Mavorixafor trihydrochloride (Synonyms: AMD-070 trihydrochloride)
目录号: PL12286 纯度: ≥98%
CAS No. :2309699-17-8
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中文名称
Mavorixafor trihydrochloride
英文名称
Mavorixafor trihydrochloride
英文别名
Mavorixafor (trihydrochloride);Mavorixafor hydrochloride;(S)-N1-((1H-Benzo[D]imidazol-2-yl)methyl)-N1-(5,6,7,8-tetrahydroquinolin-8-yl)butane-1,4-diamine trihydrochloride;AMD-070 trihydrochloride;Mavorixafor trihydrochloride
Cas No.
2309699-17-8
分子式
C21H30Cl3N5
分子量
458.86
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Mavorixafor trihydrochloride (AMD-070 trihydrochloride) 是一种有效的,选择性的,可口服的 CXCR4 拮抗剂,能够拮抗 125I-SDF 与 CXCR4 结合,IC50 值为 13 nM;Mavorixafor trihydrochloride (AMD-070 trihydrochloride) 能够抑制 HIV-1 (NL4.3 strain) 的复制,在 MT-4 和 PBMCs 细胞中,IC50 值分别为 1 和 9 nM。
生物活性
Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC 50 value of 13 nM against CXCR4 I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC 50 of 1 and 9 nM, respectively.
性状
Solid
IC50 & Target[1][2]
I-SDF-CXCR4 13 nM (IC50) HIV-1 (NL4.3 strain)
体外研究(In Vitro)
Mavorixafor (AMD-070) is a potent and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively. Mavorixafor (AMD-070) shows no effect on other chemokine receptors (CCR1, CCR2b, CCR4, CCR5, CXCR1, and CXCR2). Mavorixafor (AMD-070) (6.6 μM) significantly suppresses the anchorage-dependent growth, the migration and matrigel invasion of the B88-SDF-1 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Mavorixafor (AMD-070) (2 mg/kg, p.o.) significantly reduces the number of metastatic lung nodules in mice, and lowers the expression of human Alu DNA in mice, without body weight loss. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. Skerlj RT, et al. Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication. J Med Chem. 2010 Apr 22;53(8):3376-88.
[2]. Uchida D, et al. Effect of a novel orally bioavailable CXCR4 inhibitor, AMD070, on the metastasis of oral cancer cells. Oncol Rep. 2018 Jul;40(1):303-308.
溶解度数据
In Vitro: DMSO : 150 mg/mL (326.90 mM; Need ultrasonic)H2O : 100 mg/mL (217.93 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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