U-46619  (Synonyms: 9,11-Methanoepoxy PGH2)

U-46619 (9,11-Methanoepoxy PGH2) is a stable analogue of Thromboxane A2 (HY-113350) (TXA2) and acts as a potent TXA2 (TP) agonist. U-46619 also is a RhoA agonist. U-46619 stimulates the activation of RhoA through TXA2 receptor activation^[1][4][5].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

U-46619 (5 μg/kg; i.v.) increases blood pressure in male spontaneously hypertensive rats (SHR)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

350.49

C₂₁H₃₄O₄

56985-40-1

Liquid

Colorless to light yellow

O=C(O)CCC/C=C\C[C@H]1[C@@]2([H])CO[C@@](C2)([H])[C@@H]1/C=C/[C@@H](O)CCCCC

Room temperature in continental US; may vary elsewhere.

Solution, -20°C, 2 years

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [4]. Chen S, et al. Roles of the RhoA-ROCK Signaling Pathway in the Endothelial H2S Production and Vasodilation in Rat Cerebral Arteries. ACS Omega. 2022 May 20;7(22):18498-18508.  [Content Brief]

  [5]. Nie D, et al. Thromboxane A2 receptors in prostate carcinoma: expression and its role in regulating cell motility via small GTPase Rho. Cancer Res. 2008 Jan 1;68(1):115-21.  [Content Brief]