TAK-220
Based on 3 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 333994-00-6
- Formula: C31H41ClN4O3
- Molecular Weight:553.14
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) TAK-220
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Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
3.5 nM
Compound: 5m
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Inhibition of [125I]RANTES binding to human CCR5 expressed in CHO cells
Inhibition of [125I]RANTES binding to human CCR5 expressed in CHO cells
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[PMID: 16640339] |
| COS-7 | IC50 |
0.42 nM
Compound: 5m
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Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
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[PMID: 16640339] |
TAK-220 is a selective CCR5 antagonist, with IC50s 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 IC50 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 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[1]. TAK-220 shows potent inhibitory activity against the R5 isolates, with IC50s 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[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 333994-00-6
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Appearance Solid
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Molecular Weight 553.14
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Formula C31H41ClN4O3
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Color White to off-white
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SMILES
O=C(C1CCN(C(C)=O)CC1)N(CCCN2CCC(CC3=CC=C(C(N)=O)C=C3)CC2)C4=CC=C(C)C(Cl)=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Bioact Mater
Phosphorylation inhibition of protein-tyrosine phosphatase 1B tyrosine-152 induces bone regeneration coupled with angiogenesis for bone tissue engineering. [Abstract]2021 Jan 7;6(7):2039-2057. PMID: 33511306 -
JCI Insight
ANGPTL8 links refeeding to monocyte dynamics and metabolic inflammation via the CCL5-CCR5 axis. [Abstract]2025 Nov 25:e196605. PMID: 41289013 -
Brain Sci
Pharmacological Modulation of the MIP-1 Family and Their Receptors Reduces Neuropathic Pain Symptoms and Influences Morphine Analgesia: Evidence from a Mouse Model. [Abstract]2023 Mar 29;13(4):579. PMID: 37190544
Solvent & Solubility
DMSO : ≥ 50 mg/mL (90.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
PHA-stimulated PBMCs are inoculated with 1,000 to 1,400 CCID50s of R5 HIV-1 (JR-FL) or X4 HIV-1 (IIIB) or with 13 to 55 ng of p24 of HIV-1 clinical isolates per 4 × 106 cells and incubated for 4 h. The cells are washed to remove unadsorbed viral particles and seeded into a 96-well plate (2 × 105 cells/well) with culture medium containing various concentrations of TAK-220. The effects of high concentrations of human serum (HS) on the anti-HIV-1 activity of TAK-220 are examined with RPMI 1640 medium supplemented with either 20% FBS alone or 40% human type AB serum plus 10% FBS, 100 U/mL recombinant human interleukin 2, and antibiotics. On day 4 after infection, the cells are subcultured at 1:2 with culture medium containing the same concentrations of the test compounds. On day 7 after infection, the culture supernatants are collected and their p24 antigen levels are determined with a p24 antigen enzyme-linked immunosorbent assay kit[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8079 mL | 9.0393 mL | 18.0786 mL | 45.1965 mL |
| 5 mM | 0.3616 mL | 1.8079 mL | 3.6157 mL | 9.0393 mL | |
| 10 mM | 0.1808 mL | 0.9039 mL | 1.8079 mL | 4.5197 mL | |
| 15 mM | 0.1205 mL | 0.6026 mL | 1.2052 mL | 3.0131 mL | |
| 20 mM | 0.0904 mL | 0.4520 mL | 0.9039 mL | 2.2598 mL | |
| 25 mM | 0.0723 mL | 0.3616 mL | 0.7231 mL | 1.8079 mL | |
| 30 mM | 0.0603 mL | 0.3013 mL | 0.6026 mL | 1.5066 mL | |
| 40 mM | 0.0452 mL | 0.2260 mL | 0.4520 mL | 1.1299 mL | |
| 50 mM | 0.0362 mL | 0.1808 mL | 0.3616 mL | 0.9039 mL | |
| 60 mM | 0.0301 mL | 0.1507 mL | 0.3013 mL | 0.7533 mL | |
| 80 mM | 0.0226 mL | 0.1130 mL | 0.2260 mL | 0.5650 mL |
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