[CAS NO. 2143542-28-1] 2BAct
PRODUCTS SPECIFICATIONS [2143542-28-1]
DESCRIPTION [2143542-28-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 440.80 |
| Molecular Formula | C19H16ClF3N4O3 |
| SMILES | O=C(C(C=N1)=NC=C1C(F)F)NC(C2)(C3)CC23NC(COC(C=C4)=CC(F)=C4Cl)=O |
Summary
2BAct is a highly selective, and orally active eIF2B (eukaryotic initiation factor 2B) activator with an EC 50 of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct is able to penetrate the central nervous system (CNS). 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB (HY-12495) [1] .
IC50 & Target
EC50: 33 nM (eIF2B) [1]
In Vitro
Primary fibroblast lysates from R191H embryos has lower GEF activity than WT lysates, and 2BAct enhances this activity threefold (EC 50 =7.3 nM) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
2BAct (300 µg 2BAct/g of meal; 21 weeks) normalizes body weight gain in VWM mice
[1]
.
2BAct prevents the appearance of motor deficits, myelin loss and reactive gliosis in VWM mice
[1]
.
2BAct stimulates the remaining activity of mutant eIF2B complex in vivo, abrogating the maladaptive stress response
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 250 mg/mL ( 567.15 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2686 mL | 11.3430 mL | 22.6860 mL |
| 5 mM | 0.4537 mL | 2.2686 mL | 4.5372 mL |
| 10 mM | 0.2269 mL | 1.1343 mL | 2.2686 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution