| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 1g | |||
| Other Sizes |
| Targets |
Cinepazide is a piperazine derivative and a weak calcium channel blocker. Its vasodilatory effects are mediated through calcium channel blockade and potentiation of purinergic P1 receptor-mediated relaxation. It is used as a research tool to study cerebrovascular function.
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| ln Vitro |
In vitro, Cinepazide acts as a weak calcium channel blocker. It potentiates the relaxing responses to ATP. It protects neuronal cells against oxygen-glucose deprivation (OGD) injury by suppressing OGD-induced oxidative stress and preserving mitochondrial functions.
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| ln Vivo |
In dogs, intravertebral adenosine and cyclic AMP increase the vertebral vasodilatory response, but cinnarizine reduces these effects [1]. Cinepazide is administered intravenously at a dose of 30 mg/kg. In dogs, aminophylline partially inhibits the dose-related increase in vertebral blood flow caused by cinepazide (intravertebral injection; 1–10 mg/kg) [1].
In vivo, Cinepazide (30 mg/kg, i.v.) potentiated the vertebral vasodilator response of dogs to intravertebral adenosine and cyclic AMP. It is a potent vasodilator. It is used for the research of cerebrovascular diseases, including ischemic stroke and brain infarction. |
| Enzyme Assay |
In vitro assays for Cinepazide typically measure its effects on calcium channel activity. This can be assessed using patch-clamp electrophysiology or by measuring calcium influx using fluorescent indicators. Its vasodilatory effects can be studied using isolated blood vessel preparations.
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| Cell Assay |
Cellular assays for Cinepazide are performed using neuronal cells. Cells are subjected to oxygen-glucose deprivation (OGD) to model ischemic injury. The compound is added, and cell viability, oxidative stress markers, and mitochondrial function are assessed.
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| Animal Protocol |
In vivo animal studies with Cinepazide are conducted in animal models of cerebral ischemia, such as the middle cerebral artery occlusion (MCAO) model. The compound is administered intravenously. Cerebral blood flow, infarct size, and neurological deficits are assessed. Its efficacy in treating ischemic stroke is evaluated.
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| ADME/Pharmacokinetics |
Cinepazide is a vasodilator. Its molecular weight is 417.50 g/mol and its formula is C22H31N3O5. It is soluble in DMSO at 10 mM. For research use, it is typically dissolved in DMSO for in vitro studies. Its half-life and metabolic profile have been characterized.
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| Toxicity/Toxicokinetics |
Cinepazide is generally well tolerated. Side effects may include headache, flushing, and hypotension due to its vasodilatory effects. It should be used with caution in patients with hypotension.
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| References | |
| Additional Infomation |
Cinepazide is an olefin compound whose function is related to cinnamic acid. Cinepazide has been used in research trials for the treatment of ischemic stroke.
Cinepazide is a vasodilator used for the research of cerebrovascular diseases, including ischemic stroke and brain infarction. It acts as a weak calcium channel blocker and potentiates purinergic P1 receptor-mediated relaxation. The compound is not approved for clinical use in all countries but is available as a therapeutic agent in some regions. |
| Molecular Formula |
C22H31N3O5
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|---|---|
| Molecular Weight |
417.50
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| Exact Mass |
417.226
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| CAS # |
23887-46-9
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| Related CAS # |
Cinepazide Maleate;26328-04-1
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| PubChem CID |
5282459
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
637.8±55.0 °C at 760 mmHg
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| Melting Point |
170 - 175ºC
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| Flash Point |
339.5±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.575
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| LogP |
1.64
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
586
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N1CCN(CC(N2CCCC2)=O)CC1)/C=C/C3=CC(OC)=C(OC)C(OC)=C3
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| InChi Key |
RCUDFXMNPQNBDU-VOTSOKGWSA-N
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| InChi Code |
InChI=1S/C22H31N3O5/c1-28-18-14-17(15-19(29-2)22(18)30-3)6-7-20(26)25-12-10-23(11-13-25)16-21(27)24-8-4-5-9-24/h6-7,14-15H,4-5,8-13,16H2,1-3H3/b7-6+
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| Chemical Name |
(E)-1-[4-(2-oxo-2-pyrrolidin-1-ylethyl)piperazin-1-yl]-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
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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 |
| 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 | 2.3952 mL | 11.9760 mL | 23.9521 mL | |
| 5 mM | 0.4790 mL | 2.3952 mL | 4.7904 mL | |
| 10 mM | 0.2395 mL | 1.1976 mL | 2.3952 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.
Link: https://clinicaltrials.gov/ct2/show/NCT01851759
Conditions:Ischemic StrokeProducts are for research use only; We do not sell to patients
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