APD597 (Synonyms: JNJ-38431055)
目录号: PL04456 纯度: ≥99%
CAS No. :897732-93-3
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中文名称
APD597
中文别名
4-[[6-[(6-甲基磺酰基-2-甲基吡啶-3-基)氨基]-5-甲氧基嘧啶-4-基]氧基]哌啶-1-羧酸异丙酯;APD597 抑制剂;化合物APD597
英文名称
APD597
英文别名
propan-2-yl 4-[5-methoxy-6-[(2-methyl-6-methylsulfonylpyridin-3-yl)amino]pyrimidin-4-yl]oxypiperidine-1-carboxylate;APD 597;APD-597;APD597;JNJ-38431055;APD597 (JNJ-38431055);4-[[6-[(6-Methylsulfonyl-2-methylpyridin-3-yl)amino]-5-methoxypyrimidin-4-yl]oxy]piperidine-1-carboxylic acid isopropyl ester; APD-597; APD 597; JNJ38431055; JNJ 38431055;CS-1557;1-Piperidinecarboxylic acid, 4-[[5-methoxy-6-[[2-methyl-6-(methylsulfonyl)-3-pyridinyl]amino]-4-pyrimidinyl]oxy]-, 1-methylethyl ester
Cas No.
897732-93-3
分子式
C21H29N5O6S
分子量
479.55
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
APD597 (JNJ-38431055) 是 GPR119 激动剂, 作用于 hGPR119, EC50 为 46 nM, 可用于研究 2 型糖尿病。
生物活性
APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119. IC50 value: 46 nM (EC50) [1] Target: hGPR119 The design and synthesis of a second generation GPR119-agonist clinical candidate for the treatment of diabetes is described. APD597 was selected for preclinical development based on a good balance between agonist potency, intrinsic activity and in particular on its good solubility and reduced drug-drug interaction potential. [1]
性状
Solid
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Buzard DJ, et al. Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4332-4335.
[2]. Huan Y, et al. The dual DPP4 inhibitor and GPR119 agonist HBK001 regulates glycemic control and beta cell function ex and in vivo. Sci Rep. 2017 Jun 28;7(1):4351.
溶解度数据
In Vitro: DMSO : 100 mg/mL (208.53 mM; Need ultrasonic)H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)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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