Home Proteases Secretase modulator NGP 555

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NGP 555 Secretase modulator

Cat.No.S8603

NGP 555 is a small-molecule modulator of γ-secretase and has been successful in achieving good oral absorption, brain penetration, CNS activity, and specificity for a lipid-based membrane target preclinically.
NGP 555 Secretase modulator Chemical Structure

Chemical Structure

Molecular Weight: 406.52

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Quality Control

Batch: S860301 DMSO]40 mg/mL]false]Ethanol]3 mg/mL]false]Water]Insoluble]false Purity: 99.06%
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99.06

Solubility

In vitro
Batch:

DMSO : 40 mg/mL (98.39 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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g
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%
% Tween 80
% ddH2O
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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 406.52 Formula

C23H23FN4S

 Storage (From the date of receipt)
CAS No. 1304630-27-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCC1=CC(=C(C=C1C)C)NC2=NC(=CS2)C3=CC(=C(C=C3)N4C=C(N=C4)C)F

Mechanism of Action

Targets/IC50/Ki
γ secretase
(Cell-free assay)
In vivo
NGP 555 has very good brain penetration/absorption, distribution, metabolism, and excretion (ADME) properties. It efficiently crosses the blood-brain barrier, has a brain:plasma ratio of 0.93 (in Tg2576 mice) and shows in vivo efficacy for lowering the biomarker Aβ42 in rodent studies for brain and plasma. Chronic administration of this compound (milled into chow) to Tg2576 mice results in a significant reduction of amyloid plaques.
References

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