TAK 220

Name	TAK-220
Synonyms	TAK220 TAK-220 TAK 220 1-ACETYL-N-(3-(4-(4-CARBAMOYLBENZYL)PIPERIDIN-1-YL)PROPYL)-N-(3-CHLORO-4-METHYLPHENYL)PIPERIDINE-4-CARBOXAMIDE 4-Piperidinecarboxamide, 1-acetyl-N-[3-[4-[[4-(aminocarbonyl)phenyl]methyl]-1-piperidinyl]propyl]-N-(3-chloro-4-methylphenyl)-
CAS	333994-00-6

Molecular Formula	C31H41ClN4O3
Molar Mass	553.14
Density	1.208±0.06 g/cm3(Predicted)
Melting Point	166-167 °C(Solv: ethyl acetate (141-78-6); ethanol (64-17-5))
Boling Point	757.8±60.0 °C(Predicted)
Solubility	10 mM in DMSO
pKa	16.16±0.50(Predicted)
Storage Condition	-20℃
In vitro study	TAK-220 is a selective CCR5 antagonist, with IC 50 s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5 in CHO cells, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7. TAK-220 (0-1000 nM) interacts with CCR5 but not with RANTES and inhibits the CCR5-mediated Casup>2+ signaling. TAK-220 inhibits R5 HIV-1 (JR-FL) envelope-mediated membrane fusion, with an IC 50 value of 0.42 nM, but does not alter X4 HIV-1 (HXB2) envelope-mediated membrane fusion. TAK-220 also selectively inhibits HIV-1, with EC 50 s 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 EC 90 s 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. TAK-220 shows potent inhibitory activity against the R5 isolates, with IC 50 s 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.

Last Update：2024-01-02 23:10:35

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Product Name: TAK-220 Visit Supplier Webpage Request for quotation
CAS: 333994-00-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

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TAK 220

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