| Name | TAK-220 |
| Description | TAK-220 is a selective and orally bioavailable CCR5 antagonist with IC50 values of 3.5 nM for RANTES binding inhibition and 1.4 nM for MIP-1α binding inhibition to CCR5. |
| 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 2.5 mg/mL (4.52 mM), Sonication is recommended.
DMSO : 50 mg/mL (90.39 mM), Sonication is recommended.
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| Keywords | TAK-220 | TAK220 | TAK 220 | RANTES-CCR5 | MIP-1α-CCR5 | HIVProtease | HIV-1 KK | HIV-1 HTN | HIV-1 HNK | HIV-1 HKW | HIV-1 HHA | HIV-1 CTV | HIV-1 (HTN) | HIV-1 (HNK) | HIV-1 (HKW) | HIV-1 (HHA) | HIV Protease |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Emtricitabine | Dolutegravir intermediate-1 | Dimethyl fumarate | Lamivudine | Valproic Acid | (-)-Epigallocatechin Gallate | Pirfenidone | Decanedioic acid | Dextran sulfate sodium salt (MW 5000) | Tenofovir |
United States
