MK 1903

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Cat.No. 4622 - MK 1903 | CAS No. 1268882-43-4
Description: Potent and selective GPR109A (HCA2) agonist
Chemical Name: (4aR,5aR)-4,4a,5,5a-Tetrahydro-1H-cyclopropa[4,5]cyclopenta[1,2]pyrazole-3-carboxylic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

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.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 16.42 100
ethanol 8.21 50

Preparing Stock Solutions

The following data is based on the product molecular weight 164.16. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: MK1903 HCA2 hydroxycarboxylic acid receptors GPR109A HM74A agonists Hydroxycarboxylic Acid Receptors

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