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

Raphin1 acetate 

Cat. No.: HY-123960A Purity: 99.22%
Handling Instructions

Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=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.

For research use only. We do not sell to patients.

Raphin1 acetate Chemical Structure

Raphin1 acetate Chemical Structure

CAS No. : 2242616-04-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 160 In-stock
Estimated Time of Arrival: December 31
1 mg USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 125 In-stock
Estimated Time of Arrival: December 31
25 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 435 In-stock
Estimated Time of Arrival: December 31
100 mg USD 760 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=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[1].

IC50 & Target

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

In Vitro

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

In Vivo

Raphin1 acetate 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 acetate also decreases SDS-insoluble huntingtin assemblies and nuclear inclusions in the cortex of HD82Q mice[1].

Molecular Weight

291.13

Formula

C₁₀H₁₂Cl₂N₄O₂

CAS No.

2242616-04-0

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (143.13 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4349 mL 17.1745 mL 34.3489 mL
5 mM 0.6870 mL 3.4349 mL 6.8698 mL
10 mM 0.3435 mL 1.7174 mL 3.4349 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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Keywords:

Raphin1Raphin 1Raphin-1PhosphataseInhibitorinhibitorinhibit

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Product name:
Raphin1 acetate
Cat. No.:
HY-123960A
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