R1487 Hydrochloride|449808-64-4|-陌孚医药/Medlife

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R1487 Hydrochloride

目录号: PL08714 纯度: ≥99%

R1487 Hydrochloride 是强效、选择性的 p38α 抑制剂，其对 p38α 和 p38β 的 Kd 值分别为 0.2 nM 和 29 nM。

CAS No. :449808-64-4

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中文名称	R1487 Hydrochloride
中文别名	6-(2,4-二氟苯氧基)-8-甲基-2-[(四氢-2H-吡喃-4-基)氨基]吡啶并[2,3-D]嘧啶-7(8H)-酮盐酸盐;R1487 (Hydrochloride)
英文名称	R1487 Hydrochloride
英文别名	R1487;6-(2,4-difluorophenoxy)-8-methyl-2-(oxan-4-ylamino)pyrido[2,3-d]pyrimidin-7-one,hydrochloride;PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONE, 6-(2,4-DIFLUOROPHENOXY)-8-METHYL-2-[(TETRAHYDRO-2H-PYRAN-4-YL)AMINO]-, HYDROCHLORIDE ...;SY-R1487;6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride;CHEMBL1766582;KB-80225;Pyrido[2,3-d]pyrimidin-7(8H)-one,6-(2,4-difluorophenoxy)-8-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]-,hydrochloride;QC-6149;R 1487 Hydrochloride;R-1487 Hydrochloride;RS0052;R1487 (Hydrochloride);R1487 Hydrochloride
Cas No.	449808-64-4
分子式	C₁₉H₁₈F₂N₄O₃^.HCl
分子量	424.83
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	R1487 Hydrochloride 是强效、选择性的 p38α 抑制剂，其对 p38α 和 p38β 的 K_d 值分别为 0.2 nM 和 29 nM。
生物活性	R1487 Hydrochloride is a highly potent and selective p38α inhibitor, with K d values of 0.2 nM and 29 nM for p38α and p38β, respectively.
性状	Solid
IC50 & Target[1][2]	p38α 0.2 nM (Kd) p38β 29 nM (Kd)
体外研究(In Vitro)	R1487 Hydrochloride exhibits IC50 values of 10 nM for p38α inhibition and 200 nM for the inhibition of TNFα induced production of IL-1β. R1487 (Compounds 2a) inhibits production of TNFα by human monocytic cells (THP-1) and inhibits production of IL-1β in human whole blood (HWB) induced by LPS. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	R1487 (Compounds 2a, orally) demonstrates significant dose-dependent inhibition of serum TNFα and IL-1β. Oral bioavailability of 10 mg/kg R1487 (Compounds 2a) in monkey, rat, and dog was 51.6%, 29.3%, 10.3%, respectively. 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	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Goldstein DM et al. Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-on

溶解度数据	In Vitro: DMSO : 20.83 mg/mL (49.03 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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