Raphin1 acetate

Raphin1 acetate, an orally bioavailable, selective PPP1R15B (R15B) regulatory phosphatase inhibitor, binds tightly to the R15B-PP1c holophosphatase (KD=33 nM). It demonstrates approximately 30-fold greater selectivity for R15B-PP1c over R15A-PP1c. Capable of crossing the blood-brain barrier, Raphin1 acetate mitigates both organismal and molecular impairments in a mouse model of protein misfolding disease¹.

Raphin1 acetate induces a swift and temporary buildup of its phosphorylated substrate, leading to a brief reduction in protein synthesis¹.

Raphin1 acetate blocks the recombinant R15B-PP1c holoenzyme by disrupting substrate recruitment, without affecting the similar R15A-PP1c¹.

Raphin1 acetate enhances the weight of HD82Q mice treated orally with 2 mg/kg daily from ages 4 to 10 weeks. It also reduces SDS-insoluble huntingtin assemblies and nuclear inclusions in the cortex of HD82Q mice¹.

Raphin1 acetate enhances the weight of HD82Q mice treated orally with 2 mg/kg daily from ages 4 to 10 weeks. It also reduces SDS-insoluble huntingtin assemblies and nuclear inclusions in the cortex of HD82Q mice¹.

溶解方案(细胞实验)

DMSO 中的溶解度 : 41.67 mg/mL (143.13 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: ≥ 2.08 mg/mL (7.14 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。"

"方案 二": "请依序添加每种溶剂：10% DMSO 90% (20% SBE-β-CD in Saline)Solubility: ≥ 2.08 mg/mL (7.14 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。"

"方案 三": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 2.08 mg/mL (7.14 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"