| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Lenperone targets dopamine D2 receptors, consistent with its classification as a butyrophenone antipsychotic. It also has some alpha-adrenergic blocking activity. The compound's antipsychotic effects are primarily mediated through dopamine D2 receptor antagonism in the central nervous system.
|
|---|---|
| ln Vitro |
Lenperone is a butyrophenone antipsychotic with antipsychotic effects. It has some alpha-adrenergic blocking action and is antiemetic. Lenperone improves depressive symptoms. Specific IC50 or Ki values for receptor binding are not extensively detailed in standard reference sources.
|
| ln Vivo |
Lenperone has antipsychotic effects in vivo. It improves depressive symptoms. As a butyrophenone antipsychotic, it would be expected to show efficacy in animal models of psychosis and depression. Specific animal model data and dosing regimens are not extensively detailed in standard reference sources.
|
| Enzyme Assay |
Lenperone's receptor binding affinity can be assessed using radioligand binding assays with membrane preparations from cells expressing dopamine D2 receptors or alpha-adrenergic receptors. Competition binding experiments are performed with increasing concentrations of lenperone against a fixed concentration of a radiolabeled receptor-specific ligand. Ki values are calculated from competition curves.
|
| Cell Assay |
The cellular activity of lenperone is evaluated in cell-based assays measuring dopamine D2 receptor signaling. Cells expressing recombinant dopamine D2 receptors are treated with increasing concentrations of lenperone, and receptor-mediated signaling pathways (e.g., cAMP inhibition) are measured. The compound's antagonist activity is assessed by its ability to block dopamine-induced signaling.
|
| Animal Protocol |
Lenperone would be administered orally or intraperitoneally to animal models of psychosis or depression. In rodent models, behavioral tests such as the forced swim test, tail suspension test, and open field test would be performed to assess antipsychotic and antidepressant effects. Specific protocols are not extensively detailed in standard reference sources.
|
| ADME/Pharmacokinetics |
Lenperone has a molecular formula of C22H23F2NO2 and a molecular weight of 371.42. It is a butyrophenone antipsychotic. Specific pharmacokinetic parameters such as half-life, bioavailability, and plasma protein binding are not extensively detailed in standard reference sources.
|
| Toxicity/Toxicokinetics |
The toxicity profile of lenperone is consistent with that of other butyrophenone antipsychotics. Potential adverse effects may include extrapyramidal symptoms, sedation, and cardiovascular effects. Specific LD50 values and organ-specific toxicity data are not extensively detailed in standard reference sources.
|
| Additional Infomation |
Lenperone is an organic molecular entity.
Lenperone (CAS# 24678-13-5) is a butyrophenone antipsychotic. It has some alpha-adrenergic blocking action and is antiemetic. Lenperone has antipsychotic effects and improves depressive symptoms. It is also known as AHR 2277 free base. |
| Molecular Formula |
C22H23NO2F2
|
|---|---|
| Molecular Weight |
371.42032
|
| Exact Mass |
371.17
|
| CAS # |
24678-13-5
|
| Related CAS # |
Lenperone hydrochloride;24677-86-9
|
| PubChem CID |
32593
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.186g/cm3
|
| Boiling Point |
507.9ºC at 760mmHg
|
| Flash Point |
261ºC
|
| Vapour Pressure |
1.95E-10mmHg at 25°C
|
| Index of Refraction |
1.55
|
| LogP |
4.46
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
27
|
| Complexity |
489
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC1C=CC(C(C2CCN(CCCC(C3C=CC(F)=CC=3)=O)CC2)=O)=CC=1
|
| InChi Key |
WCIBOXFOUGQLFC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H23F2NO2/c23-19-7-3-16(4-8-19)21(26)2-1-13-25-14-11-18(12-15-25)22(27)17-5-9-20(24)10-6-17/h3-10,18H,1-2,11-15H2
|
| Chemical Name |
4-[4-(4-fluorobenzoyl)piperidin-1-yl]-1-(4-fluorophenyl)butan-1-one
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.6924 mL | 13.4618 mL | 26.9237 mL | |
| 5 mM | 0.5385 mL | 2.6924 mL | 5.3847 mL | |
| 10 mM | 0.2692 mL | 1.3462 mL | 2.6924 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
