[CAS NO. 1304630-27-0] NGP555
PRODUCTS SPECIFICATIONS [1304630-27-0]
DESCRIPTION [1304630-27-0]
Overview
| MDL | MFCD28502195 |
|---|---|
| Molecular Weight | 406.52 |
| Molecular Formula | C23H23FN4S |
| SMILES | CC1=CN(C2=CC=C(C3=CSC(NC4=CC(CC)=C(C)C=C4C)=N3)C=C2F)C=N1 |
Summary
NGP555 is a γ-secretase modulator.
IC50 & Target
γ-secretase [1]
In Vitro
NGP555 potently lowers Aβ 42 in cell cultures (9 nM) while increasing shorter forms of Aβ [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NGP555 significantly lowers Aβ 42 in the cerebrospinal fluid (CSF) at time points from 8 to10 hours post dose, panel B shows that reduction of Aβ cerebrospinal fluid (CSF) levels is significant at 3.75 mg/kg of NGP555 and above, and panel C shows an increase in Aβ 38 levels at 15 mg/kg of NGP555 and above. When combining the reduction of Aβ 42 with an increase in Aβ 38 , NGP555 is effective at raising CSF Aβ 38/42 ratio at 1.87 mg/kg and above (panel D). NGP555-treated Tg mice show a significant protection from decline in performance with >65% less decline (P<0.005) when comparing the differential of Tg to non-Tg vehicle-treated mice. NGP555 also shows good oral bioavailability and is brain-penetrant with a brain:plasma ratio of ~0.93 in mice [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02537938 | NeuroGenetic Pharmaceuticals Inc|WCCT Global |
Alzheimer´s Disease
|
January 2016 | Phase 1 |
| NCT02534480 | NeuroGenetic Pharmaceuticals Inc |
Alzheimer´s Disease
|
March 2015 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 25 mg/mL ( 61.50 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4599 mL | 12.2995 mL | 24.5990 mL |
| 5 mM | 0.4920 mL | 2.4599 mL | 4.9198 mL |
| 10 mM | 0.2460 mL | 1.2300 mL | 2.4599 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution
