ACT-389949
目录号: PL02648 纯度: ≥98%
CAS No. :1258417-54-7
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中文名称
ACT-389949
英文名称
ACT-389949
英文别名
JH0PQ88XA2;GTPL9511;2-Methyl-5-m-tolyl-oxazole-4-carboxylic Acid {2-[4-(1,1-difluoro-ethyl)-oxazol-2-ylmethyl]-2H-[1,2,3]triazol-4-yl}-amide;4-Oxazolecarboxamide, N-(2-((4-(1,1-difluoroethyl)-2-oxazolyl)methyl)-2H-1,2,3-triazol-4-yl)-2-methyl-5-(3-methylphenyl)-;N-(2-((4-(1,1-Difluoroethyl)-2-oxazolyl)methyl)-2H-1,2,3-triazol-4-yl)-2-methyl-5-(3-methylphenyl)-4-oxazolecarboxamide;N-(2-{[4-(1,1-difluoroethyl)-1,3;Unii-JH0PQ88XA2;ACT-389949
Cas No.
1258417-54-7
分子式
C20H18F2N6O3
分子量
428.39
包装储存
Powder -20°C 3 years该产品在溶液状态不稳定,建议您现用现配,即刻使用。
产品详情
ACT-389949 是一种首创、高效、选择性的甲酰肽受体 2/脂蛋白 A4 受体(FPR2)/(ALX) 激动剂,对 FPR2/ALX 进行内化入单核细胞的 EC50 值为 3 nM。ACT-389949 具有研究炎性疾病的潜力。
生物活性
ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC 50 of 3 nM for FPR2/ALX internalization into monocytes. ACT-389949 has potential for the treatment of inflammatory disorders.
性状
Solid
IC50 & Target[1][2]
(FPR2)/(ALX)
体内研究(In Vivo)
ACT-389949 has well tolerated. Maximum concentrations are reached around 2 hours after dosing, with a mean terminal half-life of 29.3 hours.
Administration of ACT-389949 results in a dose-dependent, long-lasting internalization of FPR2/ALX into leukocytes.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years该产品在溶液状态不稳定,建议您现用现配,即刻使用。
ClinicalTrial
参考文献
[1]. Stalder AK,et al. Biomarker-guided clinical development of the first-in-class anti-inflammatory FPR2/ALX agonist ACT-389949. Br J Clin Pharmacol. 2017 Mar;83(3):476-486.
[2]. Lind S, et al. Functional and signaling characterization of the neutrophil FPR2 selective agonist Act-389949. Biochem Pharmacol. 2019 Aug;166:163-173.
溶解度数据
In Vitro: DMSO : 10 mg/mL (23.34 mM; ultrasonic and adjust pH to 1 with HCl)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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