Azilsartan medoxomil monopotassium - CAS 863031-24-7
Catalog number: 863031-24-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C30H23KN4O8
Molecular Weight:
606.63
COA:
Inquire
Targets:
Angiotensin Receptor
Description:
Azilsartan medoxomil monopotassium is an azilsartan prodrug and and an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM. It is used in the treatment of adults with essential hypertension. It inhibited cell proliferation at concentrations as low as 1 μmol/l in aortic endothelial cells in vitro. It has antiproliferative effects of azilsartan were also observed in cells lacking AT1 receptors. It was developed by Takeda Corporation. It has been listed.
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Purity:
>98%
Appearance:
White or white crystalline powder
Synonyms:
1-[[2'-(2,5-Dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-carboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester potassium salt;Azilsartan MedoxoMil PotassiuM salt;Azilsartan kamedoxomil;TAK 491 monopotassium;Potassium,(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-3-[[4-[2-(5-oxo-1-oxa-2-aza-4-azanidacyclopent-2-en-3-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylate
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Azilsartan medoxomil monopotassium is used in the treatment of adults with essential hypertension.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Kilogram to ton
InChIKey:
IHWFKDWIUSZLCJ-UHFFFAOYSA-M
InChI:
InChI=1S/C30H24N4O8.K/c1-3-38-28-31-23-10-6-9-22(27(35)39-16-24-17(2)40-30(37)41-24)25(23)34(28)15-18-11-13-19(14-12-18)20-7-4-5-8-21(20)26-32-29(36)42-33-26;/h4-14H,3,15-16H2,1-2H3,(H,32,33,36);/q;+1/p-1
Canonical SMILES:
CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NC(=O)O[N-]5)C(=O)OCC6=C(OC(=O)O6)C.[K+]
Current Developer:
Azilsartan medoxomil monopotassium was developed by Takeda Corporation. It has been listed.
1.The renin-angiotensin receptor blocker azilsartan medoxomil compared with the angiotensin-converting enzyme inhibitor ramipril in clinical trials versus routine practice: insights from the prospective EARLY registry.
Bramlage P1, Schmieder RE2, Gitt AK3,4, Baumgart P5, Mahfoud F6, Buhck H7, Ouarrak T8, Ehmen M9, Potthoff SA10; EARLY Registry Group. Trials. 2015 Dec 19;16:581. doi: 10.1186/s13063-015-1100-8.
BACKGROUND: Patient characteristics and blood pressure-related outcomes in randomized clinical trials (RCTs) differ from clinical practice because of stringent selection criteria. The present study aimed to explore the relationship between clinical trials and clinical practice. We analyzed data from patients enrolled in the "Treatment with Azilsartan Compared to ACE-Inhibitors in Anti-Hypertensive Therapy" (EARLY) registry comparing blood pressure (BP) effects of the angiotensin receptor blocker (ARB) azilsartan medoxomil (AZL-M) with the angiotensin-converting enzyme (ACE) inhibitor ramipril between patients who met the eligibility criteria of a previous RCT and those who did not.
2.Population Pharmacokinetics and Exposure-Response of a Fixed-Dose Combination of Azilsartan Medoxomil and Chlorthalidone in Patients with Stage 2 Hypertension.
Tsai MC1, Wu J1, Kupfer S1, Vakilynejad M1. J Clin Pharmacol. 2015 Dec 3. doi: 10.1002/jcph.684. [Epub ahead of print]
Population pharmacokinetic and exposure-response models for azilsartan medoxomil (AZL-M) and chlorthalidone (CLD) were developed using data from an 8-week, placebo-controlled, Phase 3, factorial study of 20, 40 and 80 mg AZL-M qd and 12.5 and 25 mg CLD qd in fixed-dose combination (FDC). A two-compartment model with first-order absorption and elimination was developed to describe pharmacokinetics. An Emax model for exposure-response analysis evaluated AZL-M/CLD effects on ambulatory systolic blood pressure (SBP). Estimated oral clearance and apparent volume of distribution (central compartment) were 1.47 L/h and 3.98 L for AZL, and 4.13 L/h and 62.1 L for CLD. Age as a covariate had the largest effect on AZL and CLD exposure (±20% change). Predicted maximal SBP responses (Emax ) were -15.6 and -23.9 mmHg for AZL and CLD. Subgroup analysis identified statistically significant Emax differences for black versus non-black subjects, whereby the reduced AZL response in black subjects was offset by greater response to CLD.
3.Azilsartan medoxomil in the management of hypertension: an evidence-based review of its place in therapy.
Angeloni E1. Core Evid. 2016 Apr 5;11:1-10. doi: 10.2147/CE.S81776. eCollection 2016.
BACKGROUND: Azilsartan (AZI) is a relatively new angiotensin receptor blocker available for the treatment of any stage of hypertension, which was eventually given in combination with chlorthalidone (CLT).
4.Safety and tolerability of azilsartan medoxomil in subjects with essential hypertension: a one-year, phase 3, open-label study.
Handley A1, Lloyd E2, Roberts A2, Barger B2. Clin Exp Hypertens. 2016;38(2):180-8. doi: 10.3109/10641963.2015.1081213. Epub 2016 Jan 28.
This 56-week phase 3, open-label, treat-to-target study, involving 2 consecutive, non-randomized cohorts, evaluated the safety and tolerability of azilsartan medoxomil (AZL-M) in essential hypertension (mean baseline blood pressure [BP] 152/100 mmHg). All subjects (n = 669) initiated AZL-M 40 mg QD, force-titrated to 80 mg QD at week 4, if tolerated. From week 8, subjects could receive additional medications, starting with chlorthalidone (CLD) 25 mg QD (Cohort 1) or hydrochlorothiazide (HCTZ) 12.5-25 mg QD (Cohort 2), if required, to reach BP targets. Adverse events (AEs) were reported in 75.9% of subjects overall in the two cohorts (73.8% Cohort 1, 78.5% Cohort 2). The most common AEs were dizziness (14.3%), headache (9.9%) and fatigue (7.2%). Transient serum creatinine elevations were more frequent with add-on CLD. Clinic systolic/diastolic BP (observed cases at week 56) decreased by 25.2/18.4 mmHg (Cohort 1) and 24.2/17.9 mmHg (Cohort 2).
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CAS 863031-24-7 Azilsartan medoxomil monopotassium

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