Cas No.: | 1219737-12-8 |
Chemical Name: | MK-3903 |
Synonyms: | MK-3903;MK 3903;5-((5-([1,1'-biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic acid;MK3903;BCP29075;BDBM50246120;s8803;ZB1534;5-((5-([1,1a?biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic acid;5-[(5-biphenyl-4-yl-6-chloro-1H-benzimidazol-2-yl)oxy]-2-methylbenzoic acid;5-[[6-chloro-5-(4-phenylphenyl)-1H-benzimidazol-2-yl]oxy]-2-methylbenzoic acid;CID 45256689; MK 3903; MK3903;1219737-12-8;Benzoic acid, 5-[(5-[1,1'-biphenyl]-4-yl-6-chloro-1H-benzimidazol-2-yl)oxy]-2-methyl-;AMPK,MK3903,AMP-activated protein kinase,inhibit,Inhibitor,MK-3903 |
SMILES: | ClC1=CC2=C(C=C1C1C=CC(C3C=CC=CC=3)=CC=1)N=C(N2)OC1C=CC(C)=C(C(=O)O)C=1 |
Formula: | C27H19ClN2O3 |
M.Wt: | 454.904365777969 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM. |
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[1]. |
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=6×10-6 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)[1]. |