Losartan Carboxaldehyde


Catalog No. Size PriceQuantity
M22835-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

Losartan is an inhibitor of endothelial cyclooxygenase (COX)-2. COX-2 produces prostaglandins that inhibit apoptosis and stimulate angiogenesis and invasiveness, and thus selective COX-2 inhibitors can reduce prostaglandin synthesis and restore apoptosis. In vitro: Losartan is an intermediate aldehyde metabolite of losartan, the angiotensin II type 1 receptor antagonist. Losartan could not block angiotensin receptors, but inhibit the expression of endothelial cyclooxygenase (COX)-2, therefore exerting anti-inflammatory actions. Moreover, losartan at 1 μM was able to block the upregulation of ICAM-1 mRNA and COX-dependent generation of thromboxane A2 and prostaglandin F2α . In vivo: In animal stufdy, losartan was infused for 10 days to rats on a normal sodium intake (NNa) and rats on a high sodium intake (HNa) to suppress endogenous Ang II. Although basal plasma renin activity was markedly suppressed in HNa rats compared with NNa rats, control arterial pressure was not different between NNa and HNa rats. Losartan could decrease arterial pressure from control levels in NNa rats on the first day of infusion but had no effect on arterial pressure in HNa rats. In addition, by day 10 of losartan infusion, arterial pressure had decreased further from control levels in NNa rats but remained unchanged compared with control in HNa rats . Clinical trial: In patients with mild to moderate hypertension, losartan as monotherapy could lower blood pressure to a similar degree to enalapril, atenolol and felodipine. Losartan combined with hydrochlorothiazide could reduce blood pressure than either drug separately given. About 1/3 patients with severe hypertension have response to the combination product .

Product information

CAS Number: 114798-36-6

Molecular Weight: 420.89

Formula: C22H21ClN6O

Chemical Name: 2-butyl-4-chloro-1-{[2'-(1H-1,2,3,4-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl]methyl}-1H-imidazole-5-carbaldehyde

Smiles: CCCCC1=NC(Cl)=C(C=O)N1CC1C=CC(=CC=1)C1=CC=CC=C1C1NN=NN=1

InChiKey: FQZSMTSTFMNWQF-UHFFFAOYSA-N

InChi: InChI=1S/C22H21ClN6O/c1-2-3-8-20-24-21(23)19(14-30)29(20)13-15-9-11-16(12-10-15)17-6-4-5-7-18(17)22-25-27-28-26-22/h4-7,9-12,14H,2-3,8,13H2,1H3,(H,25,26,27,28)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.

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