MK-8666
MK-8666 is a potent and selective partial GPR40 agonist (EC50 = 0.54 nM for human GPR40). MK-8666 shows selectivity over GPR119, GPR43, GPR41, GPR120, and other G-protein-coupled receptors (GPCRs). MK-8666 reduces glucose in the rodent. MK-8666 can be used for type 2 diabetes research[1][2].
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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: 1544739-75-4
- 分子式: C29H31NO6S
- 分子量:521.62
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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
製品説明
IC50 & Target
[2]|
GPR40 0.54 nM (EC50) |
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1544739-75-4
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分子量 521.62
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分子式 C29H31NO6S
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SMILES
O=C(O)[C@H]1[C@]([H])(CC2=C3C=NC(OCC4=CC(C5=C(C=C(C=C5C)OCCCS(=O)(C)=O)C)=CC=C4)=C2)[C@@]13[H]
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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.
プロトコル
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
純度とドキュメンテーション
参考文献
[1]. Krug AW, et al. Leveraging a Clinical Phase Ib Proof-of-Concept Study for the GPR40 Agonist MK-8666 in Patients With Type 2 Diabetes for Model-Informed Phase II Dose Selection. Clin Transl Sci. 2017 Sep;10(5):404-411. [Content Brief]
[2]. Pachanski MJ, et al. GPR40 partial agonists and AgoPAMs: Differentiating effects on glucose and hormonal secretions in the rodent. PLoS One. 2017 Oct 20;12(10):e0186033. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)