Raphin1 acetate|2242616-04-0|-陌孚医药/Medlife

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Raphin1 acetate

目录号: PL09578 纯度: ≥99%

CAS No. :2242616-04-0

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中文名称	Raphin1 acetate
英文名称	Raphin1 acetate
英文别名	Raphin1 (acetate);Raphin1 acetate;(E)-2-(2,3-Dichlorobenzylidene)hydrazinecarboximidamide acetate;(E)-2-(2,3-Dichlorobenzylidene)hydrazine-1-carboximidamide acetate
Cas No.	2242616-04-0
分子式	C₁₀H₁₂Cl₂N₄O₂
分子量	291.13
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	Raphin1 acetate 是一种口服生物可利用的，选择性调节性磷酸酶 PPP1R15B (R15B) 抑制剂。Raphin1 acetate 与 R15B-PP1c 全磷酸酶强烈结合 (K_d=33 nM)，与 R15A-PP1c 相比，结合 R15B-PP1c 约为其 30 倍的选择性。Raphin1 acetate 穿过血脑屏障，并减少蛋白质错误折叠疾病的小鼠模型中的生物和分子缺陷。
生物活性	Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (K d =33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease.
性状	Solid
IC50 & Target[1][2]	Kd: 33 nM (R15B-PP1c holophosphatase)
体外研究(In Vitro)	Raphin1 acetate causes a rapid and transient accumulation of its phosphorylated substrate, resulting in a transient attenuation of protein synthesis. Raphin1 acetate inhibits the recombinant R15B-PP1c holoenzyme, but not the closely related R15A-PP1c, by interfering with substrate recruitment. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Raphin1 acetate improves weight of HD mice treated from 4 to ～10 weeks of age with 2 mg/kg of Raphin1 once a day by oral gavage. Raphin1 acetate also decreases SDS-insoluble huntingtin assemblies and nuclear inclusions in the cortex of HD mice. 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]. Krzyzosiak A, et al. Target-Based Discovery of an Inhibitor of the Regulatory Phosphatase PPP1R15B. Cell. 2018 Aug 23;174(5):1216-1228.e19.

溶解度数据	In Vitro: DMSO : 41.67 mg/mL (143.13 mM; Need ultrasonic)配制储备液

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