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Mavorixafor
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
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CAS NO:558447-26-0

AMD-070
Mavorixafor (AMD-070) 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 (AMD-070) 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 (AMD-070) is a potent, selective and orally availableCXCR4antagonist, with anIC50value of 13 nM againstCXCR4125I-SDF binding, and also inhibits the replication of T-tropicHIV-1(NL4.3 strain) in MT-4 cells and PBMCs with anIC50of 1 and 9 nM, respectively.

IC50& Target[1]

125I-SDF-CXCR4

13 nM (IC50)

HIV-1 (NL4.3 strain)

1 nM (IC50, in MT-4 cells)

HIV-1 (NL4.3 strain)

9 nM (IC50, in PBMCs)

HIV-1 (NL4.3 strain)

3 nM (IC90, in MT-4 cells)

HIV-1 (NL4.3 strain)

26 nM (IC90, in PBMCs)

体外研究
(In Vitro)

Mavorixafor (AMD-070) is a potent and orally available CXCR4 antagonist, with an IC50value of 13 nM against CXCR4125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50of 1 and 9 nM, respectively. Mavorixafor (AMD-070) shows no effect on other chemokine receptors (CCR1, CCR2b, CCR4, CCR5, CXCR1, and CXCR2)[1]. Mavorixafor (AMD-070) (6.6 μM) significantly suppresses the anchorage-dependent growth, the migration and matrigel invasion of the B88-SDF-1 cells[2].

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[2].

Clinical Trial
分子量

349.47

性状

Solid

Formula

C21H27N5

CAS 号

558447-26-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vivo:
  • 1.

    AMD-070 is prepared in oil plus vehicle (PBS) control[3].

 
 
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