| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
CGP 25454A targets the presynaptic dopamine autoreceptor, a D2-like receptor that regulates dopamine release. As an antagonist, it blocks this receptor, leading to an increase in dopamine and acetylcholine release. This mechanism makes it a valuable tool for studying the role of dopamine in brain function and disease.
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| ln Vitro |
In vitro, CGP 25454A increases the field-stimulated [3H]- and [14C]-overflow from rat striatal slices preloaded with [3H]dopamine and [14C]choline, indicating that it enhances the release of both dopamine (DA) and acetylcholine (ACh). It is a selective antagonist with a defined mechanism of action.
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| ln Vivo |
In vivo, CGP 25454A has been studied for its effects on dopamine signaling. At doses of 30-100 mg/kg, it has been shown to inhibit [3H]spiperone binding in the pituitary, a result of postsynaptic DA receptor blockade. It is used in research for major depression.
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| Enzyme Assay |
In vitro receptor binding assays for CGP 25454A are performed to measure its affinity for the dopamine autoreceptor. These assays typically involve competitive displacement of a radiolabeled ligand, such as [3H]spiperone, from receptor preparations. Its functional activity is confirmed in neurotransmitter release assays using striatal slices.
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| Cell Assay |
Cellular assays for CGP 25454A are not well-defined. As a compound that modulates neurotransmitter release, its effects can be studied in brain slice preparations, where the release of radiolabeled dopamine and acetylcholine is measured following electrical stimulation.
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| Animal Protocol |
In vivo animal studies with CGP 25454A are conducted to study its effects on the dopaminergic system. In a typical study, rats are administered the compound, and receptor binding or neurotransmitter levels are measured in brain regions such as the striatum and pituitary.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of CGP 25454A are characteristic of a small molecule. It has a molecular weight of 346.25 and a molecular formula of C15H21Cl2N3O2. Its exact PK parameters are not detailed in the provided literature. It is a hydrochloride salt.
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| Toxicity/Toxicokinetics |
The toxicological profile of CGP 25454A is not fully detailed. As a research compound, its safety is evaluated in preclinical studies. It is for research use only and is not for human therapeutic use. Standard safety precautions should be followed.
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| Additional Infomation |
CGP 25454A is a selective presynaptic dopamine autoreceptor antagonist. It is used in research for major depression and other neurological and psychiatric disorders. It induces the increase of dopamine and acetylcholine and is available for research use only.
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| Molecular Formula |
C15H21CL2N3O2
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|---|---|
| Molecular Weight |
346.252141714096
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| Exact Mass |
345.101
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| CAS # |
104391-26-6
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| PubChem CID |
9819590
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
22
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| Complexity |
378
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(CC)CCNC(=O)C1=C(C=C(C(=C1)C#N)Cl)OC.Cl
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| InChi Key |
ZETCQNUMZFZSLJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H20ClN3O2.ClH/c1-4-19(5-2)7-6-18-15(20)12-8-11(10-17)13(16)9-14(12)21-3;/h8-9H,4-7H2,1-3H3,(H,18,20);1H
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| Chemical Name |
4-chloro-5-cyano-N-[2-(diethylamino)ethyl]-2-methoxybenzamide;hydrochloride
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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) |
DMSO : ≥ 3.5 mg/mL (~10.11 mM)
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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 | 2.8881 mL | 14.4404 mL | 28.8809 mL | |
| 5 mM | 0.5776 mL | 2.8881 mL | 5.7762 mL | |
| 10 mM | 0.2888 mL | 1.4440 mL | 2.8881 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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