Product Name :
MK-4074
Description:
MK-4074 is a liver-specific inhibitor of acetyl-CoA carboxylase ACC1 and ACC2 with IC50 values of approximately 3 nM.
CAS:
1039758-22-9
Molecular Weight:
565.62
Formula:
C33H31N3O6
Chemical Name:
5-[1′-(1-cyclopropyl-4-methoxy-3-methyl-1H-indole-6-carbonyl)-4-oxo-3,4-dihydrospiro[1-benzopyran-2,4′-piperidin]-6-yl]pyridine-3-carboxylic acid
Smiles :
CC1=CN(C2CC2)C2=CC(=CC(OC)=C12)C(=O)N1CCC2(CC(=O)C3=CC(=CC=C3O2)C2C=C(C=NC=2)C(O)=O)CC1
InChiKey:
WDBNGXLHMZSUEI-UHFFFAOYSA-N
InChi :
InChI=1S/C33H31N3O6/c1-19-18-36(24-4-5-24)26-13-21(14-29(41-2)30(19)26)31(38)35-9-7-33(8-10-35)15-27(37)25-12-20(3-6-28(25)42-33)22-11-23(32(39)40)17-34-16-22/h3,6,11-14,16-18,24H,4-5,7-10,15H2,1-2H3,(H,39,40)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.BCMA/TNFRSF17 Protein, Human Epigenetic Reader Domain
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
MK-4074 is a liver-specific inhibitor of acetyl-CoA carboxylase ACC1 and ACC2 with IC50 values of approximately 3 nM.Tofacitinib Protocol |Product information|CAS Number: 1039758-22-9|Molecular Weight: 565.62|Formula: C33H31N3O6|Chemical Name: 5-[1′-(1-cyclopropyl-4-methoxy-3-methyl-1H-indole-6-carbonyl)-4-oxo-3,4-dihydrospiro[1-benzopyran-2,4′-piperidin]-6-yl]pyridine-3-carboxylic acid|Smiles: CC1=CN(C2CC2)C2=CC(=CC(OC)=C12)C(=O)N1CCC2(CC(=O)C3=CC(=CC=C3O2)C2C=C(C=NC=2)C(O)=O)CC1|InChiKey: WDBNGXLHMZSUEI-UHFFFAOYSA-N|InChi: InChI=1S/C33H31N3O6/c1-19-18-36(24-4-5-24)26-13-21(14-29(41-2)30(19)26)31(38)35-9-7-33(8-10-35)15-27(37)25-12-20(3-6-28(25)42-33)22-11-23(32(39)40)17-34-16-22/h3,6,11-14,16-18,24H,4-5,7-10,15H2,1-2H3,(H,39,40)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 50 mg/mL (88.40 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.PMID:33351443 |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|MK-4074 strongly inhibits both ACC1 and ACC2 with IC50 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.|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 ID50 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.|Products are for research use only. Not for human use.|