≥97% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Panoramica
Information
MK-3903 MK-3903 is a potent and selective AMPK activator with an EC50 of 8 nM for α1 β1 γ1 subunit. It activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation >50%.
Targets
AMPK 8 nM(EC50)
In vitro
MK-3903 activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation >50%. The compound partially activates pAMPK5 (36% max), which is only a minor component of human and mouse liver, and it does not activate pAMPK6, which is not detected in liver. MK-3903 is a weak reversible inhibitor of CYP3A4 and 2D6 in human liver microsomes (apparent IC50 > 50 μM) and does not exhibit time-dependent inhibition of CYP3A4 activity. MK-3903 is not a potent PXR agonist.
In vivo
The pharmacokinetics of MK-3903 in C57BL/6 mice, Sprague–Dawley rats, and beagle dogs were characterized by moderate systemic plasma clearance (5.0–13 mL/min/kg), a volume of distribution at steady state of 0.6–1.1 L/kg, and a terminal half-life of ∼2 h. It has low oral bioavailability (8.4%) in C57BL/6 mice, but the oral exposure is later improved using other vehicles. Oral bioavailabilities in rats and dogs are improved (27-78%). Chronic oral administration of compound MK-3903 robustly increased ACC phosphorylation in liver with more modest effects in skeletal muscle. Treatment of various mouse models with MK-3903 results in expected alterations in lipid metabolism and improvements in a measure of insulin sensitization.
Specifications
Specifiche e purezza
≥97%
Meccanismi biochimici e fisiologici
MK-3903 is a potent and selective AMPK activator with an EC50 of 8 nM for α1 β1 γ1 subunit. It activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation >50%.
Condizioni di conservazione di stoccaggio
Store at -20°C
Spedito in
Ice chest + Ice pads
Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.
This compound belongs to the class of organic compounds known as biphenyls and derivatives. These are organic compounds containing to benzene rings linked together by a C-C bond.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
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Recensioni
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Domande frequenti
What is the purity of this product?
This product is supplied at ≥97% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.
How should this product be stored?
Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.
How is this product shipped?
This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.
What are the CAS number, molecular formula and molecular weight?
The CAS Number is 1219737-12-8, the molecular formula is C27H19ClN2O3, and the molecular weight is 454.9 g/mol. InChIKey FIKQZQDYGXAUHC-UHFFFAOYSA-N.
What documentation is provided?
Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.
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