| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
The D3/D2 and D4/D2 selectivity ratios are 15 times and 136 times, respectively, according to intrinsic activity in functional assays that use the inhibition of quinpirole-stimulated mitosis of human dopamine D2 or D3 receptors transfected into Chinese Hamster Ovary (CHO) cells, L-741626, prepared by literature methods (Ki (D2) = 11.2 nM). L-741626 is a strong antagonist in functional experiments (EC50 (D2)=4.46 nM) with a moderate degree of D2 selectivity (EC50 (D3)=90.4 nM) [2].
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| ln Vivo |
In male Sprague Dawley rats trained on pramipexole, L-741626 (1.0 mg/kg; ih) successfully moves the pramipexole dose-response curve to the right [3]. Adult mice's increased production of TNF-α in microglia was decreased when cocaine and the D2 antagonist L-741626 (3 mg/kg; i.p.; 15 min before cocaine) were given together for 5 days [4].
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| References |
[1]. Lewitus GM, et al. Microglial TNF-α Suppresses Cocaine-Induced Plasticity and Behavioral Sensitization. Neuron. 2016 May 4;90(3):483-91.
[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. [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. [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. |
| Additional Infomation |
4-(4-chlorophenyl)-1-(1H-indol-3-ylmethyl)-4-piperidinol is a member of piperidines.
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| Molecular Formula |
C20H21CLN2O
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|---|---|
| Molecular Weight |
340.85
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| Exact Mass |
340.134
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| CAS # |
81226-60-0
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| PubChem CID |
133633
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.311g/cm3
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| Boiling Point |
548.8ºC at 760 mmHg
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| Flash Point |
285.7ºC
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| Index of Refraction |
1.686
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| LogP |
4.242
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
416
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC(C2(CCN(CC3C4C(=CC=CC=4)NC=3)CC2)O)=CC=1
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| InChi Key |
LLBLNMUONVVVPG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H21ClN2O/c21-17-7-5-16(6-8-17)20(24)9-11-23(12-10-20)14-15-13-22-19-4-2-1-3-18(15)19/h1-8,13,22,24H,9-12,14H2
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| Chemical Name |
4-(4-chlorophenyl)-1-(1H-indol-3-ylmethyl)piperidin-4-ol
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| Synonyms |
L741,626; L 741,626; L-741,626
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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) |
DMSO : ~50 mg/mL (~146.69 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.33 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9338 mL | 14.6692 mL | 29.3384 mL | |
| 5 mM | 0.5868 mL | 2.9338 mL | 5.8677 mL | |
| 10 mM | 0.2934 mL | 1.4669 mL | 2.9338 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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