Description
CAY10580 is a potent and selective prostaglandin EP4 receptor agonist (Ki=35 nM). 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. CAY10580 is an 8-aza-9-oxo-15-hydroxy saturated analog of PGE2. It selectively binds the EP4 receptor (Ki = 35 nM) relative to the EP1, EP2, and EP3 receptors (Ki = 3, 000, 2, 000, and >3, 000 nM, respectively). CAY10580 stimulates cAMP formation in excised mouse ovaries.
Product information
CAS Number: 64054-40-6
Molecular Weight: 341.49
Formula: C19H35NO4
Chemical Name: 2-(3-hydroxyoctyl)-5-oxo-1-pyrrolidineheptanoic acid
Smiles: CCCCCC(O)CCC1CCC(=O)N1CCCCCCC(O)=O
InChiKey: CBWGHEDGUILASE-UHFFFAOYSA-N
InChi: InChI=1S/C19H35NO4/c1-2-3-6-9-17(21)13-11-16-12-14-18(22)20(16)15-8-5-4-7-10-19(23)24/h16-17,21H,2-15H2,1H3,(H,23,24)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: To be determined
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
CAY10580 (10-10000 nM; 40 min) significantly increases apical membrane abundance of AQP2 in MDCK cells at 100 to 10000 nM.
In Vivo:
CAY10580 (200 μg/kg body weight; i.p; daily for three weeks) effectively prevents diet-induced hypercholesterolemia, enhances endogenous bile acid synthesis and their fecal excretion.
References:
- Ying F, et al. EP4 emerges as a novel regulator of bile acid synthesis and its activation protects against hypercholesterolemia. Biochim Biophys Acta Mol Cell Biol Lipids. 2018;1863(9):1029-1040.
- Ying F, et al. EP4 emerges as a novel regulator of bile acid synthesis and its activation protects against hypercholesterolemia. Biochim Biophys Acta Mol Cell Biol Lipids. 2018;1863(9):1029-1040.
Products are for research use only. Not for human use.
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