1235995-16-0
Chemical Structure
MK-1421
- CAS No.: 1235995-16-0
- Formula:C27H24FN9O2
- Molecular Weight:525.54
IUPAC Name: 5-((1R,3R)-1-(1-ethyl-1H-pyrazol-4-yl)-3-(4-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)-3-methyl-1,3,4-oxadiazol-2(3H)-one
InChIKey: RETOYYSEVCBIRN-JIPXPUAJSA-N
SMILES: FC(C=C1)=CN=C1C2=CNC([C@@H]3N[C@@](C4=CN(CC)N=C4)(C5=NN(C)C(O5)=O)C6=C(C(C=CC=C7)=C7N6)C3)=N2
Biological Activity: MK-1421 is an orally active sstr3 antagonist. MK-1421 inhibits sstr3 with IC50 values of 2.3 nM (human), 1.3 nM (mouse), 0.6 nM (rat), 2.5 nM (dog), and 1.0 nM (rhesus monkey). MK-1421 inhibits hERG (human IC50 32.2 μM). MK-1421 dose-dependently reduces blood glucose fluctuations and enhances insulin secretion under high glucose conditions but not low glucose conditions, without affecting glucagon or somatostatin release. MK-1421 can be used for research on type 2 diabetes[1].
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MK-1421 | MK-1421 is an orally active sstr3 antagonist. MK-1421 inhibits sstr3 with IC50 values of 2.3 nM (human), 1.3 nM (mouse), 0.6 nM (rat), 2.5 nM (dog), and 1.0 nM (rhesus monkey). MK-1421 inhibits hERG (human IC50 32.2 μM). MK-1421 dose-dependently reduces blood glucose fluctuations and enhances insulin secretion under high glucose conditions but not low glucose conditions, without affecting glucagon or somatostatin release. MK-1421 can be used for research on type 2 diabetes. | |||||||||||||||||||||
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