research use only
Cat.No.S1604
| Related Targets | CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas |
|---|---|
| Other Angiotensin Receptor Inhibitors | PD123319 ML221 A-779 Fimasartan Olodanrigan (EMA401) Buloxibutid AVE 0991 |
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In vitro |
DMSO
: 89 mg/mL
(159.32 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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| Molecular Weight | 558.59 | Formula | C29H30N6O6 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 144689-63-4 | Download SDF | Storage of Stock Solutions |
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| Synonyms | CS-866,RNH-6270 | Smiles | CCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)C(=O)OCC5=C(OC(=O)O5)C)C(C)(C)O | ||
| Targets/IC50/Ki |
AT1 receptor
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|---|---|
| In vitro |
Olmesartan Medoxomil significantly reduces liver hydroxyproline content, the mRNA expression of collagen alpha1(I) and alpha-smooth muscle actin (alpha-SMA), and plasma levels of transforming growth factor-beta1 (TGF-beta1). This compound is a pro-drug containing an ester moiety that, after oral administration, is rapidly cleaved to release the active form Olmesartan (RNH-6270). This chemical is a highly potent, competitive and selective All AT1 receptor antagonist with almost no antagonistic activity on AT2 and AT4 receptors. |
| In vivo |
Olmesartan Medoxomil produces a rapid and long-lasting inhibition of All-induced pressor responses in conscious rats. Oralolmesartan medoxomil also inhibits All-pressor response but onset of the action is slower compared with intravenous administration. This compound exhibits dose-dependent antihypertensive effects in several rat and dog models, with the most marked effects seen in high plasma renin models, when compared with normal or low renin types. It exhibits, beside antihypertensive effects, beneficial effects in animal models of various types of nephrosis and heart failure, and anti-atherogenic effects in hyperlipidaemic animals. This chemical dose-dependently ameliorates the colonic histopathological and biochemical injuries in rats, an effect that is comparable or even better than that of the standard Sulfasalazine. It significantly reduces the induction of hypoxic cor pulmonale not only on echocardiographical observations but also in brain natriuretic peptide (BNP) in chronic hypoxic rats, TGF-beta and endothelin gene expressions in molecular studies. |
References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00185055 | Completed | Healthy |
Daiichi Sankyo |
November 2004 | Phase 4 |
| NCT00362960 | Completed | Type 2 Diabetes Mellitus|Diabetic Nephropathy|Proteinuria|Renal Disease |
Sankyo Pharma Gmbh|Daiichi Sankyo |
May 2003 | Phase 3 |
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