U-46619
Synonym(s):9,11-Dideoxy-9α,11α-methanoepoxyprostaglandin F 2α;U46619;U-46619;U-46619 - CAS 56985-40-1 - Calbiochem
- CAS NO.:56985-40-1
- Empirical Formula: C21H34O4
- Molecular Weight: 350.49
- MDL number: MFCD00135238
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-19 23:02:33
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) |
Flame Flammables GHS02 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
New Products
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