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IT1t dihydrochloride

Catalog No.
B5650
CXCR4 antagonist, potent
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,122.00
Ship with 10-15 days
5mg
¥ 1,020.00
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10mg
¥ 1,800.00
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25mg
¥ 3,600.00
Ship with 10-15 days
50mg
¥ 6,480.00
Ship with 10-15 days
100mg
¥ 11,280.00
Ship with 10-15 days

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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.

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.

Chemical Properties

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
SDFDownload SDF
Canonical SMILESCC1(CN2C(CS/C(NC3CCCCC3)=N/C4CCCCC4)=CSC2=N1)C.Cl.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
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。

质量控制

质量控制和MSDS

批次:

化学结构

IT1t dihydrochloride