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].
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 1544739-75-4
- 화학식: C29H31NO6S
- 분자량:521.62
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
IC50 & Target
[2]|
GPR40 0.54 nM (EC50) |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1544739-75-4
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분자량 521.62
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화학식 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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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.
Protocol
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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
순도&문서
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)