239821
CXCR4 Antagonist II
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.
别名:
CXCR4 Antagonist II, 1,3-Dicyclohexyl-2-(3-methyl-6,6-dimethyl-5,6-dihydroimidazo[1,2-b]thiazole)-2-thiopseudourea, HCl, Fusin Antagonist II, IT1t
产品名称
CXCR4 Antagonist II, 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.
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
color
white
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
Disclaimer
Toxicity: Standard Handling (A)
Other Notes
Wu, B., et al. 2010. Science330, 1066.
Thoma, G., et al. 2008. J. Med. Chem.51, 7915.
Thoma, G., et al. 2008. J. Med. Chem.51, 7915.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
General description
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.
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
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