ChemicalBook > CAS DataBase List > TAK-220

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
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3506
Advantage
58
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
Advantage
58
Beijing Solarbio Science & Tecnology Co., Ltd.
Tel
010-50973130 18101056239
Email
3193328036@qq.com
Country
China
ProdList
29760
Advantage
68
Amadis Chemical Company Limited
Tel
571-89925085
Fax
0086-571-89925065
Email
sales@amadischem.com
Country
China
ProdList
131957
Advantage
58
Beijing Jin Ming Biotechnology Co., Ltd.
Tel
010-60605840 18892239720
Fax
010-60605840
Email
psaitong@jm-bio.com
Country
China
ProdList
12306
Advantage
58
Musechem
Tel
+1-800-259-7612
Fax
+1-800-259-7612
Email
info@musechem.com
Country
United States
ProdList
4660
Advantage
60
Fan De(Beijing) Biotechnology Co., Ltd.
Tel
15911056312
Email
liming@bio-fount.com
Country
China
ProdList
9729
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32435
Advantage
58
Career Henan Chemica Co
Tel
+86-0371-86658258 +8613203830695
Fax
0371-86658258
Email
laboratory@coreychem.com
Country
China
ProdList
30229
Advantage
58

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