2. Metabolic Enzyme/Protease Neuronal Signaling Membrane Transporter/Ion Channel
  3. Phosphodiesterase (PDE) Calcium Channel
  4. Drotaverine hydrochloride

Drotaverine (hydrochloride)  (Synonyms: ドロタベリン塩酸塩)

製品番号: HY-108974 純度: 99.65%
COA 取扱説明書 Technical Support

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Drotaverine hydrochloride

Drotaverine (hydrochloride) 構造式

CAS 番号 : 985-12-6

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
5 mg $60 在庫あり
10 mg $90 在庫あり
25 mg $200 在庫あり
50 mg $320 在庫あり
100 mg $550 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 0 publication(s) in Google Scholar

Other Forms of Drotaverine hydrochloride:

Drotaverine (hydrochloride) 関連抗体

Top Publications Citing Use of Products

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

Calcium Channel アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

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.

IC50 & Target

L-type calcium channel

 

PDE4

 

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
体外実験

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 (t1/2 (min)) of 5.55 and 4.9[2].

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

Drotaverine (hydrochloride) 関連抗体
体内実験

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.
臨床実験
分子量

433.97

分子式

C24H32ClNO4
CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
View the Complete Stock Solution Preparation Table

* 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

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: 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).
純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* 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.

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.

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Drotaverine hydrochloride Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Drotaverine985-12-6Phosphodiesterase (PDE)Calcium ChannelCa2+ channelsCa channelsPregnant uterine smooth muscleTracheal contractionSmooth muscle relaxantInhibitorinhibitorinhibit

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

  

カスタマ需要量 *

お名前 *

 

タイトル

メールアドレス *

 

電話番号 *

デパートメント

 

組纖名 *

市区町村

都道府県

国或いは地域 *

      

必ず会社名を記載ください。個人への返信は行いません。

備考

バルクお問い合わせ

Inquiry Information

製品名:
Drotaverine hydrochloride
製品番号:
HY-108974
数量:
MCE 日本正規代理店:

カスタマーレビュー

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

製品名

  

Lot #

お名前 *

 

メールアドレス *

電話番号 *

 

部門 *

組纖名 *

 

国或いは地域 *

備考

Request for HNMR Report

We have received your request and will respond to you as soon as possible.