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.
Publictions citing BOC Sciences Products
  • >> More
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).
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Angiotensin Receptor Products


CAS 127060-75-7 CGP-42112A

CGP-42112A
(CAS: 127060-75-7)

CGP-42112A, an angiotensin AT2 receptor agonist which could probably lead to the inhibition of ATPase and contraction of aortic rings in rabbit.

CAS 51833-78-4 Angiotensin I/II (1-7)

Angiotensin I/II (1-7)
(CAS: 51833-78-4)

Angiotensin-(1-7) is an endogenous ligand for the G protein-coupled receptor, inducing vasorelaxation through release of NO and prostaglandins.

AVE 0991 sodium salt
(CAS: 306288-04-0)

AVE 0991 sodium salt, is an agonist of nonpeptide Ang-(1-7) receptor Mas that has potential as a cardiovascular drug.

CAS 124750-99-8 Losartan Potassium (DuP 753)

Losartan Potassium (DuP 753)
(CAS: 124750-99-8)

Losartan is an angiotensin II receptor antagonist that competes with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM. It promotes vasodilatati...

BMS 183920
(CAS: 153072-33-4)

BMS 183920, a quinoline derivative, has been found to be an angiotensin II receptor antagonist that could have potential usage in antihypertensive study.

CGP 48369
(CAS: 135689-23-5)

Cgp 48369 is a nonpeptide a angiotensin type 1 receptor antagonist originated by Novartis. Treatmenf for for Hypertension in Switzerland was discontinued in 199...

CAS 53902-12-8 Tranilast

Tranilast
(CAS: 53902-12-8)

Tranilast, also called Rizaben or Tranilastum, has anti-inflammatory and immunomodulatory effect. It binds to Aβ40 monomers and increases Aβ40 fibrillation.

CAS 145040-37-5 Candesartan Cilexetil

Candesartan Cilexetil
(CAS: 145040-37-5)

Candesartan blocks the effects of angiotensin II at the angiotensin II type 1 (AT1) receptor. Candesartan cilexetil is a prodrug that is activated to candesarta...

CAS 863031-24-7 Azilsartan medoxomil monopotassium

Azilsartan medoxomil monopotassium
(CAS: 863031-24-7)

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...

CAS 144689-24-7 Olmesartan

Olmesartan
(CAS: 144689-24-7)

Olmesartan, a synthetic imidazole derivative, is a specific angiotensin II type 1 (AT1) receptor antagonist with antihypertensive effect. hAT1 receptors: IC50 =...

AVE 0991
(CAS: 304462-19-9)

AVE 0991 is an agonist of nonpeptide Ang-(1-7) receptor Mas that has potential as a cardiovascular drug.

CAS 144689-63-4 Olmesartan Medoxomil

Olmesartan Medoxomil
(CAS: 144689-63-4)

Olmesartan Medoxomil is a compound which is hydrolyzed to olmesartan that is a selective AT1 subtype angiotensin II receptor antagonist.

CAS 144701-48-4 Telmisartan

Telmisartan
(CAS: 144701-48-4)

Telmisartan, also called Pritor, a benzimidazole derivative, is an angiotensin II receptor antagonist that can be used to treat hypertension. in vitro: activate...

CAS 863031-21-4 Azilsartan Medoxomil

Azilsartan Medoxomil
(CAS: 863031-21-4)

Azilsartan Medoxomil is a potent angiotensin II type 1 (AT1) receptor antagonist that inhibits the RAAS, with an IC50 of 2.6 nM. It exhibits more than 10,000-fo...

CAS 154512-46-6 L162441

L162441
(CAS: 154512-46-6)

An antagonist of Angiotensin type 1 receptor

Tranilast Sodium
(CAS: 104931-56-8)

Tranilast, an allergic media blocker, is effective for the treatment of asthma and is also used to treat asthma, allergic rhinitis and other allergic disorders.

CAS 139481-59-7 Candesartan

Candesartan
(CAS: 139481-59-7)

Candesartan (10 mg/kg) inhibits the growth of engrafted tumors and reduces the microvessel density and VEGF expression in a mouse KU-19-19 xenograft model

CAS 133085-33-3 BIBS 39

BIBS 39
(CAS: 133085-33-3)

BIBS 39, a nonpeptide angiotensin II receptor antagonist, has been found to exhibit potential antihypertensive activity in rat. It has been already discontinued...

CAS 159748-08-0 LY285434

LY285434
(CAS: 159748-08-0)

An antagonist of angiotensin II receptor

CAS 156001-18-2 Embusartan

Embusartan
(CAS: 156001-18-2)

Embusartan, an oxopyridine derivative, has been found to be an angiotensin II receptor antagonist that was once studied against hypertension by Bayer.

Chemical Structure

CAS 863031-24-7 Azilsartan medoxomil monopotassium

Quick Inquiry

Verification code

Featured Items