AMD-070 hydrochloride

• CAT Number: I005295
• CAS Number: 880549-30-4
• Molecular Formula: C21H30Cl3N5
• Molecular Weight: 458.86
• Purity: ≥95%
• Synonyms: N/’-(1H-benzimidazol-2-ylmethyl)-N/’-[(8S)-5,6,7,8-tetrahydroquinolin-8-yl]butane-1,4-diamine;hydrochloride
• Target: CXCR
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 13 nM

AMD-070 Hcl is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay; inhibit the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.IC50 Value: 13 nMTarget: CXCR4; anti HIVAMD-070 is an investigational drug that is being studied for the treatment of HIV infection. AMD-070 belongs to a class (group) of HIV drugs called entry and fusion inhibitors.2 Entry and fusion inhibitors block HIV from getting into and infecting certain cells of the immune system. This prevents HIV from multiplying and can reduce the amount of HIV in the body. AMD-070 inhibited the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC(50) of 2 and 26 nM, respectively, while remaining noncytotoxic to cells at concentrations exceeding 23 microM.AMD-070 works by attaching to one of two proteins on the surface of the immune cells. These proteins are called the CCR5 and CXCR4 coreceptors. AMD-070 attaches to the CXCR4 coreceptor. When AMD-070 attaches to the CXCR4 coreceptor, certain strains of HIV—called X4-tropic virus—cannot attach to, enter, or infect the cell.

Reference

[1]. Effect of low-dose ritonavir on the pharmacokinetics of the CXCR4 antagonist AMD070 in healthy volunteers By Cao, Ying Jun; From Antimicrobial Agents and Chemotherapy (2008), 52(5), 1630-1634.
[2]. Skerlj R, Bridger G, McEachern E, Harwig C, Smith C, Kaller A, Veale D, Yee H, Skupinska K, Wauthy R, Wang L, Baird I, Zhu Y, Burrage K, Yang W, Sartori M, Huskens D, De Clercq E, Schols D.Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.Bioorg Med Chem Lett. 2011 Mar 1;21(5):1414-8. Epub 2011 Jan 11.
[3]. Skerlj R, Bridger G, McEachern E, Harwig C, Smith C, Wilson T, Veale D, Yee H, Crawford J, Skupinska K, Wauthy R, Yang W, Zhu Y, Bogucki D, Di Fluri M, Langille J, Huskens D, De Clercq E, Schols D.Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication.Bioorg Med Chem Lett. 2011 Jan 1;21(1):262-6. Epub 2010 Nov 6.
[4]. Miller JF, Gudmundsson KS, Richardson LD, Jenkinson S, Spaltenstein A, Thomson M, Wheelan P.Synthesis and SAR of novel isoquinoline CXCR4 antagonists with potent anti-HIV activity.Bioorg Med Chem Lett. 2010 Apr 3.
[5]. Skerlj RT, Bridger GJ, Kaller A, McEachern EJ, Crawford JB, Zhou Y, Atsma B, Langille J, Nan S, Veale D, Wilson T, Harwig C, Hatse S, Princen K, De Clercq E, Schols D.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.