239821 Sigma-AldrichCXCR4 Antagonist II - CAS 1258011-83-4 - Calbiochem
The CXCR4 Antagonist II, also referenced under CAS 1258011-83-4, controls the biological activity of CXCR4. This small molecule/inhibitor is primarily used for Cell Signaling applications.
More>> The CXCR4 Antagonist II, also referenced under CAS 1258011-83-4, controls the biological activity of CXCR4. This small molecule/inhibitor is primarily used for Cell Signaling applications. Less<<MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Synonyms: IT1t, 1,3-Dicyclohexyl-2-(3-methyl-6,6-dimethyl-5,6-dihydroimidazo[1,2-b]thiazole)-2-thiopseudourea, HCl, Fusin Antagonist II
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Overview
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Key Spec Table
| CAS # | Empirical Formula |
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| 1258011-83-4 | C₂₁H₃₄N₄S₂ • HCl |
| Description | |
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| Overview | 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 good in vivo pharmacokinetics (32% availability, tmax = 0.5 h, Cmax= 18 ng/ml, t1/2 = 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. |
| Catalogue Number | 239821 |
| Brand Family | Calbiochem® |
| Synonyms | IT1t, 1,3-Dicyclohexyl-2-(3-methyl-6,6-dimethyl-5,6-dihydroimidazo[1,2-b]thiazole)-2-thiopseudourea, HCl, Fusin Antagonist II |
| References | |
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| References | Wu, B., et al. 2010. Science 330, 1066. Thoma, G., et al. 2008. J. Med. Chem. 51, 7915. |
| Product Information | |
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| CAS number | 1258011-83-4 |
| Form | White solid |
| Hill Formula | C₂₁H₃₄N₄S₂ • HCl |
| Chemical formula | C₂₁H₃₄N₄S₂ • HCl |
| Hygroscopic | Hygroscopic |
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| Quality Level | MQ100 |
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| Purity | ≥95% by HPLC |
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| Packaged under inert gas | Packaged under inert gas |
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| Specifications |
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| Global Trade Item Number | |
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| Catalogue Number | GTIN |
| 239821 | 0 |
Documentation
CXCR4 Antagonist II - CAS 1258011-83-4 - Calbiochem SDS
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CXCR4 Antagonist II - CAS 1258011-83-4 - Calbiochem Certificates of Analysis
| Title | Lot Number |
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| 239821 |
References
| Reference overview |
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| Wu, B., et al. 2010. Science 330, 1066. Thoma, G., et al. 2008. J. Med. Chem. 51, 7915. |