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IT1t dihydrochloride  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥ 30 mg/mL)
产品描述：基本信息 产品编号： I10230 产品名称： IT1t dihydrochloride CAS: 1092776-63-0   储存条件 粉末 -20℃ 四年     分子式： C21H36Cl2N4S2 溶于液体 -80℃ 6个月 分子量： 479.57 -20℃ 1个月 化学名：  N,N'-Dicyclohexylcarbamimidothioic acid (5,6-dihydro-6,6-dimethylimidazo[2,1-b]thiazol-3-yl)methyl ester dihydrochloride Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.0852mL 10.4260mL 20.8520mL 5mM 0.4170mL 2.0852mL 4.1704mL 10mM 0.2085mL 1.0426mL 2.0852mL   生物活性 产品描述 一种高效的CXCR4拮抗剂；抑制CXCL12/CXCR4相互作用的IC50值为2.1nM。 靶点 CXCL12/CXCR4 2.1nM (IC50) HIV-1 (X4) 14.2nM (IC50,in MT-4 cells) HIV-1 (X4) 19nM (IC50,in PBMCs)   体外研究 The CXCR4 is involved in chemotaxis and serves as a coreceptor for T-tropic HIV-1 viral entry and in cancer metastasis.IT1t is a small,drug-like,isothiourea derivative.IT1t shows very potent and dose-dependent inhibition of the CXCL12/CXCR4 interaction with an IC50 of 2.1nM.This calcium flux is also inhibited by IT1t with an IC50 of 23.1.Strong electron density is observed for IT1t in the binding cavity of both subunits of the CXCR4 homodimer.In dimers of CXCR4 bound to IT1t,the monomers interact only at the extracellular side of helices V and VI,leaving at least a 4 Å gap between the intracellular regions,which is presumably filled by lipids.The IT1t compound and CVX15 peptide have both been characterized as competitive inhibitors of CXCL12,and many of the receptor-ligand contacts in the co-crystal structures presented are important for CXCL12 binding,including the acidic Asp187,Glu2887.39 and Asp972.63.The binding site of IT1t may point to the major anchor region for this domain. 体内研究 IT1t reduces the formation of TNBC early metastases in the zebrafish xenograft model.Tumor cell invasion at the metastatic site is effectively reduced upon CXCR4 silencing (Fig.7B),similar to the antagonist IT1t .   推荐实验方法(仅供参考) 细胞实验:   Jurkat cells are incubated with serial dilutions (0.001,0.01,0.1,1,10,100,1000μM) of IT1t at room temperature for two hours.Cytotoxicity of IT1t is also evaluated at 37℃ 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.
保存条件：-20℃

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