BI 689648 is a novel, highly selective aldosterone synthase inhibitor which can inhibit CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively.

Product information

CAS Number: 1633009-87-6

Molecular Weight: 298.34

Formula: C16H18N4O2

Chemical Name: 6-[5-(methoxymethyl)pyridin-3-yl]-1,2,3,4-tetrahydro-1,8-naphthyridine-1-carboxamide

Smiles: COCC1C=C(C=NC=1)C1C=NC2=C(CCCN2C(N)=O)C=1

InChiKey: DJFDCVNQDFICKV-UHFFFAOYSA-N

InChi: InChI=1S/C16H18N4O2/c1-22-10-11-5-13(8-18-7-11)14-6-12-3-2-4-20(16(17)21)15(12)19-9-14/h5-9H,2-4,10H2,1H3,(H2,17,21)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 30 mg/mL (100.56 mM; Need ultrasonic and warming).

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:

Compare with the FADs and LCI699, BI 689648 is highly selective in vitro, providing an IC50 for CYP11B2 of 2.1 nM and a selectivity factor of 149 over CYP11B1. FAD286, by comparison, shows a similar IC50 for CYP11B2 (2.5 nM); however, its greater potency against CYP11B1 (94 nM) results in a comparatively modest selectivity factor of 38, approximately 4-fold less than BI 689648.

In Vivo:

After oral administration in cyno monkeys, BI 689648 (5 mg/kg) exhibits a peak plasma concentration of ~500 nM. For BI 689648 (aldosterone EC50=2 nM), appreciable changes in 11-DOC are only noted at plasma concentrations >2000 nM or >1000-fold its aldosterone EC50 while FAD286 shows a window of ~100-fold. BI 689648 exhibits minimal impact on 11-DC and only at very high plasma concentrations (~10 μM).

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