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INCB13739

Name: INCB13739
Brand: TargetMol
SKU: T60203
Price: 100 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T60203Cas No. 869974-19-6

Alias INCB013739, INCB 13739, INCB 013739

INCB13739 is an orally active, selective, and highly efficient 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor. INCB13739 improves hyperglycemia in patients with uncontrolled type 2 diabetes on metformin monotherapy and can be used in hyperlipidemia and hypertriglyceridemia research.

INCB13739

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Purity: 99.32%

Catalog No. T60203Alias INCB013739, INCB 13739, INCB 013739Cas No. 869974-19-6

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$100	-	In Stock
5 mg	$238	-	In Stock
10 mg	$383	-	In Stock
25 mg	$759	-	In Stock
50 mg	$1,050	-	In Stock
100 mg	$1,390	-	In Stock
200 mg	$1,890	-	In Stock
1 mL x 10 mM (in DMSO)	$253	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.32%

Appearance:Solid

Color:Gray

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	INCB13739 is an orally active, selective, and highly efficient 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor. INCB13739 improves hyperglycemia in patients with uncontrolled type 2 diabetes on metformin monotherapy and can be used in hyperlipidemia and hypertriglyceridemia research.
Targets&IC50	11β-HSD1 (PBMC):1.1 nM, 11β-HSD1:3.2 nM
In vitro	INCB13739 is an orally active, potent, selective, and tissue-specific inhibitor of 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1), with an IC50 of 3.2 nM for 11β-HSD1 enzyme and 1.1 nM for 11β-HSD1 in PBMC. INCB13739 has greater than 1,000-fold selectivity for 11β-HSD2, the salt corticosteroid receptor (MR), and the glucocorticoid receptor (GR). [1]
In vivo	After oral administration, INCB13739 was efficiently distributed to adipose tissue and inhibited 11β-HSD1 activity by >90% for at least 24 h. INCB13739 (3 mg/kg i.v.; 10 mg/kg orally; single dose) exhibited good oral bioavailability in rats (F%=51%) and cynomolgus monkeys (F%=43%). [1]
Synonyms	INCB013739, INCB 13739, INCB 013739

Chemical Properties

Molecular Weight	467.52
Formula	C₂₈H₂₅N₃O₄
Cas No.	869974-19-6
Smiles	C(=O)(C1(CC1)C2=CC=C(C=C2)C=3C=CC(C(NC)=O)=NC3)N4C[C@@]5(CC4)C=6C(C(=O)O5)=CC=CC6
Relative Density.	1.39 g/cm3 (Predicted)

Storage & Solubility Information

Storage

keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (213.89 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.56 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1389 mL	10.6947 mL	21.3895 mL	106.9473 mL
5 mM	0.4278 mL	2.1389 mL	4.2779 mL	21.3895 mL
10 mM	0.2139 mL	1.0695 mL	2.1389 mL	10.6947 mL
20 mM	0.1069 mL	0.5347 mL	1.0695 mL	5.3474 mL
50 mM	0.0428 mL	0.2139 mL	0.4278 mL	2.1389 mL
100 mM	0.0214 mL	0.1069 mL	0.2139 mL	1.0695 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc