Carteolol HCl (OPC-1085 HCl)

Alias: OPC 1085; Carteolol Hydrochloride; Carteolol HCl; OPC-1085; OPC1085; Arteoptic; Cartrol; Mikelan; Abbott-43326; Hydrochloride; Carteolol; Monohydrochloride; Carteolol

Cat No.:V1104 Purity: ≥98%

COA Product Data Instructions for use SDS

Carteolol HCl (OPC-1085 HCl) Chemical Structure CAS No.: 51781-21-6
Product category: Adrenergic 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 Carteolol HCl (OPC-1085 HCl):

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Top Publications Citing lnvivochem Products

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

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

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

Carteolol HCl (OPC1085; Arteoptic; Cartrol; Mikelan; Abbott-43326), the hydrochloride salt of Carteolol, is a potent and non-selective β-adrenoceptor antagonist that was approved for the treatment of glaucoma. Carteolol was discovered to be a nonconventional partial agonist that interacts with the low-affinity propranolol-resistant site of β1-adrenoceptors to produce agonistic effects and the high-affinity site of the same receptors to produce antagonistic actions.

Biological Activity I Assay Protocols (From Reference)

Targets

Beta adrenergic Receptor

ln Vitro

In vitro activity: Carteolol HCl is a beta-adrenergic antagonist that has four main uses: it lowers blood pressure, treats angina, treats arrhythmia, and treats glaucoma. Carteolol hydrochloride was able to scavenge O2 (EC50 value: 48 mmol/L) and significantly inhibit H2O2-induced cell damage at 1 mmol/L (P<0.05). The ability of carteolol hydrochloride to scavenge radicals may play a significant role in its protective action against UVB-induced HCEC damage [1]. There are no appreciable safety differences between the new alginate formulation of long-acting carteolol 1% given once daily and standard 1% carteolol given twice daily in terms of effectiveness. At 9 AM (24 hours after the last long-acting carteolol drop or 12 hours after the last standard carteolol drop) and 11 AM (two hours after the morning drop), the effectiveness of this treatment was confirmed. Patients with glaucoma who need long-term care respond well to the new alginate formulation of long-acting carteolol 1% when taken once daily [2].

ln Vivo

Carbolelol and 8-OH carteolol both prevented rabbits' intraocular pressure (IOP) from rising in response to water load. When it came to reducing the water-load-induced increase in intracranial pressure in rabbits, 8-OH carteolol outperformed carteolol on an equimolar basis. Monkeys' IOP significantly decreased in response to both 8-OH carteolol and carteolol. In terms of lowering IOP in monkeys, 8-OH carteolol was found to be more effective than carteolol on an equimolar basis.

Animal Protocol

N/A

Monkeys

References

[1]. Carteolol hydrochloride protects human corneal epithelial cells from UVB-induced damage in vitro. Cornea, 2005. 24(2): p. 213-20.

[2]. [Efficacy and safety of long-acting carteolol 1% once daily. A double-masked, randomized study]. J Fr Ophtalmol, 2003. 26(2): p. 131-6.

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

Physicochemical Properties

Molecular Formula

C16H25CLN2O3

Molecular Weight

328.83

Exact Mass

328.16

Elemental Analysis

C, 58.44; H, 7.66; Cl, 10.78; N, 8.52; O, 14.60

CAS #

51781-21-6

Related CAS #

Carteolol-d9 hydrochloride; 1346602-13-8; Carteolol; 51781-06-7

Appearance

Solid powder

SMILES

CC(C)(C)NCC(COC1=CC=CC2=C1CCC(=O)N2)O.Cl

InChi Key

FYBXRCFPOTXTJF-UHFFFAOYSA-N

InChi Code

InChI=1S/C16H24N2O3.ClH/c1-16(2,3)17-9-11(19)10-21-14-6-4-5-13-12(14)7-8-15(20)18-13;/h4-6,11,17,19H,7-10H2,1-3H3,(H,18,20);1H

Chemical Name

5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydro-1H-quinolin-2-one;hydrochloride

Synonyms

OPC 1085; Carteolol Hydrochloride; Carteolol HCl; OPC-1085; OPC1085; Arteoptic; Cartrol; Mikelan; Abbott-43326; Hydrochloride; Carteolol; Monohydrochloride; Carteolol

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: 50~65 mg/mL (152.1~197.7 mM)

Water: <1 mg/mL

Ethanol: ~65 mg/mL (~197.7 mM)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.0411 mL	15.2054 mL	30.4109 mL
	5 mM	0.6082 mL	3.0411 mL	6.0822 mL
	10 mM	0.3041 mL	1.5205 mL	3.0411 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)

Volume (Start)

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.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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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
NCT05583474	Recruiting	Drug: OPC-1085EL Drug: 0.005% Latanoprost	Open Angle Glaucoma or Ocular Hypertension	Otsuka Beijing Research Institute	September 27, 2022	Phase 3
NCT02105285	Completed	Drug: OPC-1085EL ophthalmic solution Drug: Carteolol long-acting ophthalmic solution	Glaucoma Ocular Hypertension	Otsuka Pharmaceutical Co., Ltd.	April 2014	Phase 3
NCT02105272	Completed	Drug: OPC-1085EL ophthalmic solution Drug: Latanoprost ophthalmic	Glaucoma Ocular Hypertension	Otsuka Pharmaceutical Co., Ltd.	April 2014	Phase 3
NCT02108288	Completed	Drug: OPC-1085EL ophthalmic solution Drug: Latanoprost ophthalmic	Glaucoma Ocular Hypertension	Otsuka Pharmaceutical Co., Ltd.	April 2014	Phase 1

Biological Data

Mean concentration-effect curves for the chronotropic and inotropic effects of carteolol and xamoterol in guinea pig spontaneously beating atria.J Pharmacol Exp Ther.2005 Dec;315(3):1386-95.
Mean concentration-effect curves for the inotropic effect of carteolol and xamoterol on guinea pig left atria electrically driven at 2 Hz.J Pharmacol Exp Ther.2005 Dec;315(3):1386-95.
Concentration-effect curves for the chronotropic effects of carteolol, xamoterol, and isoprenaline in the absence and presence of propranolol.J Pharmacol Exp Ther.2005 Dec;315(3):1386-95.