MK-2894 |
| Katalog-Nr.GC16477 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1006036-87-8
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 1006036-87-8 | SDF | |
| Chemical Name | 4-[1-[[2,5-dimethyl-4-[[4-(trifluoromethyl)phenyl]methyl]thiophene-3-carbonyl]amino]cyclopropyl]benzoic acid | ||
| Canonical 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 | ||
| Formula | C25H22F3NO3S | M.Wt | 473.51 |
| Löslichkeit | DMSO : ≥ 50 mg/mL (105.59 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1119 mL | 10.5594 mL | 21.1189 mL |
| 5 mM | 0.4224 mL | 2.1119 mL | 4.2238 mL |
| 10 mM | 0.2112 mL | 1.0559 mL | 2.1119 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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