Name: Doxapram HCl
Brand: Selleck Chemicals
SKU: S4037
Availability: InStock
Rating: 5 (1 reviews)

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Quality Control

Batch: Purity: 99.75%

99.75

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel GABA Receptor TRP Channel ATPase GluR
Other Potassium Channel Inhibitors	Nicorandil TRAM-34 Hydralazine HCl Nigericin Sophocarpine ML133 HCl Gliquidone PAP-1 E-4031 dihydrochloride Ajmaline

Solubility

In vitro
Batch:

DMSO : 87 mg/mL (200.93 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 25 mg/mL

Ethanol : 2 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	Saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (11.55mM)	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	432.98	Formula	C₂₄H₃₀N₂O₂.HCl.H₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	7081-53-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCN1CC(C(C1=O)(C2=CC=CC=C2)C3=CC=CC=C3)CCN4CCOCC4.O.Cl

Mechanism of Action

Targets/IC₅₀/Ki	TASK-1 410 nM(EC50) TASK-1/TASK-3 heterodimeric 9 μM(EC50) TASK-3 37 μM(EC50)
In vitro	Doxapram inhibits both TASK-1 and TASK-3 function in a dose dependent manner. Doxapram inhibition at both hyperpolarized and depolarized potentials, as well as effects independent of extracellular potassium concentration. It is said that the carboxy terminal domain of TASK-1 is important to doxapram inhibition. Doxapram also inhibits TRESK, TASK-2, and TREK-1 but at significantly larger concentrations (EC50s of 240 μM, 460 μM, and >1 mM, respectively). Doxapram has no effect on MAC for halothane.
In vivo	Doxapram is an analeptic agent. The respiratory stimulant action is manifested by an increase in tidal volume associated with a slight increase in respiratory rate. A pressor response may result following Doxapram administration. The mean half-life is 3.4 h (range 2.4-4.1h), the mean apparent volume of distribution is 1.5 mg/kg and the whole body clearance is 370 mL/min. Enteric-coated capsules of doxapram base are absorbed rapidly after an initial delay, and the systemic availability is about 60%.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16492828/ [2] http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1429614 [3] https://pubmed.ncbi.nlm.nih.gov/12933397/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03894189	Unknown status	Weaning Failure	Beni-Suef University	May 2019	Not Applicable
NCT02421068	Completed	Premature Birth	Sinno H.P. Simons\|ZonMw: The Netherlands Organisation for Health Research and Development\|Leiden Amsterdam Centre for Drug Research (LACDR)\|Dutch Knowledge Centre for Pediatric Pharmacotherapy (NKFK)\|Centre for Human Drug Research Netherlands\|Radboud University Medical Center\|Erasmus Medical Center	August 2014	--
NCT00389909	Completed	Premature Infants\|Apnea	Jean Michel Hascoet\|Maternite Regionale Universitaire	November 2006	Phase 4

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Doxapram HCl Potassium Channel inhibitor

Chemical Structure

Molecular Weight: 432.98