| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Dopexamine hydrochloride targets dopamine D1 (DA1) receptors and β2-adrenergic receptors, with minimal direct activity at β1-adrenoceptors and no activity at vascular α-adrenoceptors; it also stimulates dopamine type 1 and 2 receptors, producing vasodilatory effects.
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| ln Vitro |
Dopexamine functions as an agonist at beta2 and dopaminergic receptors, making it an analog of dopamine. At doses that do not change general hemodynamics or local microvascular blood flow, dopexamine attenuates systemic inflammatory reactions, decreases tissue leukocyte infiltration, and prevents organ damage [1]. Dopexamine is a dopamine analogue that causes some vasodilation by stimulating dopamine 1 and 2 receptors as well as beta-adrenergic receptors. Without appreciably changing systemic hemodynamics, such as blood pressure or stroke volume, dopexamine lowers systemic inflammatory reactions to endotoxins, such as cytokine release, endothelial adhesion molecules, and oxidative stress [2].
In vitro studies demonstrate that Dopexamine hydrochloride acts as an agonist at β2 and dopaminergic receptors, increasing cardiac contractility and inducing vasodilation in isolated tissue preparations, with its receptor binding profile distinct from other catecholamines. |
| ln Vivo |
In vivo, Dopexamine hydrochloride increases cardiac output while reducing systemic vascular resistance, making it useful for managing heart failure and hemodynamic support; it also reduces endotoxin-induced systemic inflammatory responses, including cytokine release and endothelial adhesion molecule expression, without significantly altering systemic hemodynamics.
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| Enzyme Assay |
The in vitro receptor binding assay for Dopexamine hydrochloride involves incubating the compound with membranes expressing D1 dopamine receptors or β2-adrenoceptors and radiolabeled ligands (e.g., [3H]SCH23390 or [3H]CGP12177), measuring displacement to determine binding affinity (Ki) and selectivity via competitive binding experiments.
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| Cell Assay |
In vitro cell culture studies utilize cells expressing dopamine or adrenergic receptors (e.g., HEK293 cells transfected with D1 or β2 receptors) treated with Dopexamine hydrochloride, measuring receptor activation via cAMP accumulation assays or β-arrestin recruitment, with EC50 values determined from concentration-response curves.
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| Animal Protocol |
In vivo animal experiments involve administering Dopexamine hydrochloride to animal models of heart failure or endotoxemia (e.g., rats or dogs), measuring hemodynamic parameters (cardiac output, blood pressure, heart rate), inflammatory markers (cytokines, adhesion molecules) by ELISA, and oxidative stress markers in tissues.
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| ADME/Pharmacokinetics |
Dopexamine hydrochloride has a molecular weight of 392.96 g/mol and is stored as a solid powder at 2-8°C; it is soluble in DMSO and aqueous buffers, with typical doses for in vivo studies ranging from 0.5 to 5 μg/kg/min depending on the experimental model.
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| Toxicity/Toxicokinetics |
Toxicological data from clinical studies indicate that Dopexamine hydrochloride is generally well-tolerated at therapeutic doses, though it may cause tachycardia, hypotension, and arrhythmias at higher doses; it is contraindicated in patients with pheochromocytoma and should be used with caution in those with ischemic heart disease.
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| References |
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| Additional Infomation |
Dopexamine hydrochloride is an approved pharmaceutical agent used in the management of heart failure and hemodynamic support in critically ill patients; it is available as an intravenous formulation and has been studied for its anti-inflammatory properties in sepsis and other inflammatory conditions.
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| Molecular Formula |
C22H32N2O2.2[HCL]
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|---|---|
| Molecular Weight |
429.42356
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| Exact Mass |
428.2
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| CAS # |
86484-91-5
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| Related CAS # |
86197-47-9 (Parent)
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| PubChem CID |
68603
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| Appearance |
Off-white to light yellow solid powder
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| Boiling Point |
546.7ºC at 760 mmHg
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| Flash Point |
115.1ºC
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| LogP |
6.008
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
28
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| Complexity |
334
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VPDULUNRSQWWJB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H32N2O2.2ClH/c25-21-11-10-20(18-22(21)26)13-17-24-15-7-2-1-6-14-23-16-12-19-8-4-3-5-9-19;;/h3-5,8-11,18,23-26H,1-2,6-7,12-17H2;2*1H
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| Chemical Name |
4-[2-[6-(2-phenylethylamino)hexylamino]ethyl]benzene-1,2-diol;dihydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3287 mL | 11.6436 mL | 23.2872 mL | |
| 5 mM | 0.4657 mL | 2.3287 mL | 4.6574 mL | |
| 10 mM | 0.2329 mL | 1.1644 mL | 2.3287 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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