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.
For research use only. We do not sell to patients.
- CAS No.: 2639936-77-7
- Formula: C30H43ClFN5O7
- Molecular Weight:640.14
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
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. .
Parmacokinetics
In Vivo
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 2639936-77-7
-
Molecular Weight 640.14
-
Formula 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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)