INCB13739

SKU: orb1689779

Description

INCB13739 is a potent, selective, and orally bioavailable inhibitor of 11β-HSD1. It has demonstrated efficacy in improving glycemic control in clinical studies of type 2 diabetes and serves as a valuable research tool for investigating metabolic disorders, including dyslipidemia, in both in vitro and in vivo models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 869974-19-6
• MW: 467.52
• Purity: 99.81% (May vary between batches)
• Formula: C₂₈H₂₅N₃O₄
• 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
• Target: Glucocorticoid Receptor,Dehydrogenase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.56 mM);DMSO:100 mg/mL (213.89 mM)

Bioactivity

• Target IC50:
  11β-HSD1:3.2 nM|11β-HSD1 (PBMC):1.1 nM
• 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%).
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• 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).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

INCB013739, INCB 13739, INCB 013739, INCB13739, INCB-13739

Compound Identifiers

PubChem CID

66662059