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Submit ReviewMK 1903 is a potent and selective hydroxycarboxylic acid receptor 2 (HCA2, GPR109A) full agonist; exhibits greater potency than niacin in a whole cell HTRF-cAMP assay (EC50 values are 12.9 and 51 nM respectively). Exhibits no binding at the GRP109B receptor.
MK 1903 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 164.16 |
公式 | C8H8N2O2 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1268882-43-4 |
PubChem ID | 49763030 |
InChI Key | CUTZNERBKDMLAP-QWWZWVQMSA-N |
Smiles | [H][C@@]12CC3=C(NN=C3C(O)=O)[C@@]([H])1C2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 16.42 | 100 | |
ethanol | 8.21 | 50 |
以下数据基于产品分子量 164.16。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 6.09 mL | 30.46 mL | 60.92 mL |
5 mM | 1.22 mL | 6.09 mL | 12.18 mL |
10 mM | 0.61 mL | 3.05 mL | 6.09 mL |
50 mM | 0.12 mL | 0.61 mL | 1.22 mL |
参考文献是支持产品生物活性的出版物。
Boatman (2012) (1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[α]pentalene-4-carboxylic acid (MK-1903): a potent GPR109a agonist that lowers free fatty acids in humans. J.Med.Chem. 55 3644 PMID: 22435740
Lauring (2012) Niacin lipid efficacy is independent of both the niacin receptor GPR109A and free fatty acid suppression. Sci.Transl.Med. 4 148ra115 PMID: 22914621
If you know of a relevant reference for MK 1903, please let us know.
关键词: MK 1903, MK 1903 supplier, MK1903, HCA2, hydroxycarboxylic, acid, receptors, GPR109A, HM74A, agonists, Hydroxycarboxylic, Acid, Receptors, 4622, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 MK 1903 的部分引用包括:
Martin-Gallausiaux et al (2019) Butyrate Produced by Commensal Bacteria Down-Regulates Indolamine 2,3-Dioxygenase 1 (IDO-1) Expression via a Dual Mechanism in Human Intestinal Epithelial Cells. Front Immunol 9 2838 PMID: 30619249
Marinelli et al (2019) Identification of the novel role of butyrate as AhR ligand in human intestinal epithelial cells Sci.Rep. 9 643 PMID: 30679727
Elisabetta et al (2023) Targeting gut dysbiosis against inflammation and impaired autophagy in Duchenne muscular dystrophy. EMBO Mol Med 15 e16225 PMID: 36594243
Perrone et al (2023) Potential role of the hydroxyl carboxylic acid receptor type 2 (HCAR2) in microglia pathophysiology: A possible cross-talk with C-X-C chemokine receptor 1 (CXCR1) Neuropharmacology PMID: 36796675
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