Losartan Carboxaldehyde (Synonyms: DuP-167|EXP3179) |
| Catalog No.GC14013 |
Losartan Carboxaldehyde is an important intermediate aldehyde metabolite of Losartan.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 114798-36-6
Sample solution is provided at 25 µL, 10mM.
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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 [1].
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 [2].
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 [3].
References:
[1] C. Kr mer, J. Sunkomat, J. Witte, et al. Angiotensin II receptor-independent antiinflammatory and antiaggregatory properties of losartan: Role of the active metabolite EXP3179. Circulation Research 90(7), 770-776 (2002).
[2] Collister JP, Hornfeldt BJ, Osborn JW. Hypotensive response to losartan in normal rats. Role of Ang II and the area postrema. Hypertension. 1996 Mar;27(3 Pt 2):598-606.
[3] Goa KL, Wagstaff AJ. Losartan potassium: a review of its pharmacology, clinical efficacy and tolerability in the management of hypertension. Drugs. 1996 May;51(5):820-45.
| Cas No. | 114798-36-6 | SDF | |
| Synonyms | DuP-167|EXP3179 | ||
| Chemical Name | 2-butyl-4-chloro-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxaldehyde | ||
| Canonical SMILES | [H]N1N=NN=C1C2=CC=CC=C2C3=CC=C(CN4C(C([H])=O)=C(Cl)N=C4CCCC)C=C3 | ||
| Formula | C22H21ClN6O | M.Wt | 420.9 |
| Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3759 mL | 11.8793 mL | 23.7586 mL |
| 5 mM | 0.4752 mL | 2.3759 mL | 4.7517 mL |
| 10 mM | 0.2376 mL | 1.1879 mL | 2.3759 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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