MK-3903

SKU: orb1226768

Description

MK-3903 is a potent and selective, direct and oral AMPK activator with EC50 of 9 nM; activates 10 of the 12 phosphorylated AMPK (pAMPK) complexes with EC50s of 8-40 nM, improves lipid metabolism and insulin sensitization in mice.

Key Properties

• CAS Number: 1219737-12-8
• MW: 454.91
• Purity: >98% (HPLC)
• Formula: C₂₇H₁₉ClN₂O₃
• SMILES: CC1=C(C=C(C=C1)OC2=NC3=C(N2)C=C(C(=C3)C4=CC=C(C=C4)C5=CC=CC=C5)Cl)C(=O)O
• Target: AMPK
• Solubility: DMSO: 70 mg/mL; Water: Insoluble; Ethanol: Insoluble （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  The pharmacokinetics of MK-3903 (compound 42) in C57BL/6 mice, Sprague to Dawley rats, and beagle dogs are characterized by moderate systemic plasma clearance (5.0 to13 mL/min/kg), a volume of distribution at steady state of 0.6 to 1.1 L/kg, and a terminal halflife of ~2h. Acute oral administration of MK-3903 (3, 10, and 30 mg/kg) to high-fructose fed db/+ mice results in significant inhibition of hepatic fatty acid synthesis (FAS) for all three doses.
• In Vitro:
  MK-3903 (compound 42) is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM. MK-3903 activates 10 of the 12 phosphorylated AMPK (pAMPK) complexes with EC50 values in the range of 8 to 40 nM and maximal activation > 50%. MK-3903 partially activates pAMPK5 (36% max) and it does not activate pAMPK6. MK-3903 demonstrates low permeability (Papp=6x10-6 cm/s) in LLC-PK1 cells42 and is a substrate of human liver uptake transporters OATP1B1 and OATP1B3 (organic anion transporter proteins). Results show that MK-3903 binds moderately to the prostanoid DP2 (CRTH2) receptor (binding IC50 = 1.8 μM) but not in the presence of 10% human serum (binding IC50>86 μM).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MK3903

Quick Database Links

Gene Symbol

AMPK