R-268712|879487-87-3|-陌孚医药/Medlife

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R-268712

目录号: PL03057 纯度: ≥99%

CAS No. :879487-87-3

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中文名称	R-268712
中文别名	R-268712
英文名称	R-268712
英文别名	R 268712;R-268712;R268712;2-[4-[2-Fluoro-5-[3-(6-methylpyridine-2-yl)-1H-pyrazol-4-yl] phenyl] pyrazol-1-yl]ethanol;2-[4-[2-fluoro-5-[5-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl]phenyl]pyrazol-1-yl]ethanol;AMY16880;BCP25191;4-[2-Fluoro-5-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]phenyl]-1H-pyrazole-1-ethanol;CID 11703284
Cas No.	879487-87-3
分子式	C₂₀H₁₈FN₅O
分子量	363.39
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	R-268712 是一种口服有效的选择性 ALK-5 抑制剂，其 IC₅₀ 值为 2.5 nM。R-268712 能以剂量依赖的方式抑制 Smad3 的磷酸化，其 IC₅₀ 值为 10.4 nM。R-268712 通过抑制TGF-β 的信号传导来抑制肾小球肾炎以及肾小球硬化，可用于肾脏纤维化和癌症的研究。
生物活性	R-268712 is an orally active and selective ALK-5 inhibitor, with an IC 50 of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC 50 of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer.
性状	Solid
IC50 & Target[1][2]	TGFBR1 2.5 nM (IC50) Smad3 10.4 nM (IC
体外研究(In Vitro)	R-268712 (3, 10, 30, 100, 300 nM; 1 h) inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM in HFL-1 cells.R-268712 (3, 10, 30, 100, 300 nM; 72 h) inhibits myofibroblast transdifferentiation (MTD) from fibroblasts in a dose-dependent manner without inhibition of cell growth in HFL-1cells. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)	R-268712 (0.3, 1, 3, 10 mg/kg; p.o.; single) shows AUC 0-24 values of 0.075, 0.28, 1.6 and 8.2 μg?h/mL for dosages of 0.3, 1, 3, 10 mg/kg, respectively. R-268712 (1, 3, 10 mg/kg; p.o.; single daily for 3 days) inhibits renal luciferase activity in a dose-dependent manner in UUO model. R-268712 (0.3, 1 mg/kg; p.o.; single daily for 33 days) shows renoprotective effects (improves and maintains renal function as well as inhibits glomerular sclerosis) on Thy1 nephritis model when at dosage of 1 mg/kg. 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]. Terashima H, et al. Attenuation of pulmonary fibrosis in type I collagen-targeted reporter mice with ALK-5 inhibitors. Pulm Pharmacol Ther. 2019 Feb;54:31-38. [2]. Terashima H, et al. R-268712, an orally active transforming growth factor-β type I receptor inhibitor, prevents glomerular sclerosis in a Thy1 nephritis model. Eur J Pharmacol. 2014 Jul 5;734:60-6.

溶解度数据	In Vitro: DMSO : 125 mg/mL (343.98 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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