1. Metabolic Enzyme/Protease
  2. Cytochrome P450

BI 689648 

Cat. No.: HY-101217 Purity: 99.20%
Handling Instructions

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.

For research use only. We do not sell to patients.

BI 689648 Chemical Structure

BI 689648 Chemical Structure

CAS No. : 1633009-87-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 591 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 540 In-stock
Estimated Time of Arrival: December 31
10 mg USD 900 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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.

IC50 & Target

IC50: 310 nM (CYP11B1), 2.1 nM (CYP11B2)[1]

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[1].

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)[1].

Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3519 mL 16.7594 mL 33.5188 mL
5 mM 0.6704 mL 3.3519 mL 6.7038 mL
10 mM 0.3352 mL 1.6759 mL 3.3519 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Homogenized adrenal glands are used to evaluate test compounds (including BI 689648) in a 96-well plate format. A mixture of concentrated homogenate and substrate is added to compound dilutions for analysis. Values for the concentration required to inhibit CS (CYP11B1) and AS (CYP11B2) enzyme activity by 50% (IC50) are calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

For aldosterone synthase inhibitors (ASI) evaluation, the study cohort consists of 66 healthy animals. Each separate study day, 12 cyno monkeys are randomized to receive various doses of ASI or vehicle control (n=3/group); the animals are reused across studies, allowing a minimum of 2 weeks washout between studies. Aggregation of data across multiple studies is used to derive in vivo effective concentration (EC) values for aldosterone and cortisol by curve-fitting. Conscious, nonchaired monkeys receive vehicle (n=35), S-FAD (n=9), FAD286 (n=24), LCI699 (n=36), or BI 689648 (n=26) at doses ranging from 0.003 mg/kg to 10 mg/kg. Maximal adrenocorticotropin (ACTH)-induced aldosterone and cortisol production occurs quickly, within 15 minutes after challenge, at which time blood is collected for plasma aldosterone, cortisol, and test compound concentrations[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

298.34

Formula

C₁₆H₁₈N₄O₂

CAS No.

1633009-87-6

SMILES

O=C(N1CCCC2=C1N=CC(C3=CC(COC)=CN=C3)=C2)N

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
BI 689648
Cat. No.:
HY-101217
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BI 689648

Cat. No.: HY-101217