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HomeProduct name listU-46619

U-46619

Synonym(s):9,11-Dideoxy-9α,11α-methanoepoxyprostaglandin F ;U46619;U-46619;U-46619 - CAS 56985-40-1 - Calbiochem

U-46619 Structural

What is U-46619?

The Uses of U-46619

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.

What are the applications of Application

U-46619 is a stable thromboxane A2 mimetic and analog of the H2 endoperoxide prostaglandin, used as a vasoconstrictor and thromboxane receptor agonist.

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.

Properties of U-46619

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
form  solution
pka 4.76±0.10(Predicted)
color  Colorless to light yellow
BRN  4267334

Safety information for U-46619

Signal word Danger
Pictogram(s)
ghs
Flame
Flammables
GHS02
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H225:Flammable liquids
H319:Serious eye damage/eye irritation
H336:Specific target organ toxicity,single exposure; Narcotic effects
Precautionary Statement Codes P210:Keep away from heat/sparks/open flames/hot surfaces. — No smoking.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for U-46619

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