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.
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- CAS No.: 2639936-77-7
- 화학식: C30H43ClFN5O7
- 분자량:640.14
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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.
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Animal Model:Male 10-12 week old C57BL/6J mice[1]
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Dosage:30 mg/kg or combined with AM-5262 (HY-16619) (30 mg/kg)
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Administration:i.g. for a single dose
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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
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CAS No. 2639936-77-7
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분자량 640.14
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화학식 C30H43ClFN5O7
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)