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| 中文名称 |
ACT-660602
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|---|---|
| 英文名称 |
ACT-660602
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| 英文别名 |
Ethanone, 2-(3,5-dimethyl-1H-1,2,4-triazol-1-yl)-1-[(2R)-2-methyl-4-[2-(trifluoromethyl)-4-[2-(trifluoromethyl)-5-pyrimidinyl]-5-thiazolyl]-1-piperazinyl]-;ACT-660602
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| Cas No. |
1646267-59-5
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| 分子式 |
C20H20F6N8Os
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| 分子量 |
534.48
|
| 包装储存 |
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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| 产品详情 |
ACT-660602 是一种具有口服活性的趋化因子受体 CXCR3 拮抗剂， IC50 为 204 nM。ACT-660602 抑制 T 细胞迁移，并在体内急性肺损伤模型中表现出显著作用。ACT-660602 可用于自身免疫性疾病的研究。
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|---|---|
| 生物活性 |
ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC 50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
CXCR3 204 nM (IC50)
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| 体外研究(In Vitro) |
ACT-660602 shows selectivity to CXCR3 over hERG, with IC50s of 18 μM (hERG).ACT-660602 (112 nM; 6 h) inhibits cell migration and improves the metabolic stability. ACT-660602 (5, 20, 100 or 500 nM) displays an non-competitive binding mode to CXCL10 and CXCL11 in different concentration, with more stable IC50s. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Migration Assa
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| 体内研究(In Vivo) |
ACT-660602 (1 μM; 6 h) intrinsic metabolic clearance (CLint) in human, rat, mouse liver microsomes (HLM, RLM, MLM).
ACT-660602 (30 mg/kg; p.o.; once daily) displays anti-inflammatory activity and exerts efficacy in the mouse model of acute lung ingury.
Range for Pharmacokinetics of ACT-660602
Animal
Route
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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| 参考文献 |
[1]. Meyer EA, et al. Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for Autoimmune Diseases. J Med Chem. 2022 Aug 10.[2]. Caroff Eva, et al. Preparation of piperazinyltriazolylethanone derivatives for use as CXCR3 receptor modulators: World Intellectual Property Organization, WO2015011099. 2015-01-29.
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| 溶解度数据 |
In Vitro: DMSO : 110 mg/mL (205.81 mM; Need ultrasonic)配制储备液
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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。
2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。
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