Medchemexpress LLC 5H-Thieno[2',3':4,5]pyrrolo[2,3-d]pyridazin-5-one, 6-[(3-aminophenyl)methyl]-4,6-dihydro-4-methy | 1221186-53-3 | 99.9% | 372.46 | 1 ML

Supplier:  Medchemexpress LLC HY1865710MM/1ML

TEPP-46 (ML-265) is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC50 of 92 nM, showing little or no effect on PKM1, PKL and PKR.

• Potent and selective pyruvate kinase M2 (PKM2) activator with an AC50 of 92 nM.
• Exhibits good oral bioavailability with relatively low clearance, long half-life, and good volume of distribution.
• Achieves maximal PKM2 activation in A549 xenograft tumors at 150 mg/kg.
• Prevents pervanadate-induced inhibition of PKM2 activity.
• Induces a decrease in intracellular levels of acetyl-coA, lactate, ribose phosphate, and serine.
• Inhibits LPS-induced Hif-1α and IL-1β.
• Significantly downregulates expression of M1 markers Il12p40 and Cxcl-10.
• Inhibits FSL-1 and CpG-induced Il1b mRNA expression.

Catalog No. 50-003-88069