| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
L-741,742 hydrochloride targets the human dopamine D4 receptor (hD4), a G protein-coupled receptor that is involved in the regulation of cognition, attention, and reward. It acts as a potent and selective antagonist, with a Ki of 3.5 nM for the D4 receptor. The compound shows >200-fold selectivity over D2 and D3 receptors. This high selectivity makes L-741,742 hydrochloride a valuable tool for studying D4 receptor function.
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| ln Vitro |
In vitro, L-741,742 hydrochloride selectively binds to the human D4 receptor with high affinity (Ki = 3.5 nM) and shows >200-fold selectivity over D2 and D3 receptors. The compound inhibits D4 receptor-mediated signaling, as measured by cAMP accumulation or other downstream readouts. L-741,742 hydrochloride selectively inhibits the growth of glioblastoma neural stem cells (GNS) and promotes the differentiation of normal neural stem cells.
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| ln Vivo |
In vivo, L-741,742 hydrochloride has been studied in animal models of neurological disorders, particularly schizophrenia. The compound is orally bioactive and has good brain penetration. L-741,742 hydrochloride modulates D4 receptor-mediated behaviors in rodents, such as locomotor activity and prepulse inhibition. However, specific in vivo efficacy data are limited in the available literature.
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| Enzyme Assay |
The non-cellular assay for L-741,742 hydrochloride involves measuring its binding affinity for the D4 receptor using radioligand binding assays. Membrane preparations from cells expressing the human D4 receptor are incubated with a radiolabeled D4 receptor ligand (such as [³H]-spiperone or [³H]-YM-09151-2) and varying concentrations of L-741,742 hydrochloride. The inhibition of radioligand binding is measured, and the Ki is determined from competition curves.
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| Cell Assay |
The cellular assay for L-741,742 hydrochloride involves treating cells expressing the human D4 receptor with the compound and measuring its effects on receptor-mediated signaling. Cells are pre-incubated with L-741,742 hydrochloride, and the inhibition of agonist-induced cAMP accumulation is measured using a competitive immunoassay. The IC50 is determined from concentration-response curves. The effects on neural stem cell proliferation and differentiation are assessed in cell culture models.
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| Animal Protocol |
In the in vivo efficacy study, L-741,742 hydrochloride is administered orally to rodent models of schizophrenia or other neurological disorders. Behavioral assessments, such as locomotor activity, prepulse inhibition, and novel object recognition, are performed to evaluate the compound's effects on D4 receptor-mediated behaviors. Brain penetration is confirmed by measuring compound concentrations in brain tissue.
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| ADME/Pharmacokinetics |
L-741,742 hydrochloride has a molecular weight of 417.33 and a molecular formula of C₂₃H₂₆Cl₂N₂O. The compound is orally active and has good brain penetration. It should be stored as a powder at -20°C, protected from light and moisture. The compound is soluble in DMSO and other organic solvents. L-741,742 hydrochloride should be handled with appropriate laboratory safety precautions.
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| Toxicity/Toxicokinetics |
The toxicological profile of L-741,742 hydrochloride has not been extensively characterized in the published literature. As a D4 receptor antagonist, it may have effects on cognition, attention, and reward. Comprehensive toxicology data are limited, and L-741,742 hydrochloride is not approved for clinical use. The compound should be handled with appropriate laboratory safety precautions.
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| References | |
| Additional Infomation |
L-741,742 hydrochloride is a selective and high-affinity antagonist of the human dopamine D4 receptor that has been used as a research tool to study D4 receptor function. Its good brain penetration and oral bioavailability make it useful for in vivo studies of neurological disorders, particularly schizophrenia. The compound also selectively inhibits glioblastoma neural stem cell growth and promotes normal neural stem cell differentiation. L-741,742 hydrochloride is not approved for clinical use and is strictly a research compound.
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| Molecular Formula |
C23H25N2OCL.HCL
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|---|---|
| Molecular Weight |
417.37134
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| Exact Mass |
416.142
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| CAS # |
874882-93-6
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| Related CAS # |
874882-93-6 (HCl);156337-32-5;
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| PubChem CID |
24744861
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
6.465
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
440
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.C1C=CC(CCN2CCC(C3=NOC(C4C=CC(Cl)=CC=4)=C3C)CC2)=CC=1
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| InChi Key |
HZRPUQURUAXOHB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H25ClN2O.ClH/c1-17-22(25-27-23(17)20-7-9-21(24)10-8-20)19-12-15-26(16-13-19)14-11-18-5-3-2-4-6-18;/h2-10,19H,11-16H2,1H3;1H
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| Chemical Name |
5-(4-chlorophenyl)-4-methyl-3-[1-(2-phenylethyl)piperidin-4-yl]-1,2-oxazole;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 |
| 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 | 2.3960 mL | 11.9798 mL | 23.9596 mL | |
| 5 mM | 0.4792 mL | 2.3960 mL | 4.7919 mL | |
| 10 mM | 0.2396 mL | 1.1980 mL | 2.3960 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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