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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
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍

化学性质

Physical AppearanceOff-white solid
StorageStore at -20°C
M.Wt479.57
Cas No.1092776-63-0
FormulaC21H34N4S2·2HCl
SolubilitySoluble in DMSO
Chemical Name(E)-(6,6-dimethyl-5,6-dihydroimidazo[2,1-b]thiazol-3-yl)methyl N,N'-dicyclohexylcarbamimidothioate dihydrochloride
Canonical SMILESCC1(CN2C(CS/C(NC3CCCCC3)=N/C4CCCCC4)=CSC2=N1)C.Cl.Cl
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

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.

References:
[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.