化学性质:
规格 | 10mg 50mg |
CAS | 1092776-63-0 |
别名 |
|
化学名 | (E)-(6,6-dimethyl-5,6-dihydroimidazo[2,1-b]thiazol-3-yl)methyl N,N'-dicyclohexylcarbamimidothioate dihydrochloride |
分子式 | C21H34N4S2.2HCl |
分子量 | 479.57 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
IT1t dihydrochloride is a potent antagonist of CXCR4 with IC50 value of 8.0 nM [1].
C-X-C chemokine receptor type 4 (CXCR4) is an α-chemokine receptor for chemokine CXCL12. CXCR4 functions as a coreceptor for human immunodeficiency virus (HIV) envelope protein gp-120 and mediates infection of T-cells by HIV [1].
IT1t dihydrochloride is a potent CXCR4 antagonist. In binding assays, IT1t exhibited IC50 values of 8.0 and 11.0 nM for human and rat CXCR4, respectively. In Ca2+ mobilization assays, IT1t exhibited IC50 value of 1.1 nM. In the HIV attachment assay, IT1t inhibited HIV attachment with IC50 and IC90 values of 7 and 100 nM, respectively and inhibited both CXCR4/CXCL12 and CXCR4/gp120 interactions. IT1t exhibited 32% oral bioavailability.
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