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

产品编号:4156367
规格: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.
CAS NO:1258011-83-4
包装规格:10 MG
产品类别:进口试剂
品牌:Sigma-Aldrich
优惠价:立即咨询
产品价格
产品编号包装单位单价(元)国内现货国外库存询价单
415636710 MG2230
产品别名

1258011-83-4

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

1,3-Dicyclohexyl-2-(3-methyl-6,6-dimethyl-5,6-dihydroimidazo[1,2-b]thiazole)-2-thiopseudourea, HCl, Fusin Antagonist II, IT1t

基本信息
Empirical Formula【经验(实验)分子式】
C21H34N4S2 · xHCl
Molecular weight
406.65 (free base basis)
General description【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 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.
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.
Warning【警告】
Toxicity: Standard Handling (A)
Reconstitution【重悬】
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes【其他说明】
Wu, B., et al. 2010. Science330, 1066.
Thoma, G., et al. 2008. J. Med. Chem.51, 7915.
Legal Information【法律信息】
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
产品性质
Quality Level【质量水平】
100
Assay【测定】
≥95% (HPLC)
form【形式】
solid
manufacturer/tradename
Calbiochem®
storage condition【储存条件】
OK to freeze
desiccated (hygroscopic)
protect from light
color【颜色】
white
solubility【溶解性】
DMSO: 50 mg/mL
shipped in【运输】
ambient
storage temp.【储存温度】
−20℃
packaging【包装】
Packaged under inert gas
安全信息
Storage Class Code【储存分类代码】
11 - Combustible Solids
WGK
WGK 1
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