TAK-220

• Description :

  TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.

• UNSPSC :

  12352005

• Target :

  CCR; HIV

• Type :

  Reference compound

• Related Pathways :

  Anti-infection; GPCR/G Protein; Immunology/Inflammation

• Applications :

  COVID-19-anti-virus

• Field of Research :

  Infection; Endocrinology

• Assay Protocol :

  https://www.medchemexpress.com/TAK-220.html

• Purity :

  99.95

• Solubility :

  DMSO : ≥ 50 mg/mL

• Smiles :

  O=C(C1CCN(C(C)=O)CC1)N(CCCN2CCC(CC3=CC=C(C(N)=O)C=C3)CC2)C4=CC=C(C)C(Cl)=C4

• Molecular Formula :

  C31H41ClN4O3

• Molecular Weight :

  553.14

• References & Citations :

  [1]Takashima K, et al. Highly potent inhibition of human immunodeficiency virus type 1 replication by TAK-220, an orally bioavailable small-molecule CCR5 antagonist. Antimicrob Agents Chemother. 2005 Aug;49 (8) :3474-82.|[2]Tremblay CL, et al. TAK-220, a novel small-molecule CCR5 antagonist, has favorable anti-human immunodeficiency virus interactions with other antiretrovirals in vitro. Antimicrob Agents Chemother. 2005 Aug;49 (8) :3483-5.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 1

• Isoform :

  CCR5; HIV-1

• CAS Number :

  [333994-00-6]