2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. Doxapram

Doxapram is a respiratory stimulant. Doxapram increases breathing rate and depth by acting on the brain's respiratory centers and peripheral chemoreceptors. Doxapram inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50s of 410 nM, 37 μM, 9 μM, respectively. Doxapram inhibits the Ca²⁺-activated potassium current (IC50 ≈ 13 μM) and Ca²⁺-independent potassium current (IC50 ≈ 20 μM) in type I cells of the carotid body. Doxapram significantly prolongs the effective refractory period of the atrium and has an anti-arrhythmic effect. Doxapram can be used for the study of respiratory depression such as post-anesthesia respiratory depression, chronic obstructive pulmonary disease and apnea of prematurity.

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Doxapram

Doxapram 構造式

CAS 番号 : 309-29-5

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 27 在庫あり
Solution
10 mM * 1 mL in DMSO USD 27 在庫あり
Solid
10 mg $25 在庫あり
25 mg $45 在庫あり
50 mg $65 在庫あり
100 mg $100 在庫あり
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Doxapram 関連抗体

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製品説明

Doxapram is a respiratory stimulant. Doxapram increases breathing rate and depth by acting on the brain's respiratory centers and peripheral chemoreceptors. Doxapram inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50s of 410 nM, 37 μM, 9 μM, respectively. Doxapram inhibits the Ca²⁺-activated potassium current (IC50 ≈ 13 μM) and Ca²⁺-independent potassium current (IC50 ≈ 20 μM) in type I cells of the carotid body. Doxapram significantly prolongs the effective refractory period of the atrium and has an anti-arrhythmic effect. Doxapram can be used for the study of respiratory depression such as post-anesthesia respiratory depression, chronic obstructive pulmonary disease and apnea of prematurity[1][2][3][4][5][6].

体外実験

Doxapram (0.01-100 μM, 10-30 min) inhibits human and porcine TASK-1 with IC50s of 0.88 and 0.93 μM in human and porcine atrial muscle cells[6].

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

Doxapram 関連抗体
体内実験

Doxapram (0.05-0.25 mg/kg, i.v.) selectively but indirectly activate medullary respiratory neurons through carotid and aortic chemoreceptor stimulation in cats[4].
Doxapram (> 1 mg/kg, i.v.) stimulates the brainstem respiratory center rather than the peripheral chemoreceptors in dogs[4].
Doxapram (1-2 mg/kg, i.v., single dose or once daily for 14 days) has a specific anti-arrhythmic effect on the atrium in domestic pigs[6].

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

Animal Model: Acute atrial fibrillation and persistent atrial fibrillation models established in domestic pigs[6]
Dosage: 1 and 2 mg/kg (single dose) and 2 mg/kg (continuous administration)
Administration: Intravenous injection (i.v.), single dose or once daily for 14 days
Result: Prolonged the effective refractory period of the atrium (AERP), but has no effect on ventricular repolarization.
Reversed the electrical remodeling associated with AF (increased TASK-1 current and shortened APD) in long-term treatment.
分子量

378.51

分子式

C24H30N2O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(CC)CC(CCN2CCOCC2)C1(C3=CC=CC=C3)C4=CC=CC=C4
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: 

DMSO : 50 mg/mL (132.10 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 2.6419 mL 13.2097 mL 26.4194 mL
5 mM 0.5284 mL 2.6419 mL 5.2839 mL
10 mM 0.2642 mL 1.3210 mL 2.6419 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.

  • Molarity Calculator

  • Dilution Calculator

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

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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 (6.60 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 (6.60 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 1 mM 2.6419 mL 13.2097 mL 26.4194 mL 66.0485 mL
5 mM 0.5284 mL 2.6419 mL 5.2839 mL 13.2097 mL
10 mM 0.2642 mL 1.3210 mL 2.6419 mL 6.6048 mL
15 mM 0.1761 mL 0.8806 mL 1.7613 mL 4.4032 mL
20 mM 0.1321 mL 0.6605 mL 1.3210 mL 3.3024 mL
25 mM 0.1057 mL 0.5284 mL 1.0568 mL 2.6419 mL
30 mM 0.0881 mL 0.4403 mL 0.8806 mL 2.2016 mL
40 mM 0.0660 mL 0.3302 mL 0.6605 mL 1.6512 mL
50 mM 0.0528 mL 0.2642 mL 0.5284 mL 1.3210 mL
60 mM 0.0440 mL 0.2202 mL 0.4403 mL 1.1008 mL
80 mM 0.0330 mL 0.1651 mL 0.3302 mL 0.8256 mL
100 mM 0.0264 mL 0.1321 mL 0.2642 mL 0.6605 mL
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Doxapram 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:

Doxapram309-29-5Potassium ChannelKcsAAntiarrhythmic pharmacotherapyatrial fibrillationdoxapramrhythm controlTASK-1Inhibitorinhibitorinhibit

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