Cat. No.: HY-108974

Drotaverine hydrochloride

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Based on 1 Customer Validation

Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.

For research use only. We do not sell to patients.

Purity: 99.65%
CAS No.: 985-12-6
Formula: C₂₄H₃₂ClNO₄
Molecular Weight:433.97

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Drotaverine hydrochloride Chemical Structure

CAS No.: 985-12-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

L-type calcium channel

PDE4

All Phosphodiesterase (PDE) Isoforms :

All Calcium Channel Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	CC₅₀	9 μM Compound: DROTAVERINE	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	6.07 μM Compound: DROTAVERINE	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1

In Vitro

Drotaverine hydrochloride is a relaxant for pre-contracted airways that shows concentration-dependent and medium-dependent effects. The ED ₅₀ for histamine, methacholine, and potassium chloride as contractile agents are 4.7×10^-5, 4.3×10^-5, and 2.2×10^-5 mol/L^[1].
Drotaverine hydrochloride suppresses bronchial contractions in guinea pigs, with ED ₅₀ values for histamine, methacholine, and potassium chloride being 8.5×10^-5, 9.3×10^-5, and 7.4×10^-5 mol/L^[1].
Drotaverine hydrochloride shows higher selectivity for KCl-induced contractions^[1].
Drotaverine hydrochloride inhibits the specific binding of nifedipine and diltiazem, with IC₅₀ values of 5.6 and 2.6 μM^[2].
Drotaverine hydrochloride significantly increases the dissociation rate constants (k^-1 (min^-1)) for nifedipine and diltiazem from the uterine membranes of pregnant rats to 0.055 and 0.062, respectively, with corresponding half-lives (t_1/2 (min)) of 5.55 and 4.9^[2].

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

In Vivo

Drotaverine (10-80 mg/kg, i.p., single dose) hydrochloride improves cognitive impairment and shows the ability to regulate levels of neurotransmitters in the brain^[3].

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

Animal Model:

STZ-induced AD white mice ^[3]
Dosage:

10, 20, 40, 80 mg/kg; single dose
Administration:

Intraperitoneal injection (i.p.)
Result:

Increased physical activity in a dose-dependent manner, with more time spent in the open arms, increased in the number of crossings and time spent in the north quadrant.
Increased in brain antioxidant levels (SOD, CAT, GSH), a reduction in nitrite levels, and significant increased in serotonin, dopamine, and norepinephrine levels.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 985-12-6
Appearance Solid
Molecular Weight 433.97
Formula C₂₄H₃₂ClNO₄
Color White to light yellow
SMILES

CCOC1=CC2=C(C=C1OCC)CCN/C2=C\C3=CC=C(OCC)C(OCC)=C3.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (230.43 mM; Need ultrasonic)

DMSO : 62.5 mg/mL (144.02 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.3043 mL

11.5215 mL

23.0431 mL

5 mM

0.4609 mL

2.3043 mL

4.6086 mL

10 mM

0.2304 mL

1.1522 mL

2.3043 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. 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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: ≥ 2.08 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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) .

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 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)
Handling Instructions (2659 KB)

References

[1]. Patai Z, Guttman A, Mikus EG. Assessment of the Airway Smooth Muscle Relaxant Effect of Drotaverine. Pharmacology. 2018;101(3-4):163-169. [Content Brief]

[2]. Zsuzsanna Tömösközi, et al. Drotaverine interacts with the L-type Ca(2+) channel in pregnant rat uterine membranes. Eur J Pharmacol. 2002 Aug 2;449(1-2):55-60. [Content Brief]

[3]. Samra Nazir, et al. Drotaverine Inhibitor of PDE4: Reverses the Streptozotocin Induced Alzheimer's Disease in Mice. Neurochem Res. 2021 Jul;46(7):1814-1829. [Content Brief]

[4]. Athanas D. Kristev, et al. Comparing hyoscine and drotaverine effects on colon in CT colonography. Cent. Eur. J. Med.6(2) . 2011 . 234-242

[5]. Ioana Z Pavel, et al. Drotaverine - a Concealed Cytostatic!.Arch Pharm (Weinheim). 2017 Jan;350(1). [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

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	2.3043 mL	11.5215 mL	23.0431 mL	57.6077 mL
	5 mM	0.4609 mL	2.3043 mL	4.6086 mL	11.5215 mL
	10 mM	0.2304 mL	1.1522 mL	2.3043 mL	5.7608 mL
	15 mM	0.1536 mL	0.7681 mL	1.5362 mL	3.8405 mL
	20 mM	0.1152 mL	0.5761 mL	1.1522 mL	2.8804 mL
	25 mM	0.0922 mL	0.4609 mL	0.9217 mL	2.3043 mL
	30 mM	0.0768 mL	0.3841 mL	0.7681 mL	1.9203 mL
	40 mM	0.0576 mL	0.2880 mL	0.5761 mL	1.4402 mL
	50 mM	0.0461 mL	0.2304 mL	0.4609 mL	1.1522 mL
	60 mM	0.0384 mL	0.1920 mL	0.3841 mL	0.9601 mL
	80 mM	0.0288 mL	0.1440 mL	0.2880 mL	0.7201 mL
	100 mM	0.0230 mL	0.1152 mL	0.2304 mL	0.5761 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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Drotaverine hydrochloride

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All Phosphodiesterase (PDE) Isoforms

All Calcium Channel Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Drotaverine hydrochloride Related Classifications

HY-108974 Related Classifications