[CAS NO. 1039758-22-9] MK-4074
PRODUCTS SPECIFICATIONS [1039758-22-9]
DESCRIPTION [1039758-22-9]
Overview
| MDL | MFCD31630723 |
|---|---|
| Molecular Weight | 565.62 |
| Molecular Formula | C33H31N3O6 |
| SMILES | O=C1CC2(CCN(C(C3=CC(OC)=C4C(N(C5CC5)C=C4C)=C3)=O)CC2)OC6=CC=C(C7=CN=CC(C(O)=O)=C7)C=C16 |
3 Publications Citing Use of MCE
Summary
MK-4074 is a liver-specific inhibitor of acetyl-CoA carboxylase ACC1 and ACC2 with IC 50 values of approximately 3 nM.
IC50 & Target
IC50: 3 nM (Acetyl-CoA Carboxylase) [1]
In Vitro
MK-4074 strongly inhibits both ACC1 and ACC2 with IC 50 values of approximately 3 nM. MK-4074 is highly liver specific because it is a substrate of organic anion transport protein (OATP) transporters that are present only in hepatocytes, and excretion of MK-4074 from hepatocytes into bile is dependent on the MRP2 efflux transporter [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
In male KKAy mice, a mouse model of obesity, type 2 diabetes, and fatty liver, a single oral dose of MK-4074 (0.3-3 mg/kg) significantly decreases DNL in a dose-dependent manner with an ID 50 value of 0.9 mg/kg 1 hr post-administration. In a time course study, MK-4074 orally at 30 mg/kg reduces hepatic DNL by 83%, 70%, and 51% at 4, 8, and 12 hr post-dose, respectively. Single oral doses of MK-4074 at 30 and 100 mg/kg significantly increases plasma total ketones, a surrogate biomarker for hepatic FAO, by 1.5-fold to 3-fold for up to 8 hr [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01431521 | Merck Sharp & Dohme LLC |
Non-alcoholic Fatty Liver Disease
|
October 26, 2011 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 88.40 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7680 mL | 8.8399 mL | 17.6797 mL |
| 5 mM | 0.3536 mL | 1.7680 mL | 3.5359 mL |
| 10 mM | 0.1768 mL | 0.8840 mL | 1.7680 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution