TCS 2510 (Synonyms: CAY10598) |
Catalog No.GC11122 |
EP4 agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 346673-06-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, cancer, and atherosclerosis.[1],[2],[3] CAY10598 is a very potent agonist of EP4, binding with a Ki value of 1.2 nM.[4] Moreover, it does not bind EP1, EP2, EP3, or other prostanoid receptors, including DP, FP, IP, and TP.[4] First generation EP4 receptor-selective agonists have been shown to reduce inflammation, improve bone healing, provide cardio- and neuroprotection, and reduce renal dysfunction, suggesting some clinical applications for EP4 agonists.[5],[6],[7],[8],[9]
Reference
[1]. Li, M., Thompson, D.D., and Paralkar, V.M. Prostaglandin E2 receptors in bone formation. Int. Orthop. 31(6), 767-772 (2007).
[2]. Hawcroft, G., Ko, C.W.S., and Hull, M.A. Prostaglandin E2-EP4 receptor signalling promotes tumorigenic behaviour of HT-29 human colorectal cancer cells. Oncogene 26, 3006-3019 (2007).
[3]. Babaev, V.R., Chew, J.D., Ding, L., et al. Macrophage EP4 deficiency increases apoptosis and suppresses early atherosclerosis. Cell Metabolism 8, 492-501 (2008).
[4]. Billot, X., Chateauneuf, A., Chauret, N., et al. Discovery of a potent and selective agonist of the prostaglandin EP4 receptor. Bioorganic & Medicinal Chemistry Letters 13, 1129-1132 (2003).
[5]. Yamane, H., Sugimoto, Y., Tanaka, S., et al. Prostaglandin E2 receptors, EP2 and EP4, differentially modulate TNF-α and IL-6 production induced by lipopolysaccharide in mouse peritoneal neutrophils. Biochemical and Biophysical Research Communications 278, 224-228 (2000).
[6]. Marui, A., Hirose, K., Maruyama, T., et al. Prostaglandin E2 EP4 receptor-selective agonist facilitates sternal healing after harvesting bilateral internal thoracic arteries in diabetic rats. J.Thorac.Cardiovasc.Surg. 131(3), 587-593 (2006).
[7]. Xiao, C.Y., Yuhki, K.i., Hara, A., et al. Prostaglandin E2 protects the heart from ischemia-reperfusion injury via its receptor subtype EP4. Circulation 109, 2462-2468 (2004).
[8]. Ahmad, A.S., Ahmad, M., de Brum-Fernandes, A.J., et al. Prostaglandin EP4 receptor agonist protects against acute neurotoxicity. Brain Research 1066, 71-77 (2005).[
[9]. Li, J.H., Chou, C.L., Li, B., et al. A selective EP4 PGE2 receptor agonist alleviates disease in a new mouse model of X-linked nephrogenic diabetes insipidus. Journal of Clinical Investigation 119(10), 3115-3126 (2009).
Cas No. | 346673-06-1 | SDF | |
Synonyms | CAY10598 | ||
Chemical Name | (R)-1-(6-(2H-tetrazol-5-yl)hexyl)-5-((R,Z)-3-hydroxy-4-phenylbut-1-en-1-yl)pyrrolidin-2-one | ||
Canonical SMILES | O=C1N(CCCCCCC2=NNN=N2)[C@@H](/C=C\[C@@H](CC3=CC=CC=C3)O)CC1 | ||
Formula | C21H29N5O2 | M.Wt | 383.49 |
Solubility | 12.5mg/mL in DMSO, 12.5mg/mL in DMF, 15mg/mL in Ethanol | 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 | 2.6076 mL | 13.0381 mL | 26.0763 mL |
5 mM | 0.5215 mL | 2.6076 mL | 5.2153 mL |
10 mM | 0.2608 mL | 1.3038 mL | 2.6076 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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.
Average Rating: 5
(Based on Reviews and 18 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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