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BOC Sciences |
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| | CAY10580 Basic information |
| Product Name: | CAY10580 | | Synonyms: | 2-(3-HYDROXYOCTYL)-5-OXO-1-PYRROLIDINEHEPTANOIC ACID;CAY10580;CAY10580 Exclusive;CBWGHEDGUILASE-UHFFFAOYSA-N;1-Pyrrolidineheptanoic acid, 2-(3-hydroxyoctyl)-5-oxo- | | CAS: | 64054-40-6 | | MF: | C19H35NO4 | | MW: | 341.49 | | EINECS: | | | Product Categories: | | | Mol File: | 64054-40-6.mol |  |
| | CAY10580 Chemical Properties |
| Boiling point | 534.4±25.0 °C(Predicted) | | density | 1.049±0.06 g/cm3(Predicted) | | solubility | DMF: 10 mg/ml; DMSO: 10 mg/ml; Ethanol: 20 mg/ml; PBS (pH 7.2): 2.5 mg/ml | | pka | 4.77±0.10(Predicted) | | form | Liquid | | color | Colorless to light yellow |
| | CAY10580 Usage And Synthesis |
| Uses | 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.[Cayman Chemical] | | Uses | 2-(3-hydroxyoctyl)-5-oxo-1-pyrrolidineheptanoic acid is an analog of PGE2. | | Definition | ChEBI: 2-(3-hydroxyoctyl)-5-oxo-1-pyrrolidineheptanoic acid is a pyrrolidin-2-one substituted by 6-carboxyhexyl and 3-hydroxyoctyl groups at positions 1 and 2, respectively. It is a potent prostaglandin EP4 receptor agonist (Ki=35 nM). It has a role as a prostaglandin receptor agonist. It is a member of pyrrolidin-2-ones, a hydroxy monocarboxylic acid and a secondary alcohol. | | 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[3]. | Animal Model: | Six-week old male EP4+/+ mice (Treating high fat diet-challenged mice)[3] | | Dosage: | 200 μg/kg body weight | | Administration: | Intraperitoneal injection; daily for remaining three weeks | | Result: | High fat diet fed mice exhibited lower total cholesterol levels compared to the vehicle group by 28.5%. Total cholesterol levels decreased from 137.4 to 98.2 mg/dl, restoring plasma cholesterol back to near-normal values.
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| | IC 50 | EP4: 35 nM (Ki); EP2: 3000 nM (Ki); EP3: 2000 nM (Ki); EP1: >3000 nM (Ki) |
| | CAY10580 Preparation Products And Raw materials |
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