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TAK-220

CAT: 0804-HY-19974-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-19974-01Size:5 mg
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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.
CAS Number
333994-00-6
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

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