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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. Find out more about compound libraries available from Tocris.
M. Wt | 164.16 |
Formula | C8H8N2O2 |
Storage | Store at +4°C |
Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 16.42 | 100 | |
ethanol | 8.21 | 50 |
The following data is based on the product molecular weight 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.
Concentration / Solvent Volume / Mass | 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 |
References are publications that support the biological activity of the product.
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.
Keywords: MK 1903, MK 1903 supplier, MK1903, HCA2, hydroxycarboxylic, acid, receptors, GPR109A, HM74A, agonists, Hydroxycarboxylic, Acid, Receptors, 4622, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for MK 1903 include:
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
Elisabetta et al (2023) Targeting gut dysbiosis against inflammation and impaired autophagy in Duchenne muscular dystrophy. EMBO Mol Med 15 e16225 PMID: 36594243
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
Do you know of a great paper that uses MK 1903 from Tocris? Please let us know.
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