U-46619 Property

Boiling point:

519.7±30.0 °C(Predicted)

Density 

1.092±0.06 g/cm3(Predicted)

Flash point:

-10 °C

storage temp. 

-20°C

solubility 

≥100 mg/mL in DMSO, ≥100 mg/mL in Ethanol, ≥100 mg/mL in DMF, ≥2 mg/mL in PBS pH 7.2

pka

4.76±0.10(Predicted)

form 

solution

color 

Colorless to light yellow

BRN 

4267334

Safety

Hazard Codes 

F,Xi

Risk Statements 

11-36-66-67

Safety Statements 

16-26

RIDADR 

UN 1231 3/PG 2

WGK Germany 

2

RTECS 

MJ9681090

F 

8-10-23

Toxicity

LD50 intravenous in mouse: 66ug/kg

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H225Highly Flammable liquid and vapour

H319Causes serious eye irritation

H336May cause drowsiness or dizziness

Precautionary statements

P210Keep away from heat/sparks/open flames/hot surfaces. — No smoking.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

U-46619 Chemical Properties,Usage,Production

Uses

U 46619 is a PGH2 analog that may be used as a thromboxane A2 (TP) receptor agonist affecting mitogenic growth of vascular smooth muscle in humans.

Biological Activity

PGH 2 (TXA 2 ) analog that is a potent and stable thromboxane A 2 (TP) receptor agonist (EC 50 = 0.035 μ M). Potently stimulates TP receptor-mediated, but not other prostaglandin receptor-mediated responses in various in vitro preparations. Activates ERK-1 and ERK-2 in HEK-293 cells expressing TP α and TP β receptors.

Biochem/physiol Actions

Thromboxane receptor agonist.

in vitro

u46619 showed a biphasic effect on human platelets. shape change and mlcp occurred at low concentrations of this compound (ec50 = 0.035 um and 0.057 um), whereas serotonin release, platelet at higher concentrations (ec50 = 0.536 um and 1.31 um). the effect on platelet shape change and mlcp is receptor mediated [3].

in vivo

u46619, through activation of eta and etb receptors, elicits renal cortical vasoconstriction and medullary vasodilation in the rat [2]. in conscious shr (spontaneously hypertensive rats), 1-100 nmol/kg u-46619 (i.c.v.) induced a dose-related increase in blood pressure but had no significant effect on heart rate [1].

storage

Store at -20°C

References

[1] sirén al, svartstrm-fraser m, paakkari i. central cardiovascular effects of the endoperoxide analogue u-46619 in rats. prostaglandins leukot med. 1985 mar; 17 (3): 381-6.
[2] hantz h, adesuyi a, adebayo o. differential effects of u46619 on renal regional hemodynamics in the rat: involvement of endothelin. j pharmacol exp ther. 2001 oct; 299 (1): 372-6.
[3] morinelli ta1, niewiarowski s, daniel jl, smith jb. receptor-mediated effects of a pgh2 analogue (u 46619) on human platelets. am j physiol. 1987 nov; 253 (5 pt 2): h1035-43.