Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H22N4O5 |
| Molecular Weight | 386.4018 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(CC1=NC(=NO1)C2=NC=C(O)C=C2)C(=O)NC3=C(CCCC3)C(O)=O
InChI
InChIKey=CJHXBFSJXDUJHP-UHFFFAOYSA-N
InChI=1S/C19H22N4O5/c1-19(2,18(27)21-13-6-4-3-5-12(13)17(25)26)9-15-22-16(23-28-15)14-8-7-11(24)10-20-14/h7-8,10,24H,3-6,9H2,1-2H3,(H,21,27)(H,25,26)
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/20184326
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20184326
MK-6892 is niacin receptor 2 agonist, developed by Merkc. In preclinical experiments, it demonstrated reduction of free fatty acid levels by ~85%, with flushing side-effect evident only at the highest dose tested.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3785 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20184326 |
4.0 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20184326
In preclinical experiments MK-6892 was administered to rats at doses between 1 and 100 mg/kg. Compound was administered orally. Plasma free fatty acid levels and vasodilation was monitored.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20184326
Binding to niacin receptor 2 was measured by 3H-NA competition. In these experiments Ki was found to be 4.0 nM (595 nM in 4% human serum). In the guanine nucleotide exchange (GTPγS) assays with membranes from CHO cells expressing the recombinant human GPR109A, the functional activity of GPR109A agonists was determined.
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ACTIVE MOIETY