An orally bioavailable CCR5 antagonist; binds to human CCR5 (IC50 = 3.5 nM)

TAK-220 – 1 mg

Brand:
Cayman
CAS:
333994-00-6
Storage:
-20
UN-No:
Non-Hazardous - /

TAK-220 is an orally bioavailable antagonist of chemokine (C-C motif) receptor 5 (CCR5).{46460} It binds to CCR5 (IC50 = 3.5 nM for the human receptor in CHO cells), but not CCR1, CCR2b, CCR3, CCR4, or CCR7.{46460,46459} TAK-220 inhibits the binding of chemokine (C-C motif) ligand 5 (CCL5) and CCL3 to CCR5 (IC50s = 3.5 and 1.4 nM, respectively) but does not inhibit binding of CCL4.{46459} It inhibits HIV-1 envelope-mediated membrane fusion in a macrophage (M-tropic) R5, but not in a T cell (T-tropic) X4, strain of HIV-1 (IC50s = 0.42 and >1,000 nM, respectively). TAK-220 inhibits the replication of six strains of R5 HIV-1 clinical isolates (EC90 overall mean = 13 nM) and the R5 JR-FL laboratory-adapted strain (EC50 = 0.6 nM), but not of X4 HIV-1 clinical isolates or the X4 IIIB laboratory-adapted strain (EC50s = >10,000 nM for both), in human peripheral blood mononuclear cells (PBMCs).  

 

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SKU: 28448 - 1 mg Category:

Description

An orally bioavailable CCR5 antagonist; binds to human CCR5 (IC50 = 3.5 nM), but not to CCR1, CCR2b, CCR3, CCR4, or CCR7, expressed in CHO cells; inhibits the binding of CCL5 and CCL3 to CCR5 (IC50s = 3.5 and 1.4 nM, respectively) but not the binding of CCL4; inhibits HIV-1 envelope-mediated membrane fusion in an M-tropic R5 but not in a T-tropic X4 HIV-1 strain (IC50s = 0.42 and >1,000 nM, respectively); inhibits the replication of six strains of R5 HIV-1 clinical isolates (EC90 overall mean = 13 nM) and the R5 JR-FL laboratory-adapted strain (EC50 = 0.6 nM), but not of X4 HIV-1 clinical isolates or the X4 IIIB laboratory-adapted strain (EC50s = >10,000 nM for both), in human PBMCs

Formal name: 1-acetyl-N-[3-[4-[[4-(aminocarbonyl)phenyl]methyl]-1-piperidinyl]propyl]-N-(3-chloro-4-methylphenyl)-4-piperidinecarboxamide

Synonyms: 

Molecular weight: 553.1

CAS: 333994-00-6

Purity: ≥98%

Formulation: A crystalline solid

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