Raphin1 is an orally bioavailable, selective R15B (PPP1R15B, a regulatory subunit of protein phosphatase 1) inhibitor, strongly binding to the R15B-PP1c holophosphatase with Kd of 33 nM. Raphin1 decreases SDS-insoluble huntingtin assemblies and nuclear inclusions in the cortex of HD82Q mice.
| Molecular Weight | 231.08 |
| Formula | C8H8Cl2N4 |
| CAS Number | 2022961-17-5 |
| Solubility (25°C) | DMSO 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Phosphatase Products |
|---|
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| DPM-1003
DPM-1003 is an orally potent, specific inhibitor of PTP1B. |
| D-3
D-3, a phosphorpeptide, is an efficient, simple, and specific iPSC-eliminating agent. |
| EGF Receptor Substrate 2 (Phospho-Tyr5)
EGF Receptor Substrate 2 (Phospho-Tyr5) acetate, a biologically active peptide, is a tyrosine phosphate substrate. |
| Calcineurin autoinhibitory peptide
Calcineurin autoinhibitory peptide is a selective inhibitor of Ca2+/calmodulin-dependent protein phosphatase (calcineurin), with an IC50 of ~10 μM. |
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