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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2639936-77-7
- 分子式: C30H43ClFN5O7
- 分子量:640.14
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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 |
化学情報
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CAS 番号 2639936-77-7
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分子量 640.14
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)