634193-54-7
634193-54-7 structure
- Name: L-902688
- Chemical Name: 5-(4,4-difluoro-3-hydroxy-4-phenylbut-1-enyl)-1-[6-(2H-tetrazol-5-yl)hexyl]pyrrolidin-2-one
- CAS Number: 634193-54-7
- Molecular Formula: C21H27F2N5O2
- Molecular Weight: 419.468
- Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
- Create Date: 2017-01-09 22:00:11
- Modify Date: 2024-01-05 18:13:00
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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].
| Name | 5-(4,4-difluoro-3-hydroxy-4-phenylbut-1-enyl)-1-[6-(2H-tetrazol-5-yl)hexyl]pyrrolidin-2-one |
|---|---|
| Synonyms |
(5R)-5-[(1E,3R)-4,4-Difluoro-3-hydroxy-4-phenyl-1-buten-1-yl]-1-[6-(2H-tetrazol-5-yl)hexyl]-2-pyrrolidinone
2-Pyrrolidinone, 5-[(1E,3R)-4,4-difluoro-3-hydroxy-4-phenyl-1-buten-1-yl]-1-[6-(2H-tetrazol-5-yl)hexyl]-, (5R)- l-902,688 2-Pyrrolidinone, 5-[(1E,3R)-4,4-difluoro-3-hydroxy-4-phenyl-1-buten-1-yl]-1-[6-(2H-tetrazol-5-yl)hexyl]- 5-[(1E,3R)-4,4-Difluoro-3-hydroxy-4-phenyl-1-buten-1-yl]-1-[6-(2H-tetrazol-5-yl)hexyl]-2-pyrrolidinone |
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
EP4:0.38 nM (Ki) EP4:0.6 nM (EC50) |
| In Vitro | L-902688 (1 µM; 24 hours; HUVE cells) treatment attenuates TGF-β-induced Twist and α-smooth muscle actin (α-SMA) expression[1]. Western Blot Analysis[1] Cell Line: Human umbilical vein endothelial cells (HUVECs) Concentration: 1 µM Incubation Time: 24 hours Result: Attenuated TGF-β-induced Twist and α-smooth muscle actin (α-SMA) expression. |
| 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. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 645.8±65.0 °C at 760 mmHg |
| Molecular Formula | C21H27F2N5O2 |
| Molecular Weight | 419.468 |
| Flash Point | 344.4±34.3 °C |
| Exact Mass | 419.213287 |
| PSA | 95.00000 |
| LogP | 2.49 |
| Vapour Pressure | 0.0±2.0 mmHg at 25°C |
| Index of Refraction | 1.597 |