t_max= 0.5 h, C_max= 18 ng/ml, t_1/2= 7.6 h, based on an oral dose of 1 mg/kg). Comparing to AMD3100 (Cat. No. 239820), CXCR4 Antagonist II is ~30-times more potent as a CXCR4-CXCL12 interaction blocker, while being ~2-fold less potent in blocking gp120-mediated HIV attachment.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Wu, B., et al. 2010.Science330,1066.
Thoma, G., et al. 2008.J. Med. Chem.51,7915.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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