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TAK-220

Chemical Structure : TAK-220

CAS No.: 333994-00-6

TAK-220 (TAK 220;TAK220)

Catalog No.: PC-45771Not For Human Use, Lab Use Only.

TAK-220 (TAK220) is a potent, specific, orally bioavailable CCR5 antagonist that blocks the binding of MIP-1α to CCR5 with IC50 of 1.4 nM.

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Biological Activity

TAK-220 (TAK220) is a potent, specific, orally bioavailable CCR5 antagonist that blocks the binding of MIP-1α to CCR5 with IC50 of 1.4 nM.
TAK-220 shows no affinity for CCR1, CCR2b, CCR3, CCR4, or CCR7.
TAK-220 inhibits the replication of 6 CCR5-using (R5) HIV-1 clinical isolates in peripheral blood mononuclear cells (PBMCs) with mean EC90 of 13 nM.
TAK-220 selectively inhibits R5 HIV-1 replication by interfering with coreceptor-mediated entry of the virus into host cells; exhibits a good pharmacokinetic profile in monkeys.

Physicochemical Properties

M.Wt 553.1353
Formula C31H41ClN4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-Piperidinecarboxamide, 1-acetyl-N-[3-[4-[[4-(aminocarbonyl)phenyl]methyl]-1-piperidinyl]propyl]-N-(3-chloro-4-methylphenyl)-

References

1. Tremblay CL, et al. Antimicrob Agents Chemother. 2005 Aug;49(8):3483-5.

2. Takashima K, et al. Antimicrob Agents Chemother. 2005 Aug;49(8):3474-82.

3. Imamura S, et al. J Med Chem. 2006 May 4;49(9):2784-93.

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