NGP555

• CAT Number: I012942
• CAS Number: 1304630-27-0
• Molecular Formula: C23H23FN4S
• Molecular Weight: 406.52
• Purity: ≥95%
• Synonyms: N-(5-ethyl-2,4-dimethylphenyl)-4-[3-fluoro-4-(4-methylimidazol-1-yl)phenyl]-1,3-thiazol-2-amine
• InChI: InChI=1S/C23H23FN4S/c1-5-17-10-20(15(3)8-14(17)2)26-23-27-21(12-29-23)18-6-7-22(19(24)9-18)28-11-16(4)25-13-28/h6-13H,5H2,1-4H3,(H,26,27)
• InChIKey: WDEKUGNKKOGFOA-UHFFFAOYSA-N
• SMILES: CCC1=CC(=C(C=C1C)C)NC2=NC(=CS2)C3=CC(=C(C=C3)N4C=C(N=C4)C)F

NGP555 is a γ-secretase modulator. NGP555 Lowers the Amyloid Biomarker Aβ42[1].
NGP555 potently lowers Aβ42 in cell cultures (9 nM) while increasing shorter forms of Aβ[1].
NGP555 significantly lowers Aβ42 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 Aβ38 levels at 15 mg/kg of NGP555 and above. When combining the reduction of Aβ42 with an increase in Aβ38, NGP555 is effective at raising CSF Aβ38/42 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].

Reference

[1]. Kounnas MZ, et al. NGP 555, a γ-Secretase Modulator, Lowers the Amyloid Biomarker, Aβ42, in Cerebrospinal Fluid while Preventing Alzheimer’s Disease Cognitive Decline in Rodents. Alzheimers Dement (N Y). 2017 Jan;3(1):65-73.
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