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IT1t dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
IT1t dihydrochloride图片
CAS NO:1092776-63-0
规格:98%
分子量:479.57
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
CXCR4 antagonist, potent
CAS:1092776-63-0
分子式:C21H34N4S2.2HCl
分子量:479.57
纯度:98%
存储:Store at -20°C

Background:

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.


参考文献:
[1].  Thoma G, Streiff MB, Kovarik J, et al. Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo. J Med Chem, 2008, 51(24): 7915-7920.