Losartan carboxylic acid

Bezeichnung:Losartan carboxylic acid

CAS-Nr124750-92-1

Englisch Name:Losartan carboxylic acid

CBNumberCB4399601

SummenformelC22H21ClN6O2

Molgewicht436.89

MOL-Datei124750-92-1.mol

Losartan carboxylic acid physikalisch-chemischer Eigenschaften

Schmelzpunkt	130-132°C
Siedepunkt	707.8±70.0 °C(Predicted)
Dichte	1.41±0.1 g/cm3(Predicted)
storage temp.	Inert atmosphere,2-8°C
Löslichkeit	Dimethylformamide, Dimethyl Sulfoxide, Methanol
Aggregatzustand	Solid
pka	0.79±0.50(Predicted)
Farbe	Light-Yellow
InChIKey	ZEUXAIYYDDCIRX-UHFFFAOYSA-N
SMILES	C1(CCCC)N(CC2=CC=C(C3=CC=CC=C3C3=NNN=N3)C=C2)C(C(O)=O)=C(Cl)N=1

Sicherheit

S-Sätze:	24/25
HS Code	29339900

Gefahreninformationscode (GHS)

Losartan carboxylic acid Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Losartan carboxylic acid is a physiologically active metabolite of losartan , produced by cytochrome P450 isoforms in the liver. Like the parent compound, losartan carboxylic acid is a potent AT₁ antagonist (K_is = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation. When administered intravenously, losartan carboxylic acid is more potent and has a longer duration of action than losartan. However, the metabolite has very low oral bioavailability. Losartan, but not its metabolite, inhibits platelet aggregation in vitro.
Chemische Eigenschaften
Light-Yellow Solid
Verwenden
Losartan carboxylic acid is used as a metabolite of Losartan.
Definition
ChEBI: A biphenylyltetrazole that is losartan with the hydroxymethyl group at position 5 on the imidazole ring replaced with a carboxylic acid.
in vitro
e-3174 potently blocked the specific binding of [125i]-aii to vsmc isolated from rat aorta. e-3174 was able to dampen the platelet-derived growth factor-induced increase in cell dna synthesis and protein, which led to the blockade of the aii-induced increase in cell protein [1].
in vivo
rats were administrated e-3174 intravenously at a dose of l.0 mg/kg. after 6 hours, e-3174 markedly attenuated the cardiovascular effects of aii in rats. e-3174 induced a progressive fall in mean arterial pressure and a marked increase in renal flow only [2].
Lager
Store at -20°C
Einzelnachweise
[1]. li, x. & widdop, r. angiotensin type i receptor antagonists cy-11974 and exp 3174 cause selective renal vasodilatation in conscious spontaneously hypertensive rats. clinical science, 1996; 91(2): 147-154.
[2]. sachinidis, a., ko, y., weisser, p., zu bricbkwedde, m., dsing, r., & christian, r. et al. exp3174, a metabolite of losartan (mk954, dup753) is more potent than losartan in blocking the angiotensin ll-induced responses in vascular smooth muscle cells. journal of hypertension. 1993; 11(2): 155-162.

Losartan carboxylic acid Upstream-Materialien And Downstream Produkte

Losartan carboxylic acid Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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