1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor mAChR Adrenergic Receptor
  3. Promethazine hydrochloride

プロメタジン塩酸塩  (Synonyms: Promethazine (hydrochloride))

製品番号: HY-B0781 純度: 99.85%
COA 取扱説明書 Technical Support

Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors.

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Promethazine hydrochloride

プロメタジン塩酸塩 構造式

CAS 番号 : 58-33-3

容量 価格(税別) 在庫状況 数量
500 mg $25 在庫あり
1 g $35 在庫あり
5 g $50 在庫あり
10 g   お問い合わせ  
50 g   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 1 publication(s) in Google Scholar

Other Forms of Promethazine hydrochloride:

Top Publications Citing Use of Products

Histamine Receptor アイソフォーム固有の製品をすべて表示:

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Adrenergic Receptor アイソフォーム固有の製品をすべて表示:

  • 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

Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors[1][2].

IC50 & Target

H1 Receptor

 

5-HT2A Receptor

 

5-HT2C Receptor

 

Cellular Effect
Cell Line Type Value Description References
Vero C1008 CC50
>42.59 μM
Compound: Promethazine Hydrochloride
CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 CC50
>42.59 μM
Compound: Promethazine Hydrochloride
CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 IC50
10.44 μM
Compound: Promethazine Hydrochloride
IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 IC50
9.21 μM
Compound: Promethazine Hydrochloride
IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
10.1101/2020.03.25.008482
体外実験

Promethazine hydrochloride (1.25-10 μM, 3 days) inhibits adipocyte formation in a dose-dependent manner[1].
Promethazine hydrochloride (10 μM, 0-12 days) decreases the expression of peroxisome proliferator activated receptor γ (PPARG) and reduces the phosphorylation level of CREB in PDGFRα+ cells[1].
Promethazine hydrochloride (10-1000 μM, 1-24 h) has cytotoxic at concentrations greater than 100 μM in L929 lung fibroblast cells[3].

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

体内実験

Promethazine hydrochloride (0.05-0.1 mg/mL, p.o., 4 weeks) possesses inhibitory effect on ectopic fat cell formation in skeletal muscle in a mouse achilles tendon rupture model[1].
Promethazine hydrochloride (2.4-9.6 mg/kg, p.o.) has no effect on the development of femoral osteoporosis and retarded normal femoral expansion in the adult castrate male rats[4].

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

分子量

320.88

分子式

C17H21ClN2S

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

CC(N(C)C)CN1C(C=CC=C2)=C2SC3=CC=CC=C13.[H]Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture and light

*The compound is unstable in solutions, freshly prepared is recommended.

溶剤 & 溶解度
体外: 

H2O : 100 mg/mL (311.64 mM; Need ultrasonic)

DMSO : 50 mg/mL (155.82 mM; Need ultrasonic; 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 3.1164 mL 15.5821 mL 31.1643 mL
5 mM 0.6233 mL 3.1164 mL 6.2329 mL
10 mM 0.3116 mL 1.5582 mL 3.1164 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

* 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: ≥ 2.5 mg/mL (7.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

    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: ≥ 2.5 mg/mL (7.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

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: 120 mg/mL (373.97 mM); Clear solution; Need ultrasonic

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. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 3.1164 mL 15.5821 mL 31.1643 mL 77.9107 mL
5 mM 0.6233 mL 3.1164 mL 6.2329 mL 15.5821 mL
10 mM 0.3116 mL 1.5582 mL 3.1164 mL 7.7911 mL
15 mM 0.2078 mL 1.0388 mL 2.0776 mL 5.1940 mL
20 mM 0.1558 mL 0.7791 mL 1.5582 mL 3.8955 mL
25 mM 0.1247 mL 0.6233 mL 1.2466 mL 3.1164 mL
30 mM 0.1039 mL 0.5194 mL 1.0388 mL 2.5970 mL
40 mM 0.0779 mL 0.3896 mL 0.7791 mL 1.9478 mL
50 mM 0.0623 mL 0.3116 mL 0.6233 mL 1.5582 mL
60 mM 0.0519 mL 0.2597 mL 0.5194 mL 1.2985 mL
80 mM 0.0390 mL 0.1948 mL 0.3896 mL 0.9739 mL
100 mM 0.0312 mL 0.1558 mL 0.3116 mL 0.7791 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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  • 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.

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製品名:
Promethazine hydrochloride
製品番号:
HY-B0781
数量:
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