1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. Raphin1

Raphin1 

目录号: HY-123960
产品使用指南

Raphin1 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 与 R15B-PP1c 全磷酸酶强烈结合 (Kd=33 nM),与 R15A-PP1c 相比,结合 R15B-PP1c 约为其 30 倍的选择性。Raphin1 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。

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Raphin1 Chemical Structure

Raphin1 Chemical Structure

CAS No. : 2022961-17-5

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Description

Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease[1].

IC50 & Target

Kd:33 nM (R15B-PP1c holophosphatase)[1]

In Vitro

Raphin1 causes a rapid and transient accumulation of its phosphorylated substrate, resulting in a transient attenuation of protein synthesis[1].
Raphin1 inhibits the recombinant R15B-PP1c holoenzyme, but not the closely related R15A-PP1c, by interfering with substrate recruitment[1].

In Vivo

Raphin1 improves weight of HD82Q mice treated from 4 to ∼10 weeks of age with 2 mg/kg of Raphin1 once a day by oral gavage. Raphin1 also decreases SDS-insoluble huntingtin assemblies and nuclear inclusions in the cortex of HD82Q mice[1].

Molecular Weight

231.08

Formula

C₈H₈Cl₂N₄

CAS No.

2022961-17-5

SMILES

N=C(N/N=C/C1=CC=CC(Cl)=C1Cl)N

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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产品名称:
Raphin1
目录号:
HY-123960
需求量:

Raphin1

Cat. No.: HY-123960