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(R)-BMS-816336 

Cat. No.: HY-101930B
Handling Instructions

(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively .

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

(R)-BMS-816336 Chemical Structure

(R)-BMS-816336 Chemical Structure

CAS No. : 1009583-83-8

Size Price Stock
10 mM * 1 mL in DMSO USD 265 Ask For Quote & Lead Time
5 mg USD 350 Ask For Quote & Lead Time
10 mg USD 550 Ask For Quote & Lead Time
50 mg USD 1650 Ask For Quote & Lead Time
100 mg USD 2250 Ask For Quote & Lead Time

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Description

(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively [1].

IC50 & Target

IC50: 14.5 nM (Human 11β-HSD1), 50.3 nM (Mouse 11β-HSD1) and 16 nM (Cynomolgus monkey 11β-HSD1)[1]

In Vivo

During the in vivo studies of BMS-816336 (Compound 6n-2) in animals, its enantiomer (R)-BMS-816336 (Compound 6n-1) in the plasma samples, together with trace amount of Ketone A are detected. The interconversion of BMS-816336 and (R)-BMS-816336 take place via the intermediate Ketone A through physiological oxidation and reduction process. In vivo studies in rat, dog, and cynomolgus monkey, the plasma ratios of (R)-BMS-816336/BMS-816336 decrease in the order: dog ≫ rat >cynomolgus monkey[1].

Molecular Weight

341.44

Formula

C₂₁H₂₇NO₃

CAS No.

1009583-83-8

SMILES
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 300 mg/mL (878.63 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9288 mL 14.6439 mL 29.2877 mL
5 mM 0.5858 mL 2.9288 mL 5.8575 mL
10 mM 0.2929 mL 1.4644 mL 2.9288 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 7.5 mg/mL (21.97 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 7.5 mg/mL (21.97 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 7.5 mg/mL (21.97 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

(R)-BMS-816336Others11β-HSD1BMS-816336enantiomerplasmaratiosInhibitorinhibitorinhibit

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(R)-BMS-816336
Cat. No.:
HY-101930B
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