K-833
K-833 is a GPR119 agonist with EC50 values of 39.8 nM (human), 100nM (mouse), 75.4 nM (rat) and 12.6 nM (dog). K-833 demonstrates a modest increase in GLP-1 secretion and leads to a synergistic increase in GLP-1 levels when combined with AM-5262 (HY-16619) in acute gut peptide secretion assays in mice. K-833 can be used in studies on weight loss.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 2639936-77-7
- Formule: C30H43ClFN5O7
- Masse moléculaire:640.14
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
K-833 shows modest antagonism of the human M1 receptor (IC50 = 4.5 μM), inhibition of agonist binding to the human nonselective sigma receptors (IC50 = 2.7 μM) and moderate reversible inhibition of the CYP2B6 (IC50 = 8.6 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male 10-12 week old C57BL/6J mice[1]
-
Dosage:30 mg/kg or combined with AM-5262 (HY-16619) (30 mg/kg)
-
Administration:i.g. for a single dose
-
Result:Led to a modest increase in GLP-1 secretion.
Led to a synergistic increase in GLP-1 levels when combined with AM-5262.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 2639936-77-7
-
Masse moléculaire 640.14
-
Formule C30H43ClFN5O7
-
SMILES
OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)CNCC1CN(C(CC2=CC=C(OCCCC3CCN(C4=NC=C(Cl)C=N4)CC3)C=C2F)=O)C1
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)