| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vivo |
JNJ-37822681 (0.0025-40 mg/kg; ih; once) is efficacious in animal models of psychosis and inhibits D2 receptors in the rat brain at a reasonably low dose (ED50 = 0.39 mg/kg) [2]. Inducing little prolactin release at the lowest dose necessary for central D2 receptor inhibition is JNJ-37822681 (0.01-2.5 mg/kg; ih; once) [2].
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| Animal Protocol |
Animal/Disease Models: Female SD (SD (Sprague-Dawley)) rats, apomorphine-induced, d-amphetamine-induced or phencyclidine-induced [2]
Doses: 0.0025-40 mg/kg Route of Administration: subcutaneous injection; 20mg/kg . Experimental Results: Inhibition of excessive movement caused by D-amphetamine, ED50 value is 1.0 mg/kg. Inhibits apomorphine-induced stereotypy with an ED50 value of 0.19 mg/kg. Inhibits phencyclidine-induced hypermotility with an ED50 value of 4.7 mg/kg. Animal/Disease Models: Female SD (SD (Sprague-Dawley)) rat [2] Doses: 0.01, 0.02, 0.04, 0.08, 0.16, 0.31, 0.63, 1.25 and 2.5 mg/kg Route of Administration: subcutaneous injection; Experimental Results: Increased lactation in a dose-dependent manner hormone release. |
| References |
[1]. Langlois X, et, al. Pharmacology of JNJ-37822681, a specific and fast-dissociating D2 antagonist for the treatment of schizophrenia. J Pharmacol Exp Ther. 2012 Jul;342(1):91-105.
[2]. de Waal EJ, et, al. Differential responses to JNJ-37822681, a specific and fast dissociating dopamine D2 receptor antagonist, in cynomolgus monkey and Sprague-Dawley rat general toxicology studies: clinical observations, prolactin levels, mammary histopat |
| Molecular Formula |
C17H19CL2F5N4
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|---|---|
| Molecular Weight |
445.2576
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| Exact Mass |
444.09
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| CAS # |
2108806-02-4
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| Related CAS # |
935776-74-2;2108806-02-4 (2HCl);
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| PubChem CID |
91826482
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
441
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UOLHGUUKFNZTNS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17F5N4.2ClH/c18-13-2-1-11(9-14(13)19)10-26-7-5-12(6-8-26)23-16-4-3-15(24-25-16)17(20,21)22;;/h1-4,9,12H,5-8,10H2,(H,23,25);2*1H
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| Chemical Name |
N-[1-[(3,4-difluorophenyl)methyl]piperidin-4-yl]-6-(trifluoromethyl)pyridazin-3-amine;dihydrochloride
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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 : ~33.33 mg/mL (~74.86 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.61 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 (5.61 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 (5.61 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 | 2.2459 mL | 11.2294 mL | 22.4588 mL | |
| 5 mM | 0.4492 mL | 2.2459 mL | 4.4918 mL | |
| 10 mM | 0.2246 mL | 1.1229 mL | 2.2459 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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