Cat. No.: HY-135336

(R)-Verapamil hydrochloride

(Synonyms: (R)-(+)-Verapamil hydrochloride)

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(R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is an orally active P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport. (R)-Verapamil hydrochloride induces Apoptosis and inhibits L-type calcium channels BZPcc, DHPcc and PLLcc. (R)-Verapamil hydrochloride has anti-septic shock and anti-diabetic effects.

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Pureté: 99.37%
CAS No.: 38176-02-2
Formule: C₂₇H₃₉ClN₂O₄
Masse moléculaire:491.06

Stockage:

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

(R)-Verapamil hydrochloride Chemical Structure

CAS No.: 38176-02-2

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform Calcium Channel :

In Vitro

(R)-Verapamil (10-1000 µM, contraction of RPE cells is complete after 15-18 h) hydrochloride inhibits the contraction of RPE cells^[3].
(R)-Verapamil (24 h) hydrochloride induces apoptosis in CH^RC5 cells at levels comparable to those induced by racemic verapamil^[4].
(R)-Verapamil (10 µM) hydrochloride inhibits L-type calcium channels BZPcc, DHPcc and PLLcc with 90%, 85% and 104% inhibition respectively^[5].
(R)-Verapamil (3-30 μM) hydrochloride exerts a consistent growth inhibition on BFU-E cells^[6].
(R)-Verapamil hydrochloride has a slight inhibitory effect on CFU-L colony growth, and combined with Daunorubicin (DNR) (HY-13062A) can reduce the average IC₅₀ of DNR^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

(R)-Verapamil (50-100 mg/kg, p.o., dissolved in drinking water, daily, 10 days in type 1 diabetes mouse model; 30-150 mg/kg; oral gavage; twice daily; 17 days-6 weeks in type 2 diabetes mouse model) hydrochloride shows antidiabetic effects in type 1 and type 2 diabetes mellitus mouse models^[5].
(R)-Verapamil (100 mg/kg, i.p., 1 h before the injection of LPS) hydrochloride significantly reduces mortality and cytokine (TNF-α and IFN-γ) expression in murine model of septic shock^[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male wild type C57BL/6J mice (7 weeks old), male C57BLKS/J Iar-+Lepr^db/+Lepr^db mice (male, 50 g, 9-10 weeks old); Streptozotocin (HY-13753)-induced type 1 diabetes mellitus model and db/db type 2 diabetes mellitus model^[5]
Dosage:

In type 1 diabetes mellitus model, 50 mg/kg/day and 100 mg/kg/day (dissolved in drinking water); in type 2 diabetes mellitus model, 30-150 mg/kg/day (dissolved in distilled water for monotherapy, and in 1% Tween 80 or 0.25% carboxymethylcellulose for combination therapy)
Administration:

In type 1 diabetes mellitus model, administered via drinking water, daily, for 10 days; in type 2 diabetes mellitus model, administered by oral gavage, twice daily, for 6 weeks (Experiment 2) or 17 days (Experiment 3)
Result:

Significantly reduced fasting blood glucose levels, downregulated Txnip expression, and decreased β-cell apoptosis at 100 mg/kg/day (the type 1 diabetes mellitus model).
Had the best effect on reducing blood glucose and increasing serum insulin levels at 60 mg/kg/day (the type 2 diabetes mellitus model).

Chemical Information

CAS No. 38176-02-2
Appearance Solid
Masse moléculaire 491.06
Formule C₂₇H₃₉ClN₂O₄
Color White to off-white
SMILES

COC1=C(OC)C=CC(CCN(C)CCC[C@](C#N)(C2=CC(OC)=C(OC)C=C2)C(C)C)=C1.Cl
Synonyms

(R)-(+)-Verapamil hydrochloride
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (203.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 100 mg/mL (203.64 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0364 mL

10.1821 mL

20.3641 mL

5 mM

0.4073 mL

2.0364 mL

4.0728 mL

10 mM

0.2036 mL

1.0182 mL

2.0364 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (10.18 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (10.18 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (10.18 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 50 mg/mL (101.82 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Plumb JA, et al. The activity of verapamil as a resistance modifier in vitro in drug resistant human tumour cell lines is not stereospecific. Biochem Pharmacol. 1990 Feb 15;39(4):787-92. [Content Brief]

[2]. Perrotton T, et al. (R)- and (S)-verapamil differentially modulate the multidrug-resistant protein MRP1. J Biol Chem. 2007 Oct 26;282(43):31542-8. Epub 2007 Jul 22. [Content Brief]

[3]. Faude F, et al. R-(+)-verapamil, S-(-)-verapamil, and racemic verapamil inhibit human retinal pigment epithelial cell contraction. Graefes Arch Clin Exp Ophthalmol. 2000 Jun;238(6):537-41. [Content Brief]

[4]. Karwatsky J, et al. A mechanism for P-glycoprotein-mediated apoptosis as revealed by verapamil hypersensitivity. Biochemistry. 2003 Oct 28;42(42):12163-73. [Content Brief]

[5]. Chen YS, et al. Evaluating the antidiabetic effects of R-verapamil in type 1 and type 2 diabetes mellitus mouse models. PLoS One. 2021 Aug 6;16(8):e0255405. [Content Brief]

[6]. Visani G, et al. Comparative effects of racemic verapamil vs R-verapamil on normal and leukemic progenitors. Ann Hematol. 1993 Jun;66(6):273-6. [Content Brief]

[7]. Wyska E. Pretreatment with R(+)-verapamil significantly reduces mortality and cytokine expression in murine model of septic shock. Int Immunopharmacol. 2009 Apr;9(4):478-90. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	2.0364 mL	10.1821 mL	20.3641 mL	50.9103 mL
	5 mM	0.4073 mL	2.0364 mL	4.0728 mL	10.1821 mL
	10 mM	0.2036 mL	1.0182 mL	2.0364 mL	5.0910 mL
	15 mM	0.1358 mL	0.6788 mL	1.3576 mL	3.3940 mL
	20 mM	0.1018 mL	0.5091 mL	1.0182 mL	2.5455 mL
	25 mM	0.0815 mL	0.4073 mL	0.8146 mL	2.0364 mL
	30 mM	0.0679 mL	0.3394 mL	0.6788 mL	1.6970 mL
	40 mM	0.0509 mL	0.2546 mL	0.5091 mL	1.2728 mL
	50 mM	0.0407 mL	0.2036 mL	0.4073 mL	1.0182 mL
	60 mM	0.0339 mL	0.1697 mL	0.3394 mL	0.8485 mL
	80 mM	0.0255 mL	0.1273 mL	0.2546 mL	0.6364 mL
	100 mM	0.0204 mL	0.1018 mL	0.2036 mL	0.5091 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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(R)-Verapamil hydrochloride

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Neuroprotective Compound Library

Calcium Channel Blocker Library

FDA-Approved Anticancer Drug Library

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Off-patent Drug Library

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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Voir tous les produits spécifiques à Isoform Calcium Channel

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

(R)-Verapamil hydrochloride Related Classifications

HY-135336 Related Classifications