MK-2894EP4 receptor inhibitor CAS# 1006036-87-8 |
- ONO-AE3-208
Catalog No.:BCC1822
CAS No.:402473-54-5
Quality Control & MSDS
3D structure
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| Cas No. | 1006036-87-8 | SDF | Download SDF |
| PubChem ID | 24952929 | Appearance | Powder |
| Formula | C25H22F3NO3S | M.Wt | 473.51 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 50 mg/mL (105.59 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 4-[1-[[2,5-dimethyl-4-[[4-(trifluoromethyl)phenyl]methyl]thiophene-3-carbonyl]amino]cyclopropyl]benzoic acid | ||
| SMILES | CC1=C(C(=C(S1)C)C(=O)NC2(CC2)C3=CC=C(C=C3)C(=O)O)CC4=CC=C(C=C4)C(F)(F)F | ||
| Standard InChIKey | QJZQFVRFJCGDKF-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C25H22F3NO3S/c1-14-20(13-16-3-7-19(8-4-16)25(26,27)28)21(15(2)33-14)22(30)29-24(11-12-24)18-9-5-17(6-10-18)23(31)32/h3-10H,11-13H2,1-2H3,(H,29,30)(H,31,32) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | MK-2894 is a highly potent and selective inhibitor of EP4 receptor with IC50 value of 2.5 nM. | |||||
| Targets | EP4 receptor | |||||
| IC50 | 2.5 nM (Ki=0.56±0.1 nM） | |||||
MK-2894 Dilution Calculator
MK-2894 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1119 mL | 10.5594 mL | 21.1189 mL | 42.2378 mL | 52.7972 mL |
| 5 mM | 0.4224 mL | 2.1119 mL | 4.2238 mL | 8.4476 mL | 10.5594 mL |
| 10 mM | 0.2112 mL | 1.0559 mL | 2.1119 mL | 4.2238 mL | 5.2797 mL |
| 50 mM | 0.0422 mL | 0.2112 mL | 0.4224 mL | 0.8448 mL | 1.0559 mL |
| 100 mM | 0.0211 mL | 0.1056 mL | 0.2112 mL | 0.4224 mL | 0.528 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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MK-2894 is a highly potent and selective inhibitor of EP4 receptor with IC50 value of 2.5 nM [1].
MK-2894 is a highly selective and potent second generation EP4 antagonist with a Ki of 0.56±0.1nM in the radio ligand binding assay using membranes prepared from human EP1-4 overexpressed HEK 293 cell lines. And the EP4 functional assay measures the inhibition of PGE2-induced cAMP accumulation with IC50 of 2.5±0.7nM. In the AIA model and GI tolerability model in male SD rats, MK-2894 shows a dose-dependent inhibition of pain response with ED50 of 0.36 mg/kg. It also has the potent activity in inhibiting chronic pawswelling with ED50 of 0.02 mg/kg/day. Overall, MK-2894 displays the desired potency, selectivity, pharmacokinetic, and GI tolerability profile for further development and represents a potential safer alternative for treating pain and inflammation than traditional NSAIDs and coxibs [1].
References:
[1] Marc Blouin, Yongxin Han, Jason Burch, Julie Farand, Christophe Mellon, Mireille Gaudreault, Mark Wrona, Jean-Francois Levesque, Danielle Denis, Marie-Claude Mathieu, Rino Stocco, Erika Vigneault, Alex Therien, Patsy Clark, Steve Rowland, Daigen Xu, Gary O’Neill, Yves Ducharme and Rick Friesen. The Discovery of 4-{1-[({2,5-Dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic Acid (MK-2894), A Potent and Selective Prostaglandin E2 Subtype 4 Receptor Antagonist. J. Med. Chem. 2010, 53: 2227–2238.
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The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclo propyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.[Pubmed:20163116]
J Med Chem. 2010 Mar 11;53(5):2227-38.
The discovery of highly potent and selective second generation EP(4) antagonist MK-2894 (34d) is discussed. This compound exhibits favorable pharmacokinetic profile in a number of preclinical species and potent anti-inflammatory activity in several animal models of pain/inflammation. It also shows favorable GI tolerability profile in rats when compared to traditional NSAID indomethacin.
