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- 详细信息
- 技术资料
- 保存条件：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
TAK-220
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
333994-00-6
- 规格：
10mg/5mg/1mg
| 规格： | 10mg | 产品价格： | ￥4990.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥3490.0 |
| 规格： | 1mg | 产品价格： | ￥1490.0 |
| 基本信息 | |
| CAS | No.333994-00-6 |
| 英文名称 | TAK-220 |
| 分子式 | C31H41ClN4O3 |
| 分子量 | 553.14 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 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 |
| InChIKey | ASSJTMUEFHUKMJ-UHFFFAOYSA-N |
| InChI | InChI=1S/C31H41ClN4O3/c1-22-4-9-28(21-29(22)32)36(31(39)27-12-18-35(19-13-27)23(2)37)15-3-14-34-16-10-25(11-17-34)20-24-5-7-26(8-6-24)30(33)38/h4-9,21,25,27H,3,10-20H2,1-2H3,(H2,33,38) |
| PubChem CID | 5275766 |
| 靶点 | CCR5 |
| 通路 | Immunology & Inflammation;GPCR & G Protein |
| 背景说明 | TAK-220是一种选择性的 CCR5 拮抗剂。 |
| 生物活性 | 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.[1]{2} |
| In Vitro | 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]. |
| 细胞实验 | 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]. |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
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￥1490 - 4990
