124750-99-8 Losartan potassium AKSci J10063
 
 
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  J10063    AKSci Reference Standard
Losartan potassium
, 99% (HPLC), powder
 
2-Butyl-4-chloro-1-{[2'-(1H-tetrazol-5-yl)(1,1''-biphenyl)-4-yl]methyl}-1H-imidazole-5-methanol monopotassium salt




IDENTITY
CAS Number:124750-99-8
MDL Number:MFCD02092704
MF:C22H22CIKN6OK
MW:461.01
SPECIFICATIONS & PROPERTIES
Purity:99% (HPLC), powder
Spectra:NMR, LCMS, HPLC
Physical Form:White to off-white crystalline powder
Melting Point:268-271°C
Long-Term Storage:Store at room temperature

BIOLOGICAL INFO
Solubility:Soluble in ethanol, DMSO, DMF at 20mg/ml
Application(s):Angiotensin II receptor antagonist drug.

REVIEW

 Losartan competitively inhibits the binding of angiotensin II to AT1 in many tissues including vascular smooth muscle and the adrenal glands. Losartan is metabolized to its active metabolite, E-3174, which is 10 to 40 times more potent than losartan and acts as a non-competitive AT1 antagonist. Inhibition of angiotensin II binding to AT1 inhibits its AT1-mediated vasoconstrictive and aldosterone-secreting effects and results in decreased vascular resistance and blood pressure. Losartan is 1,000 times more selective for AT1 than AT2. Inhibition of aldosterone secretion may increase sodium and water excretion while decreasing potassium excretion. Losartan is effective for reducing blood pressure and may be used to treat essential hypertension, left ventricular hypertrophy and diabetic nephropathy.

REFERENCES
[1]Dahlof B, Devereux RB, Kjeldsen SE, Julius S, Beevers G, de Faire U, Fyhrquist F, Ibsen H, Kristiansson K, Lederballe-Pedersen O, Lindholm LH, Nieminen MS, Omvik P, Oparil S, Wedel H: Cardiovascular morbidity and mortality in the Losartan Intervention For Endpoint reduction in hypertension study (LIFE): a randomised trial against atenolol. Lancet. 2002 Mar 23;359(9311):995-1003.
[2] Guo ZX, Qiu MC: [Losartan downregulates the expression of transforming growth factor beta type I and type II receptors in kidney of diabetic rat] Zhonghua Nei Ke Za Zhi. 2003 Jun;42(6):403-8.
[3] Habashi JP, Judge DP, Holm TM, Cohn RD, Loeys BL, Cooper TK, Myers L, Klein EC, Liu G, Calvi C, Podowski M, Neptune ER, Halushka MK, Bedja D, Gabrielson K, Rifkin DB, Carta L, Ramirez F, Huso DL, Dietz HC: Losartan, an AT1 antagonist, prevents aortic aneurysm in a mouse model of Marfan syndrome. Science. 2006 Apr 7;312(5770):117-21.
[4] Sica, D.A., Gehr, T.W.B., & Ghosh, S. (2005). Clinical pharmacokinetics of losartan. Clinical Pharmacokinetics, 44(8), 797-814. PMID: 16029066

GHS

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501


RELATED PRODUCTS
I497Losartan
I934Losartan potassium
I971Trityl losartan

Current as of June 25, 2019

AKSci Reference Standards are high-purity, low-impurity compounds suitable for use as standards.


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CATEGORIES

 APIs and Bioactives > Angiotensin Receptor Blockers


PubChem