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BI 689648

Catalog No. T14664   CAS 1633009-87-6

BI 689648 is a highly selective inhibitor of aldosterone synthase(CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively).

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BI 689648 Chemical Structure
BI 689648, CAS 1633009-87-6
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 985.00
50 mg 6-8 weeks $ 1,280.00
100 mg 6-8 weeks $ 1,940.00
1 mL * 10 mM (in DMSO) 6-8 weeks $ 272.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BI 689648 is a highly selective inhibitor of aldosterone synthase(CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively).
Targets&IC50 CYP11B2:2.1 nM, CYP11B1:310 nM
In vitro In comparison with FADs and LCI699, BI 689648 exhibits remarkable selectivity in vitro, demonstrating an IC50 value of 2.1 nM for CYP11B2 and a selectivity factor of 149 over CYP11B1. Meanwhile, FAD286 presents a comparable IC50 value for CYP11B2 at 2.5 nM, but its higher efficacy against CYP11B1 (94 nM) yields a relatively lower selectivity factor of 38, which is about fourfold lesser than that of BI 689648[1].
In vivo After oral administration in cyno monkeys, BI 689648 (5 mg/kg) exhibits a peak plasma concentration of ~500 nM. BI 689648 exhibits minimal impact on 11-DC and only at very high plasma concentrations (~10 μM)[1]. 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.
Molecular Weight 298.34
Formula C16H18N4O2
CAS No. 1633009-87-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (100.56 mM), Sonication and heating are recommended.

TargetMolReferences and Literature

1. Weldon SM, et al. Selectivity of BI 689648, a Novel, Highly Selective Aldosterone Synthase Inhibitor: Comparison with FAD286 and LCI699 in Nonhuman Primates. J Pharmacol Exp Ther. 2016 Oct;359(1):142-50.

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Keywords

BI 689648 1633009-87-6 Others BI689648 BI-689648 inhibitor inhibit

 

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