TAK-220 |
رقم الكتالوجGC32135
One-Click Copy Product Info
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TAK-220 هو مضاد CCR5 انتقائي ومتوفر حيوياً عن طريق الفم ، مع IC50s من 3.5 نانومتر و 1.4 نانومتر لتثبيط ربط RANTES و MIP-1α بـ CCR5 ، على التوالي ، لكنه لا يظهر أي تأثير على الارتباط بـ CCR1 ، CCR2b ، CCR3 ، CCR4 أو CCR7 ؛ يثبط TAK-220 أيضًا بشكل انتقائي فيروس نقص المناعة البشرية -1 ، مع EC50s لـ 1.2 نانومتر (HIV-1 KK) ، 0.72 نانومتر (HIV-1 CTV) ، 1.7 نانومتر (HIV-1 HKW) ، 1.7 نانومتر (HIV-1 HNK) ، 0.93 نانومتر (HIV-1 HTN) ، و 0.55 نانومتر (HIV-1 HHA) ، و EC90s من 12 نانومتر (HIV-1 KK) ، 5 نانومتر (HIV-1 CTV) ، 12 نانومتر (HIV-1 HKW) ، 28 نانومتر (HIV-1 HNK) ، 15 نانومتر (HIV-1 HTN) ، و 4 نانومتر (HIV-1 HHA) في PBMCs
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 333994-00-6
Sample solution is provided at 25 µL, 10mM.
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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.
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].
[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. [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.
Cell experiment: | 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]. |
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. | |
| Cas No. | 333994-00-6 | SDF | |
| Canonical 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 | ||
| Formula | C31H41ClN4O3 | M.Wt | 553.14 |
| الذوبان | DMSO : ≥ 50 mg/mL (90.39 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8079 mL | 9.0393 mL | 18.0786 mL |
| 5 mM | 361.6 μL | 1.8079 mL | 3.6157 mL |
| 10 mM | 180.8 μL | 903.9 μL | 1.8079 mL |
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)