TAK-220

• CAT Number: I003210
• CAS Number: 333994-00-6
• Molecular Formula: C31H41ClN4O3
• Molecular Weight: 553.14
• Purity: ≥95%
• Target: CCR
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C

TAK-220 is an orally bioavailable small-molecule CCR5 antagonist.Target: CCRTAK-220 is a member of a novel class of chemokine receptor antagonists and is highly specific to CCR5. TAK-220 inhibits RANTES binding to CCR5-expressing cells, with an IC50 of 3.5 nM, whereas it inhibits membrane fusion and viral replication, with EC50s of 0.42 nM and 0.60 to 0.68 nM, respectively. TAK-220 inhibits R5 HIV-1 (JR-FL) envelope-mediated membrane fusion, with an IC50 value of 0.42 nM, but does not affect X4 HIV-1 (HXB2) envelope-mediated membrane fusion, even when it was used at a concentration of 1,000 nM. [1]

Reference

1:Discovery of a piperidine-4-carboxamide CCR5 antagonist (TAK-220) with highly potent Anti-HIV-1 activity. Imamura S, Ichikawa T, Nishikawa Y, Kanzaki N, Takashima K, Niwa S, Iizawa Y, Baba M, Sugihara Y.J Med Chem. 2006 May 4;49(9):2784-93. PMID: 16640339 2:Analysis of binding sites for the new small-molecule CCR5 antagonist TAK-220 on human CCR5. Nishikawa M, Takashima K, Nishi T, Furuta RA, Kanzaki N, Yamamoto Y, Fujisawa J.Antimicrob Agents Chemother. 2005 Nov;49(11):4708-15. PMID: 16251315 Free PMC Article3:TAK-220, a novel small-molecule CCR5 antagonist, has favorable anti-human immunodeficiency virus interactions with other antiretrovirals in vitro. Tremblay CL, Giguel F, Guan Y, Chou TC, Takashima K, Hirsch MS.Antimicrob Agents Chemother. 2005 Aug;49(8):3483-5. PMID: 16048964 Free PMC Article4:Highly potent inhibition of human immunodeficiency virus type 1 replication by TAK-220, an orally bioavailable small-molecule CCR5 antagonist. Takashima K, Miyake H, Kanzaki N, Tagawa Y, Wang X, Sugihara Y, Iizawa Y, Baba M.Antimicrob Agents Chemother. 2005 Aug;49(8):3474-82. PMID: 16048963 Free PMC Article