WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H532185
CAS#: 1268882-43-4
Description: MK-1903 is an agonist of hydroxycarboxylic acid receptor 2 (HCA2), known previously as G protein-coupled receptor 109A (GPR109A). It reduces forskolin-induced cAMP production in a homogenous time-resolved fluorescence (HTRF) assay using CHO cells expressing the human receptor (EC50 = 12.9 nM). MK-1903 is selective for HCA2 over a panel of G protein-coupled receptors (GPCRs) and ion channels (IC50s = >10 µM for all). It reduces plasma free fatty acid levels in fasted rats when administered at doses ranging from 0.001 to 100 mg/kg.
Hodoodo Cat#: H532185
Name: MK-1903
CAS#: 1268882-43-4
Chemical Formula: C8H8N2O2
Exact Mass: 164.06
Molecular Weight: 164.160
Elemental Analysis: C, 58.53; H, 4.91; N, 17.06; O, 19.49
Synonym: MK 1903; MK1903; MK-1903.
IUPAC/Chemical Name: (4aR,5aR)-4,4a,5,5a-tetrahydro-1H-cyclopropa[4,5]cyclopenta[1,2-c]pyrazole-3-carboxylic acid
InChi Key: CUTZNERBKDMLAP-QWWZWVQMSA-N
InChi Code: InChI=1S/C8H8N2O2/c11-8(12)7-5-2-3-1-4(3)6(5)9-10-7/h3-4H,1-2H2,(H,9,10)(H,11,12)/t3-,4-/m1/s1
SMILES Code: O=C(C1=NNC2=C1C[C@]3([H])[C@@]2([H])C3)O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 25.0 | 152.29 | |
| DMSO | 30.0 | 182.75 | |
| DMSO:PBS (pH 7.2) (1:2) | 0.3 | 1.83 | |
| Ethanol | 20.0 | 121.83 |
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 | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Hughes-Large JM, Pang DK, Robson DL, Chan P, Toma J, Borradaile NM. Niacin receptor activation improves human microvascular endothelial cell angiogenic function during lipotoxicity. Atherosclerosis. 2014 Dec;237(2):696-704. doi: 10.1016/j.atherosclerosis.2014.10.090. PubMed PMID: 25463108.
2: Lauring B, Taggart AK, Tata JR, Dunbar R, Caro L, Cheng K, Chin J, Colletti SL, Cote J, Khalilieh S, Liu J, Luo WL, Maclean AA, Peterson LB, Polis AB, Sirah W, Wu TJ, Liu X, Jin L, Wu K, Boatman PD, Semple G, Behan DP, Connolly DT, Lai E, Wagner JA, Wright SD, Cuffie C, Mitchel YB, Rader DJ, Paolini JF, Waters MG, Plump A. Niacin lipid efficacy is independent of both the niacin receptor GPR109A and free fatty acid suppression. Sci Transl Med. 2012 Aug 22;4(148):148ra115. doi: 10.1126/scitranslmed.3003877. PubMed PMID: 22914621.
3: Boatman PD, Lauring B, Schrader TO, Kasem M, Johnson BR, Skinner P, Jung JK, Xu J, Cherrier MC, Webb PJ, Semple G, Sage CR, Knudsen J, Chen R, Luo WL, Caro L, Cote J, Lai E, Wagner J, Taggart AK, Carballo-Jane E, Hammond M, Colletti SL, Tata JR, Connolly DT, Waters MG, Richman JG. (1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (MK-1903): a potent GPR109a agonist that lowers free fatty acids in humans. J Med Chem. 2012 Apr 26;55(8):3644-66. doi: 10.1021/jm2010964. PubMed PMID: 22435740.
