Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TAK-220 is a selective and orally bioavailable CCR5 antagonist (IC50s: 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | 6-8 weeks | $ 347.00 | |
25 mg | 6-8 weeks | $ 1,140.00 | |
50 mg | 6-8 weeks | $ 1,490.00 | |
100 mg | 6-8 weeks | $ 1,990.00 | |
1 mL * 10 mM (in DMSO) | 6-8 weeks | $ 382.00 |
Description | TAK-220 is a selective and orally bioavailable CCR5 antagonist (IC50s: 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively). |
Targets&IC50 | HIV-1 (HTN):0.93 nM (EC50)(in PBMCs), HIV-1 (KK):1.2 nM (EC50)(in PBMCs), HIV-1 (KK):12 nM (EC90)(in PBMCs), MIP-1α-CCR5:1.4 nM (in CHO cells), HIV-1 (HHA):4 nM (EC90)(in PBMCs), HIV-1 (HKW):1.7 nM (EC50)(in PBMCs), HIV-1 (HKW):12 nM (EC90)(in PBMCs), HIV-1 (HNK):1.7 nM (EC50)(in PBMCs), HIV-1 (HTN):15 nM (EC90)(in PBMCs), X4 HIV-1 (CTV):0.72 nM (EC50)(in PBMCs), X4 HIV-1 (CTV):5 nM (EC90)(in PBMCs), RANTES-CCR5:3.5 nM (in CHO cells), HIV-1 (HNK):28 nM (EC90)(in PBMCs), HIV-1 (HHA):0.55 nM (EC50)(in PBMCs) |
In vitro | TAK-220 inhibits R5 HIV-1 (JR-FL) envelope-mediated membrane fusion (IC50: 0.42 nM). TAK-220 shows potent inhibitory activity against the R5 isolates, with IC50s of 3.12 nM against HIV-1 R5-08, 13.47 nM against HIV-1 R5-06, and 2.26 nM against HIV-1 R5-18. TAK-220 (>100 nM) has no toxicity in uninfected PBMCs. TAK-220 (0-1000 nM) interacts with CCR5 but not with RANTES and inhibits the CCR5-mediated Casup>2+ signaling. 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 [1][2]. |
Molecular Weight | 553.14 |
Formula | C31H41ClN4O3 |
CAS No. | 333994-00-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (90.39 mM)
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
TAK-220 333994-00-6 Microbiology/Virology Proteases/Proteasome HIV Protease TAK 220 TAK220 inhibitor inhibit