IT1t dihydrochloride
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mL(10 mM in DMSO) | ¥867.00 | 现货 | |
| 5mg | ¥807.00 | 现货 | |
| 10mg | ¥1425.00 | 现货 | |
| 25mg | ¥2850.00 | 现货 | |
| 50mg | ¥5130.00 | 现货 | |
| 100mg | ¥8208.00 | 现货 |
特色产品
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
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.
产品性质
| 物理外观 | Off-white solid |
| CAS号 | 1092776-63-0 |
| 分子式 | C21H34N4S2·2HCl |
| 分子量 | 479.57 |
| 化学名称 | (E)-(6,6-dimethyl-5,6-dihydroimidazo[2,1-b]thiazol-3-yl)methyl N,N'-dicyclohexylcarbamimidothioate dihydrochloride |
| 溶解度 | ≥8.8 mg/mL in DMSO with ultrasonic; ≥50.6 mg/mL in EtOH; ≥50 mg/mL in H2O |
| SMILES | CC1(C)N=C2SC=C(CS/C(\NC3CCCCC3)=N/C3CCCCC3)N2C1.Cl.Cl |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
| 生物活性描述 | IT1t 二盐酸盐是一种强效的 CXCR4 拮抗剂;抑制 CXCL12/CXCR4 相互作用的 IC50 为 2.1 nM。 |



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