L-741626
Based on 2 publication(s) in Google Scholar
L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively.
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- Pureté: 99.0%
- CAS No.: 81226-60-0
- Formule: C20H21ClN2O
- Masse moléculaire:340.85
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) L-741626
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Activité biologique
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D4 Receptor |
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
4.46 nM
Compound: 1, L-741626
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Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
Antagonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
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[PMID: 17095222] |
| CHO | EC50 |
90.4 nM
Compound: 1, L-741626
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Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
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[PMID: 17095222] |
Intrinsic activities in a functional assay using inhibition of quinpirole stimulation of mitogenesis in human dopamine D2 or D3 receptors transfected into Chinese hamster ovary (CHO) cells, L-741626 is prepared by literature methods (Ki (D2)=11.2 nM) and displays a D3/D2 and D4/D2 selectivity ratio of 15-fold and 136-fold, respectively. In the functional assay L-741626 is a potent antagonist (EC50 (D2)=4.46 nM) with some D2 selectivity (EC50 (D3)=90.4 nM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Coadministrating Cocaine with the D2 antagonist L-741626 (3 mg/kg; i.p.; 15 min before Cocaine) for 5 days reduces the Cocaine-induced increase in microglial TNF-α production in adult mice[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 81226-60-0
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Appearance Solid
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Masse moléculaire 340.85
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Formule C20H21ClN2O
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Color White to off-white
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SMILES
OC1(C2=CC=C(Cl)C=C2)CCN(CC3=CNC4=C3C=CC=C4)CC1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
2025 Nov 29:244:117576. PMID: 41319924 -
Biol Direct
L-741626 inhibits hepatocellular carcinoma progression by targeting Ref-1 to suppress MAPK/ERK signalling pathway activity. [Abstract]2025 Apr 16;20(1):54. PMID: 40241114
Solvant et solubilité
DMSO : 50 mg/mL (146.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Lewitus GM, et al. Microglial TNF-α Suppresses Cocaine-Induced Plasticity and Behavioral Sensitization. Neuron. 2016 May 4;90(3):483-91. [Content Brief]
[2]. Grundt P, et al. Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR. Bioorg Med Chem Lett. 2007 Feb 1;17(3):745-9. [Content Brief]
[3]. Koffarnus MN, et al. The discriminative stimulus effects of dopamine D2- and D3-preferring agonists in rats. Psychopharmacology (Berl). 2009 Apr;203(2):317-27. [Content Brief]
[4]. Kulagowski JJ, et al. 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. J Med Chem. 1996 May 10;39(10):1941-2. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.9338 mL | 14.6692 mL | 29.3384 mL | 73.3460 mL |
| 5 mM | 0.5868 mL | 2.9338 mL | 5.8677 mL | 14.6692 mL | |
| 10 mM | 0.2934 mL | 1.4669 mL | 2.9338 mL | 7.3346 mL | |
| 15 mM | 0.1956 mL | 0.9779 mL | 1.9559 mL | 4.8897 mL | |
| 20 mM | 0.1467 mL | 0.7335 mL | 1.4669 mL | 3.6673 mL | |
| 25 mM | 0.1174 mL | 0.5868 mL | 1.1735 mL | 2.9338 mL | |
| 30 mM | 0.0978 mL | 0.4890 mL | 0.9779 mL | 2.4449 mL | |
| 40 mM | 0.0733 mL | 0.3667 mL | 0.7335 mL | 1.8337 mL | |
| 50 mM | 0.0587 mL | 0.2934 mL | 0.5868 mL | 1.4669 mL | |
| 60 mM | 0.0489 mL | 0.2445 mL | 0.4890 mL | 1.2224 mL | |
| 80 mM | 0.0367 mL | 0.1834 mL | 0.3667 mL | 0.9168 mL | |
| 100 mM | 0.0293 mL | 0.1467 mL | 0.2934 mL | 0.7335 mL |
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