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INCB13739

🥰Excellent
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

INCB13739

🥰Excellent
Catalog No. T60203Alias INCB013739, INCB 13739, INCB 013739Cas No. 869974-19-6
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.
Pack SizePriceAvailabilityQuantity
1 mg$109In Stock
5 mg$238In Stock
10 mg$383In Stock
25 mg$759In Stock
50 mg$1,050In Stock
100 mg$1,390In Stock
200 mg$1,890In Stock
1 mL x 10 mM (in DMSO)$253In Stock
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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 in 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]
AliasINCB013739, INCB 13739, INCB 013739
Chemical Properties
Molecular Weight467.52
FormulaC28H25N3O4
Cas No.869974-19-6
SmilesC(=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
Storagekeep 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.
Solubility Information
DMSO: 100 mg/mL (213.89 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1389 mL10.6947 mL21.3895 mL106.9473 mL
5 mM0.4278 mL2.1389 mL4.2779 mL21.3895 mL
10 mM0.2139 mL1.0695 mL2.1389 mL10.6947 mL
20 mM0.1069 mL0.5347 mL1.0695 mL5.3474 mL
50 mM0.0428 mL0.2139 mL0.4278 mL2.1389 mL
100 mM0.0214 mL0.1069 mL0.2139 mL1.0695 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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Keywords

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