Olmesartan (RNH-6270; CS-866)

Alias: Benicar; Olmetec; Votum; RNH-6270; RNH6270; RNH 6270; CS-866; CS866; CS 866; Olmesartan; Olmesartan medoxomil; Olmetec; Olsertain; Azor; Benicar

Cat No.:V5109 Purity: ≥98%

COA Product Data Instructions for use SDS

Olmesartan (formerly also known as CS-866) is a potent and selective angiotensin II type 1 (AT(1)) receptor antagonist used in the treatment of high blood pressure.

Olmesartan (RNH-6270; CS-866) Chemical Structure CAS No.: 144689-24-7
Product category: Angiotensin Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Olmesartan (RNH-6270; CS-866):

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

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Nature 597, 119–125 (2021)

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Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Olmesartan (formerly also known as CS-866) is a potent and selective angiotensin II type 1 (AT(1)) receptor antagonist used in the treatment of high blood pressure. It also prevents renin secretion from receiving a negative regulatory feedback. Vasodilation and a decrease in peripheral resistance occur as a result of receptor suppression. Lipid hydroxyproline content and TGF-beta1 are markedly decreased by olmesartan medoxomil.

Biological Activity I Assay Protocols (From Reference)

ln Vitro

In vitro activity: Olmesartan (0.7-5 mM; 24, 48 and 72 h) inhibits the growth of HeLa cells in a concentration- and time-dependent manner[3].

ln Vivo

Olmesartan (1 mg/kg, 2 mg/kg, p.o.) is dose-dependently lowered in SHR after repeated administration, with no discernible effects on body weight or food consumption over a 10-week period[1]. Mice treated with Hyd and olemesartan (5 mg/kg/d, p.o.) exhibit comparable reductions in systolic blood pressure. Treatment with olmesartan prevents cardiac hypertrophy as determined by gene expression, heart weight, cardiomyocyte cross-sectional area, and echocardiography. Treatment with omesartan reverses the downregulation of Ren-Tg mice's ACE2 and Mas receptor gene expressions, and it prevents the upregulation of NADPH oxidase (Nox)4 expression and reactive oxygen species[2].

Enzyme Assay

Olmesartan medoxomil, with an IC50 of 66.2 μM, is a strong and specific inhibitor of the angiotensin AT1 receptor.

Cell Assay

Cell Line: Human cervical cancer cell line (HeLa)
Concentration: 0.7- 5 mM
Incubation Time: 24, 48 and 72 h
Result: IC50s against HeLa cell line are 4.685 and 1.651 mM for 48 and 72 h, respectively

Animal Protocol

Male db/db diabetic mice aged 10 to 12 weeks, using background strain C57BL/KsJ, are employed, along with age-matched non-diabetic lean control mice (C57BL).For a period of 12 weeks, ten diabetic mice and ten non-diabetic control mice were given a placebo (0.5% sodium CMC/saline solution), while the other ten diabetic mice received daily gavages of 20 mg/kg Olmesartan (MB5704). Every two weeks, the blood glucose, body weight, and urine output of the mice are observed. Following therapy, mice are put to sleep, and trunk blood is taken, centrifuged, and then aliquoted and kept at -80°C to extract plasma. Mice's kidney tissues are extracted. Kidney tissue slices are frozen in liquid nitrogen and kept at -80°C in order to extract proteins. The remaining kidney tissue is embedded in paraffin and fixed with 4% paraformaldehyde in order to be immunostained.

Mice

References

[1]. Effects of telmisartan and olmesartan on insulin sensitivity and renal function in spontaneously hypertensive rats fed a high fat diet. J Pharmacol Sci. 2016 Jul;131(3):190-7.

[2]. Olmesartan Inhibits Cardiac Hypertrophy in Mice Overexpressing Renin Independently of Blood Pressure: Its Beneficial Effects on ACE2/Ang(1-7)/Mas Axis and NADPH Oxidase Expression. J Cardiovasc Pharmacol. 2016 Jun;67(6):503-9.

[3]. Synergistic, cytotoxic and apoptotic activities of olmesartan with NF-κB inhibitor against HeLa human cell line. Toxicol Mech Methods. 2015;25(8):614-21.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C24H26N6O3

Molecular Weight

446.50

Exact Mass

446.21

Elemental Analysis

C, 64.56; H, 5.87; N, 18.82; O, 10.75

CAS #

144689-24-7

Related CAS #

Olmesartan-d4; 1420880-41-6; Olmesartan-d6; 1185144-74-4; Olmesartan medoxomil; 144689-63-4

Appearance

Solid powder

SMILES

CCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)C(=O)O)C(C)(C)O

InChi Key

VTRAEEWXHOVJFV-UHFFFAOYSA-N

InChi Code

InChI=1S/C24H26N6O3/c1-4-7-19-25-21(24(2,3)33)20(23(31)32)30(19)14-15-10-12-16(13-11-15)17-8-5-6-9-18(17)22-26-28-29-27-22/h5-6,8-13,33H,4,7,14H2,1-3H3,(H,31,32)(H,26,27,28,29)

Chemical Name

5-(2-hydroxypropan-2-yl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylic acid

Synonyms

Benicar; Olmetec; Votum; RNH-6270; RNH6270; RNH 6270; CS-866; CS866; CS 866; Olmesartan; Olmesartan medoxomil; Olmetec; Olsertain; Azor; Benicar

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: ≥ 55 mg/mL

Water: <1 mg/mL

Ethanol: <1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (5.60 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (5.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.2396 mL	11.1982 mL	22.3964 mL
	5 mM	0.4479 mL	2.2396 mL	4.4793 mL
	10 mM	0.2240 mL	1.1198 mL	2.2396 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

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Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05103332	Active Recruiting	Drug: Olmesartan Drug: Amlodipine	Hypertension	Alnylam Pharmaceuticals	November 5, 2021	Phase 2
NCT05411887	Recruiting	Drug: Rosuvastatin, Olmesartan Medoxomil	Hyperlipidemias Hypertension	Daewoong Pharmaceutical Co. LTD.	June 20, 2022	N/A
NCT02483936	Not yet recruiting	Drug: Olmesartan medoxomil 40mg + chlorthalidone 12,5mg Drug: Olmesartan 40mg + Hydrochlorothiazide 25mg	Arterial Hypertension	EMS	April 2023	Phase 3
NCT02493322	Not yet recruiting	Drug: Olmesartan Medoxomil 20mg + Chlorthalidone 12,5mg Drug: Olmesartan medoxomil 20mg + Chlortalidone 25mg	Essential Arterial Hypertension	EMS	April 2023	Phase 3
NCT05917275	Not yet recruiting	Drug: Amlodipine Drug: Olmesartan	Primary Hypertension	Radboud University Medical Center	October 2023	Phase 4

Biological Data

Effects of telmisartan (Tel) (A) and olmesartan (Olm) (B) after dosing for more than 4 weeks on mean arterial blood pressure (MAP) in SHR fed a high fat diet (HFD). J Pharmacol Sci . 2016 Jul;131(3):190-7.

Effects of telmisartan (HFD-Tel) and olmesartan (HFD-Olm) for 10 weeks on body weight (BW) change (A), food intake (B) and blood pressure (BP) (C) in SHR fed a high fat diet (HFD). J Pharmacol Sci . 2016 Jul;131(3):190-7.

Effects of telmisartan (HFD-Tel) and olmesartan (HFD-Olm) for 9 weeks on insulin tolerance test (ITT) (A) and for 11 weeks on serum adiponectin concentration (B) in SHR fed a high fat diet (HFD). J Pharmacol Sci . 2016 Jul;131(3):190-7.