Description
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
Product information
CAS Number: 1914989-49-3
Molecular Weight: 418.47
Formula: C23H23FN6O
Chemical Name: N-[(1S)-1-(4-fluorophenyl)ethyl]-6-[6-methoxy-5-(4-methyl-1H-imidazol-1-yl)pyridin-2-yl]-4-methylpyridazin-3-amine
Smiles: CC1=CC(=NN=C1N[C@@H](C)C1C=CC(F)=CC=1)C1C=CC(=C(N=1)OC)N1C=NC(C)=C1
InChiKey: JZCREVMHGYOLRL-INIZCTEOSA-N
InChi: InChI=1S/C23H23FN6O/c1-14-11-20(28-29-22(14)26-16(3)17-5-7-18(24)8-6-17)19-9-10-21(23(27-19)31-4)30-12-15(2)25-13-30/h5-13,16H,1-4H3,(H,26,29)/t16-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (238.97 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vivo:
BPN-15606 (oral administration; 10 mg/kg, 25 mg/kg and 50 mg/kg; 7 days) shows excellent dose-dependent efficacy in both plasma and brain on lowering of Aβ42 and Aβ40 levels in mice. BPN-15606 (oral administration; 5 mg/kg, 25 mg/kg and 50 mg/kg; 9 days) dose-dependently reduces CSF on lowering of Aβ42 and Aβ40 levels in rats. BPN-15606 (oral administration; 25 mg/kg; single dose) shows a robust effect on both brain and plasma Aβ 42 and Aβ40 levels, which begins approximately 30–60 minutes following the single dose administration and lasted for ≥24 hours in C57BL/6 mice.
References:
- Wagner SL, et al. Pharmacological and Toxicological Properties of the Potent Oral γ-Secretase Modulator BPN-15606. J Pharmacol Exp Ther. 2017 Jul;362(1):31-44.
Products are for research use only. Not for human use.
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