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IT1t dihydrochloride Sale

目录号 : GC10432

A CXCR4 antagonist

IT1t dihydrochloride Chemical Structure

Cas No.:1092776-63-0

规格 价格 库存 购买数量
5mg
¥765.00
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10mM * 1mL in DMSO
¥842.00
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10mg
¥1,350.00
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25mg
¥2,700.00
现货
50mg
¥4,860.00
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100mg
¥8,460.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment:

Jurkat cells are incubated with serial dilutions (0.001, 0.01, 0.1, 1, 10, 100, 1000 μM) of IT1t at room temperature for two hours. Cytotoxicity of IT1t is also evaluated at 37°C over a longer period of time in MT-4 cells and PHA-stimulated PBMCs (ten day incubation) because these cell types are used in anti-HIV activity assays which last up to ten days. Cytotoxicity is evaluated microscopically and viability is assessed using the a kit[1].

References:

[1]. Van Hout A, et al. Comparison of cell-based assays for the identification and evaluation of competitive CXCR4 inhibitors. PLoS One. 2017 Apr 14;12(4):e0176057.
[2]. Wu B, et al. Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science. 2010 Nov 19;330(6007):1066-71.
[3]. Tulotta C, et al. Inhibition of signaling between human CXCR4 and zebrafish ligands by the small molecule IT1timpairs the formation of triple-negative breast cancer early metastases in a zebrafish xenograft model. Dis Model Mech. 2016 Feb;9(2):141-53.

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.

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

Cas No. 1092776-63-0 SDF
化学名 (E)-(6,6-dimethyl-5,6-dihydroimidazo[2,1-b]thiazol-3-yl)methyl N,N'-dicyclohexylcarbamimidothioate dihydrochloride
Canonical SMILES CC1(CN2C(CS/C(NC3CCCCC3)=N/C4CCCCC4)=CSC2=N1)C.Cl.Cl
分子式 C21H34N4S2.2HCl 分子量 479.57
溶解度 H2O : 50 mg/mL (104.26 mM; Need ultrasonic); DMSO : ≥ 30 mg/mL (62.56 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.0852 mL 10.426 mL 20.852 mL
5 mM 0.417 mL 2.0852 mL 4.1704 mL
10 mM 0.2085 mL 1.0426 mL 2.0852 mL
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