| Bioactivity | U-46619 (9,11-Methanoepoxy PGH2) is a stable analogue of thromboxane A2 (TXA2) and acts as a potent TXA2 agonist[1]. |
| Target | TXA2 |
| Invitro | U-46619 (1 nM-10 μM) causes platelets shape change and aggregation in a concentration-dependent manner, and with EC50s of 0.58 μM and 0.013 μM for aggregation and shape change, respectively[1].U-46619 (10 nM-10 μM) increases internal Ca2+ concentration ([Ca2+]i) and activates phosphoinositide (PI) hydrolysis in a concentration-dependent manner with a similar concentration-dependency[1].U-46619 (3 nM-10 μM) also activates GTPase concentration-dependently in the membranes derived from platelets[1].U-46619 improves the differentiation efficiency of human induced pluripotent stem cells into endothelial cells by activating both p38MAPK and ERK1/2 signaling pathways[2]. |
| In Vivo | U-46619 (5 μg/kg; i.v.) increases blood pressure in male spontaneously hypertensive rats (SHR)[3]. Animal Model: |
| Name | U-46619 |
| CAS | 56985-40-1 |
| Formula | C21H34O4 |
| Molar Mass | 350.49 |
| Appearance | Liquid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Solution, -20°C, 2 years |
| Reference | [1]. Ohkubo S, et al. Thromboxane A2-mediated shape change: independent of Gq-phospholipase C--Ca2+ pathway in rabbit platelets. Br J Pharmacol. 1996 Mar;117(6):1095-104. [2]. Su L, et al. The prostaglandin H2 analog U-46619 improves the differentiation efficiency of human induced pluripotent stem cells into endothelial cells by activating both p38MAPK and ERK1/2 signaling pathways. Stem Cell Res Ther. 2018 Nov 15;9(1):313. [3]. Schirner M, et al. U 46619 induces different blood pressure effects in male and female spontaneously hypertensive rats (SHR). Prostaglandins Leukot Essent Fatty Acids. 1993 Jun;48(6):469-73. |