| Identification | Back Directory | [Name]
L-902,688 | [CAS]
634193-54-7 | [Synonyms]
L-902,688
L902688,L 902688
L-902,688 Exclusive
(5R)-5-[(E,3R)-4,4-difluoro-3-hydroxy-4-phenylbut-1-enyl]-1-[6-(2H-tetrazol-5-yl)hexyl]pyrrolidin-2-one
2-Pyrrolidinone, 5-[(1E,3R)-4,4-difluoro-3-hydroxy-4-phenyl-1-buten-1-yl]-1-[6-(2H-tetrazol-5-yl)hexyl]-, (5R)- | [Molecular Formula]
C21H27F2N5O2 | [MDL Number]
MFCD32661895 | [MOL File]
634193-54-7.mol | [Molecular Weight]
419.468 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF:30.0(Max Conc. mg/mL);71.52(Max Conc. mM)
DMSO:30.0(Max Conc. mg/mL);71.52(Max Conc. mM)
Ethanol:30.0(Max Conc. mg/mL);71.52(Max Conc. mM)
Ethanol:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.19(Max Conc. mM) | [form ]
Liquid | [color ]
Colorless to light yellow |
| Hazard Information | Back Directory | [Description]
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. L-902,688 is a highly potent agonist of the human PGE2 receptor, EP4. It demonstrates a Ki value of 0.38 nM and an EC50 value of 0.6 nM and is >4,000-fold selective for EP4 over other EP and prostanoid receptors. L-902,688 induces thermal hyperalgesia when injected into guinea pig forepaw and increases vasodilation of human pulmonary vein. | [Uses]
L-902688 is a potent, selective and orally active EP4 receptor agonist with a Ki of 0.38 nM and an EC50 of 0.6 nM. L-902688 shows >4,000-fold selective for EP4 over other EP and prostanoid receptors[1][2]. | [in vivo]
L-902688 (0.25-1 μg/kg/day; intraperitoneal injection; daily; for 3 weeks; adult male Sprague-Dawley rats) treatment reduces right ventricle fibrosis in the monocrotaline (MCT)-induced PAH rat model[1]. | Animal Model: | Adult male Sprague-Dawley rats injected with crotaline to induce pulmonary arterial hypertension (PAH) and right ventricular (RV) hypertrophy[1] | | Dosage: | 0.25 μg/kg/day, 0.4 μg/kg/day or 1 μg/kg/day | | Administration: | Intraperitoneal injection; daily; for 3 weeks | | Result: | Reduced right ventricle fibrosis in the monocrotaline (MCT)-induced PAH rat model. |
| [IC 50]
EP4: 0.38 nM (Ki); EP4: 0.6 nM (EC50) | [References]
[1] Lai YJ, et al. EP4 Agonist L-902,688 Suppresses EndMT and Attenuates Right Ventricular Cardiac Fibrosis in Experimental Pulmonary Arterial Hypertension. Int J Mol Sci. 2018 Mar 3;19(3). pii: E727. DOI:10.3390/ijms19030727
[2] [2]Young, R.N., Billot, X., Han, Y., et al. Discovery and synthesis of a potent, selective and orally bioavailable EP4 receptor agonist. Heterocycles. 2004, 64, 437-445. |
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