2. Immunology/Inflammation Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. Glucocorticoid Receptor Mineralocorticoid Receptor 11β-HSD
  4. INCB13739

INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC), respectively. INCB13739 can be used for type 2 diabetes mellitus (T2DM) and obesity research.

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

INCB13739 Chemical Structure

INCB13739 Chemical Structure

CAS No. : 869974-19-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 309 In-stock
Solution
10 mM * 1 mL in DMSO USD 309 In-stock
Solid
5 mg USD 300 In-stock
10 mg USD 480 In-stock
25 mg USD 950 In-stock
50 mg USD 1450 In-stock
100 mg USD 2250 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

INCB13739 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC), respectively. INCB13739 can be used for type 2 diabetes mellitus (T2DM) and obesity research[1].

IC50 & Target

IC50: 3.2 nM (11β-HSD1 enzymatic), 1.1 nM (11β-HSD1 PBMC)[1]
In Vitro

INCB13739 is >1000-fold selective towards 11β-HSD2, mineralocorticoid receptor (MR), and glucocorticoid receptor (GR)[1].

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

INCB13739 Related Antibodies
In Vivo

INCB13739 (Orally) is effectively distributed in the adipose tissue and is inhibiting 11β-HSD1 activity > 90% for at least 24 h post-dose[1].
INCB13739 (3 mg/kg, IV; 10 mg/kg, PO; once) displays decent oral bioavailability in both rats and cynomolgus monkeys[1].
Pharmacokinetic Parameters of INCB13739 in rats[1].

IV (3 mg/kg) PO (10 mg/kg)
Cmax (µM) 6.46 ± 2.41
AUC0-24 (ng/mL∗h) 11.2 ± 3.27
t1/2 (h) 1.4 ± 0.2 1.2 ± 0.3
CL ((L/h)/kg) 1.0 ± 0.2
Vdss (L/kg) 1.6 ± 0.5
F (%) 51 ± 15

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

Animal Model: Rats, cynomolgus monkeys[1]
Dosage: 3 mg/kg (IV), 10 mg/kg (PO)
Administration: IV and PO, once (Pharmacokinetic Analysis)
Result: Displayed decent oral bioavailability in both rats (F%=51 ± 15%) and cynomolgus monkeys (F%=43%).
Clinical Trial
Molecular Weight

467.52

Formula

C28H25N3O4
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=NC=C(C2=CC=C(C3(C(N4C[C@]5(CC4)OC(C6=C5C=CC=C6)=O)=O)CC3)C=C2)C=C1)NC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (267.37 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 2.1389 mL 10.6947 mL 21.3895 mL
5 mM 0.4278 mL 2.1389 mL 4.2779 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)

Mass
=
Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.08 mg/mL (4.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1389 mL 10.6947 mL 21.3895 mL 53.4736 mL
5 mM 0.4278 mL 2.1389 mL 4.2779 mL 10.6947 mL
10 mM 0.2139 mL 1.0695 mL 2.1389 mL 5.3474 mL
15 mM 0.1426 mL 0.7130 mL 1.4260 mL 3.5649 mL
20 mM 0.1069 mL 0.5347 mL 1.0695 mL 2.6737 mL
25 mM 0.0856 mL 0.4278 mL 0.8556 mL 2.1389 mL
30 mM 0.0713 mL 0.3565 mL 0.7130 mL 1.7825 mL
40 mM 0.0535 mL 0.2674 mL 0.5347 mL 1.3368 mL
50 mM 0.0428 mL 0.2139 mL 0.4278 mL 1.0695 mL
60 mM 0.0356 mL 0.1782 mL 0.3565 mL 0.8912 mL
80 mM 0.0267 mL 0.1337 mL 0.2674 mL 0.6684 mL
100 mM 0.0214 mL 0.1069 mL 0.2139 mL 0.5347 mL
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INCB13739 Related Classifications

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:

INCB13739869974-19-6INCB 13739INCB-13739Glucocorticoid ReceptorMineralocorticoid Receptor11β-HSD11beta-HSD11β-hydroxysteroid dehydrogenases11 beta-hydroxysteroid dehydrogenasetype 2 diabetesglucosemellitusMetabolic syndromeSteroid mimeticSpiro heterocyclic compoundsTissue specificperipheral blood mononuclear cellPBMCInhibitorinhibitorinhibit

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