(R)-BMS-816336

Cat. No.: HY-101930B: FAQs
Data Sheet SDS Handling Instructions

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(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

CAS No. : 1009583-83-8

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Other Forms of (R)-BMS-816336:

BMS-816336 Get quote
(Rac)-BMS-816336 Get quote

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Purity & Documentation
References
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Description

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].

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

Molecular Weight

341.44

Formula

C₂₁H₂₇NO₃

CAS No.

1009583-83-8

Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1[C@H]2C[C@@H]3[C@@](C4=CC=CC=C4)(CC(N5CC(O)C5)=O)[C@@H](C[C@H]1C3)C2

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 7.5 mg/mL (21.97 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Data Sheet (274 KB) SDS (102 KB) Handling Instructions (2659 KB)

References

[1]. Ye XY, et al. Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3'-hydroxyazetidin-1-yl)ethanone [BMS-816336], an Orally Active Novel Selective 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor. J Med Chem. 2017 Jun 22;60(12):4932-4948. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9288 mL	14.6439 mL	29.2877 mL	73.2193 mL
	5 mM	0.5858 mL	2.9288 mL	5.8575 mL	14.6439 mL
	10 mM	0.2929 mL	1.4644 mL	2.9288 mL	7.3219 mL
	15 mM	0.1953 mL	0.9763 mL	1.9525 mL	4.8813 mL
	20 mM	0.1464 mL	0.7322 mL	1.4644 mL	3.6610 mL
	25 mM	0.1172 mL	0.5858 mL	1.1715 mL	2.9288 mL
	30 mM	0.0976 mL	0.4881 mL	0.9763 mL	2.4406 mL
	40 mM	0.0732 mL	0.3661 mL	0.7322 mL	1.8305 mL
	50 mM	0.0586 mL	0.2929 mL	0.5858 mL	1.4644 mL
	60 mM	0.0488 mL	0.2441 mL	0.4881 mL	1.2203 mL
	80 mM	0.0366 mL	0.1830 mL	0.3661 mL	0.9152 mL
	100 mM	0.0293 mL	0.1464 mL	0.2929 mL	0.7322 mL

(R)-BMS-816336 Related Classifications

Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(R)-BMS-8163361009583-83-811β-HSD11beta-HSD11β-hydroxysteroid dehydrogenases11 beta-hydroxysteroid dehydrogenase11β-HSD1BMS-816336enantiomerplasmaratiosInhibitorinhibitorinhibit

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