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Avagacestat (BMS-708163)

This product is for research use only, not for human use. We do not sell to patients.

Avagacestat (BMS-708163)
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
250mg$1500Check With Us
500mg$2400Check With Us
1g$3600Check With Us

Cat #: V0718 CAS #: 1146699-66-2 Purity ≥ 98%

Description: Avagacestat (formerly known as BMS708163) is a potent, selective, orally bioactive γ -secretase inhibitor of Aβ40 and Aβ42 with potential anti-AD (Alzheimer's disease) activity.

References: Gillman KW, et al. Letter Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor. Med Chem Lett, 2010, 1 (3), 120-124.

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Molecular Weight (MW)520.88
Molecular FormulaC20H17ClF4N4O4S
CAS No.1146699-66-2
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 104 mg/mL (199.7 mM)r
Water: <1 mg/mLr
Ethanol: <1 mg/mL
SMILES CodeO=C(N)[C@H](N(CC1=CC=C(C2=NOC=N2)C=C1F)S(=O)(C3=CC=C(Cl)C=C3)=O)CCC(F)(F)F
SynonymsBMS-708163; BMS708163; Avagacestat; BMS 708163
ProtocolIn VitroAvagacestat (BMS-708163) exhibits weaker potency for inhibition of Notch processing, IC50=58±23 nM, as compared to its inhibition potency for APP cleavage.
In VivoAvagacestat (BMS-708163) significantly reduces both plasma and brain Aβ40 levels relative to control at 10 and 100 mg/kg for the entire dosing interval, demonstrates significant Aβ40 lowering for 8 h after an oral dose of 1 mg/kg, and significantly lowers CSF Aβ40 levels in rats, when measured 5 h after single oral doses ranging from 3 to 100 mg/kg.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.9198 mL9.5991 mL19.1983 mL38.3966 mL
5mM0.3840 mL1.9198 mL3.8397 mL7.6793 mL
10mM0.1920 mL0.9599 mL1.9198 mL3.8397 mL
20mM0.0960 mL0.4800 mL0.9599 mL1.9198 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.