TM-N1324
目录号: PL09210 纯度: ≥99%
CAS No. :1144477-35-9
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中文名称
TM-N1324
英文名称
TM-N1324
英文别名
TM-N1324;TM N1324;4-(2-Chloro-4-fluorophenyl)-1,4,5,7-tetrahydro-3-methyl-1-(9H-purin-6-yl)-6H-pyrazolo[3,4-b]pyridin-6-one;4-(2-chloro-4-fluorophenyl)-3-methyl-1-(9H-purin-6-yl)-4,5-dihydro-1H-pyrazolo[3,4-b]pyridin-6-ol;BDBM50232401;STK648472;STL287778;4-(2-chloro-4-fluorophenyl)-3-methyl-1-(9H-purin-6-yl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-b]pyridin-6-one;4-(2-chloro-4-fl
Cas No.
1144477-35-9
分子式
C18H13ClFN7O
分子量
397.79
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
TM-N1324 是 G 蛋白偶联受体 39 (GPR39) 的激动剂,在 Zn2+ 存在的情况下,对人和鼠 GPR39 的 EC50 值分别为 9 nM 和 5 nM,在 Zn2+ 不存在的情况下,对人和鼠 GPR39 的 EC50 值分别为 280 nM 和 180 nM。
生物活性
TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC 50 s of 9 nM/5 nM in the presence of Zn, and 280 nM/180 nM in the absence of Zn for human/murine GPR39.
性状
Solid
IC50 & Target[1][2]
EC50: 280 nM (human GPR39 without Zn), 9 nM (human GPR39 with Zn), 180 nM (murine GPR39 without Zn), 5 nM (murine GPR39 with Zn)
体外研究(In Vitro)
TM-N1324 activates human GPR39 with high efficacy and potencies of 280 nM and 9 nM in the absence and presence of Zn, respectively. TM-N1324 has similar potencies on murine GPR39, 180 nM and 5 nM. TM-N1324 is also found to have promising in vitro ADME properties. TM-N1324 has reasonably good aqueous solubility (65 μM at pH 7.0). Measurements of somatostatin confirms that the GPR39 agonist TM-N1324 increases somatostatin release by 53%. 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;4°C 2 years
参考文献
[1]. Frimurer TM, et al. Model-Based Discovery of Synthetic Agonists for the Zn2+-Sensing G-Protein-Coupled Receptor 39 (GPR39) Reveals Novel Biological Functions. J Med Chem. 2017 Feb 9;60(3):886-898.
溶解度数据
In Vitro: DMSO : 12.22 mg/mL (30.72 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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