MedKoo Cat#: 532185 | Name: MK-1903
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

MK-1903
MK-1903
CAS#1268882-43-4

Theoretical Analysis

MedKoo Cat#: 532185

Name: MK-1903

CAS#: 1268882-43-4

Chemical Formula: C8H8N2O2

Exact Mass: 164.0586

Molecular Weight: 164.16

Elemental Analysis: C, 58.53; H, 4.91; N, 17.06; O, 19.49

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 Weeks
10mg USD 650.00 2 Weeks
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Related CAS #
No Data
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
Solvent mg/mL mM comments
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
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
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
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.