| 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].
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| Related Catalog |
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| Target |
EP4:0.38 nM (Ki)
EP4:0.6 nM (EC50)
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| 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.
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| 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.
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| 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. [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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