product name Avagacestat (BMS-708163)
Description: Avagacestat (also known as BMS-708163) is a potent, selective, orally bioactive γ -secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, it demonstrated a 193-fold selectivity against Notch. Avagacestat is designed for selective inhibition of Aβ synthesis currently in development for the treatment of mild to moderate and predementia AD. Avagacestat produced up to 190-fold greater selectivity for Aβ synthesis than Notch processing in preclinical studies and may therefore produce less toxic adverse events than other less selective compounds.
References: Med Chem Lett, 2010, 1 (3), 120–124.
520.88
Formula
C20H17ClF4N4O4S
CAS No.
1146699-66-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 104 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
BMS-708163
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19401338
| In Vitro |
In vitro activity: BMS-708163 exhibits weaker selectivity for inhibition of Notch processing with 193-fold IC50 value. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Oral administration of BMS-708163 significantly reduces Aβ40 levels for sustained periods in brain, plasma, and cerebrospinal fluid in rats and dogs. BMS-708163 has no dose-limiting effects in dogs (3 mg/kg during 6 months), with a high brain to plasma ratio (2.4). |
| Animal model | Female Harlan Sprague-Dawley rats or ATM-405-142K9 with 7- 10 month old Naive, grade II beagles |
| Formulation & Dosage | Dissolved in 99% PEG-400, 1% Tween-80 (rats) or 94% labrafil-1944, 5% ethanol, 1% tween-80 (dogs); 10 mg/kg (rats) or 2.5 mg/kg (dogs); Oral gavage |
| References | Med Chem Lett, 2010, 1 (3), 120–124. |
Related Posts
product name Avagacestat (BMS-708163)
Description: Avagacestat (also known as BMS-708163) is a potent, selective, orally bioactive γ -secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, it demonstrated a 193-fold selectivity against Notch. Avagacestat is designed for selective inhibition of Aβ synthesis currently in development for the treatment of mild to moderate and predementia AD. Avagacestat produced up to 190-fold greater selectivity for Aβ synthesis than Notch processing in preclinical studies and may therefore produce less toxic adverse events than other less selective compounds.
References: Med Chem Lett, 2010, 1 (3), 120–124.
520.88
Formula
C20H17ClF4N4O4S
CAS No.
1146699-66-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 104 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
BMS-708163
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19401338
| In Vitro |
In vitro activity: BMS-708163 exhibits weaker selectivity for inhibition of Notch processing with 193-fold IC50 value. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Oral administration of BMS-708163 significantly reduces Aβ40 levels for sustained periods in brain, plasma, and cerebrospinal fluid in rats and dogs. BMS-708163 has no dose-limiting effects in dogs (3 mg/kg during 6 months), with a high brain to plasma ratio (2.4). |
| Animal model | Female Harlan Sprague-Dawley rats or ATM-405-142K9 with 7- 10 month old Naive, grade II beagles |
| Formulation & Dosage | Dissolved in 99% PEG-400, 1% Tween-80 (rats) or 94% labrafil-1944, 5% ethanol, 1% tween-80 (dogs); 10 mg/kg (rats) or 2.5 mg/kg (dogs); Oral gavage |
| References | Med Chem Lett, 2010, 1 (3), 120–124. |