TAK-220

Product Name: TAK-220
CAS No.: 333994-00-6
Chemical Name: TAK-220
Synonyms: TAK-220;TAK 220;TAK220;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)-
CBNumber: CB13122935
Molecular Formula: C31H41ClN4O3
Formula Weight: 553.14
MOL File: 333994-00-6.mol

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TAK-220 Property

Melting point:: 166-167 °C(Solv: ethyl acetate (141-78-6); ethanol (64-17-5))
Boiling point:: 757.8±60.0 °C(Predicted)
Density: 1.208±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO: soluble
form: A crystalline solid
pka: 16.16±0.50(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 28448
Product name: TAK-220
Packaging: 1mg
Price: $153
Updated: 2024/03/01

ChemScene

Product number: CS-5579
Product name: TAK-220
Purity: 99.95%
Packaging: 1mg
Price: $180
Updated: 2021/12/16

AK Scientific

Product number: 1559AL
Product name: 1-Acetyl-N-(3-(4-(4-carbamoylbenzyl)piperidin-1-yl)propyl)-N-(3-chloro-4-methylphenyl)piperidine-4-carboxamide
Packaging: 1mg
Price: $268
Updated: 2021/12/16

ChemScene

Product number: CS-5579
Product name: TAK-220
Purity: 99.95%
Packaging: 5mg
Price: $420
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb611449
Product name: TAK-220
Packaging: 5mg
Price: $569.5
Updated: 2021/12/16

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TAK-220 Chemical Properties,Usage,Production

Description

TAK-220 is an orally bioavailable antagonist of chemokine (C-C motif) receptor 5 (CCR5). It binds to CCR5 (IC₅₀ = 3.5 nM for the human receptor in CHO cells), but not CCR1, CCR2b, CCR3, CCR4, or CCR7. 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. 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).

Uses

TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; 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.

IC 50

MIP-1α-CCR5: 1.4 nM (IC₅₀, in CHO cells); RANTES-CCR5: 3.5 nM (IC₅₀, in CHO cells); HIV-1 (HHA): 0.55 nM (EC₅₀, in PBMCs); HIV-1 (CTV): 0.72 nM (EC₅₀, in PBMCs); HIV-1 (HTN): 0.93 nM (EC₅₀, in PBMCs); HIV-1 (KK): 1.2 nM (EC₅₀, in PBMCs); HIV-1 (HKW): 1.7 nM (EC₅₀, in PBMCs); HIV-1 (HNK): 1.7 nM (EC₅₀, in PBMCs); HIV-1 (HHA): 4 nM (EC90, in PBMCs); HIV-1 (CTV): 5 nM (EC90, in PBMCs); HIV-1 (KK): 12 nM (EC90, in PBMCs); HIV-1 (HKW): 12 nM (EC90, in PBMCs); HIV-1 (HTN): 15 nM (EC90, in PBMCs); HIV-1 (HNK): 28 nM (EC90, in PBMCs)

References

[1] Takashima K, et al. Highly potent inhibition of human immunodeficiency virus type 1 replication by TAK-220, an orally bioavailable small-molecule CCR5 antagonist. Antimicrob Agents Chemother. 2005 Aug;49(8):3474-82. DOI:10.1128/AAC.49.8.3474-3482.2005
[2] Tremblay CL, et al. TAK-220, a novel small-molecule CCR5 antagonist, has favorable anti-human immunodeficiency virus interactions with other antiretrovirals in vitro. Antimicrob Agents Chemother. 2005 Aug;49(8):3483-5. DOI:10.1128/AAC.49.8.3483-3485.2005

TAK-220 Preparation Products And Raw materials

Raw materials

Preparation Products

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TAK-220 Suppliers

China 26 United States 6 Global 32

ShangHai Caerulum Pharma Discovery Co., Ltd.

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Amadis Chemical Company Limited

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Career Henan Chemica Co

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ChemeGen

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Nanjing Shizhou Biology Technology Co.,Ltd

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Shanghai Qiming Biological Technology Co., Ltd.

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333994-00-6, TAK-220Related Search:

TAK-220

1-ACETYL-N-(3-(4-(4-CARBAMOYLBENZYL)PIPERIDIN-1-YL)PROPYL)-N-(3-CHLORO-4-METHYLPHENYL)PIPERIDINE-4-CARBOXAMIDE

TAK 220;TAK220

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

333994-00-6

C31H41ClN4O3