PeptideDB

gamma-Secretase Modulators 937812-80-1

gamma-Secretase Modulators 937812-80-1

CAS No.: 937812-80-1

Gamma-Secretase Modulators (Amyloid-β production inhibitor) are amyloid-β production inhibitors that can act on Alzhei
Data collection:peptidedb@qq.com

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

Gamma-Secretase Modulators (Amyloid-β production inhibitor) are amyloid-β production inhibitors that can act on Alzheimer's disease (AD).

Physicochemical Properties


Molecular Formula C26H24N3O3F3
Molecular Weight 483.48226
Exact Mass 483.177
CAS # 937812-80-1
PubChem CID 24781184
Appearance White to off-white solid powder
Density 1.37g/cm3
LogP 4.69
Hydrogen Bond Donor Count 0
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 4
Heavy Atom Count 35
Complexity 789
Defined Atom Stereocenter Count 2
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture.
Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


References

[1]. Watahiki H, Yagishita S, Futai E, Ishiura S.CTF1-51, a truncated carboxyl-terminal fragment of amyloid precursor protein, suppresses the effects of Aβ42-lowering γ-secretase modulators.Neurosci Lett. 2012 Sep 27;526(2):96-9. Epub 2012 Aug 23.

[2]. Wanngren J, Ottervald J, Parpal S, Portelius E, Str?mberg K, Borgeg?rd T, Klintenberg R, Juréus A, Blomqvist J, Blennow K, Zetterberg H, Lundkvist J, Rosqvist S, Karlstr?m H.Second generation γ-secretase modulators exhibit different modulation of Notch β.

[3]. Wagner SL, Tanzi RE, Mobley WC, Galasko D.Potential Use of γ-Secretase Modulators in the Treatment of Alzheimer Disease.Arch Neurol. 2012 Jul 16:1-4.

[4]. Bulic B, Ness J, Hahn S, Rennhack A, Jumpertz T, Weggen S.Chemical Biology, Molecular Mechanism and Clinical Perspective of γ-Secretase Modulators in Alzheimer's Disease.Curr Neuropharmacol. 2011 Dec;9(4):598-622.

[5]. Kretner, Benedikt; Fukumori, Akio; Gutsmiedl, Amelie; Page, Richard M.; Luebbers, Thomas; Galley, Guido; Baumann, Karlheinz; Haass, Christian; Steiner, Harald. Attenuated A.beta.42 Responses to Low Potency .gamma.-Secretase Modulators Can Be Overcome for.


Solubility Data


Solubility (In Vitro) DMSO : ≥ 100 mg/mL (~206.83 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.5 mg/mL (5.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (5.17 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

Solubility in Formulation 3: ≥ 2.5 mg/mL (5.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0683 mL 10.3417 mL 20.6834 mL
5 mM 0.4137 mL 2.0683 mL 4.1367 mL
10 mM 0.2068 mL 1.0342 mL 2.0683 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.