BPN-15606 besylate

BPN-15606 besylate 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 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance.

Product information

Molecular Weight: 576.64

Formula: C29H29FN6O4S

Chemical Name: benzenesulfonic acid;N-[(1S)-1-(4-fluorophenyl)ethyl]-6-[6-methoxy-5-(4-methylimidazol-1-yl)pyridin-2-yl]-4-methylpyridazin-3-amine

Smiles: CC1C=C(N=NC=1N[C@@H](C)C1C=CC(F)=CC=1)C1=CC=C(C(=N1)OC)N1C=NC(C)=C1.OS(=O)(=O)C1C=CC=CC=1

InChiKey: GUUNWNSGODFODV-NTISSMGPSA-N

InChi: InChI=1S/C23H23FN6O.C6H6O3S/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;7-10(8,9)6-4-2-1-3-5-6/h5-13,16H,1-4H3,(H,26,29);1-5H,(H,7,8,9)/t16-;/m0./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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 Vitro:

BPN-15606 besylate (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 besylate (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 besylate (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.

Products are for research use only. Not for human use.