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5mg |
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10mg |
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50mg |
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100mg |
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WAY-100635 (WAY100635) is a selective antagonist of serotonin 5-HT1A receptor with neuroprotective activity. It inhibits 5-HT1A receptor with IC50 of 0.95 nM.
ln Vitro |
In HEK 293 cells that consistently express dopamine D2L or D4.4 receptors, the functional characteristics and binding affinities of WAY-100635 are assessed[1]. WAY-100635 exhibits binding affinities at D2L, D3, and D4. 2 receptors of 940, 370, and 16 nM, respectively. The Kd of [3H] WAY-100635 at D4.2 receptors is 2.4 nM, as shown by saturation analyses. WAY-100635 has an EC50 of 9.7 nM, making it a strong agonist in HEK-D4.4 cells. WAY-100635 has a strong 3.3 nM affinity for the D4.4 receptor [1].
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ln Vivo |
Treatment with WAY-100635 (1 mg/kg; subcutaneous injection; male Sprague-Dawley rats) eliminates the reduction in abstinence signs severity brought on by administration of Rhodiola rosea in nicotine-dependent rats[2].
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Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (220-240 g)[2]
Doses: 1 mg/kg Route of Administration: subcutaneous (sc) injection (pharmacokinetic/PK study) Experimental Results: decreased total abstinence score, increased immobility time and the burying behavior was increased. |
References |
[1]. Chemel BR, et al. WAY-100635 is a potent dopamine D4 receptor agonist. Psychopharmacology (Berl). 2006 Oct;188(2):244-51.
[2]. Mannucci C, et al. Serotonin involvement in Rhodiola rosea attenuation of nicotine withdrawal signs in rats. Phytomedicine. 2012 Sep 15;19(12):1117-24. [3]. Al Hussainy R, et al. Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinatedanalogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptor. J Med Chem. 2011 May 26;54(10):3480-91. |
Molecular Formula |
C25H34N4O2
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Molecular Weight |
422.573
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Exact Mass |
422.2682
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CAS # |
162760-96-5
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Related CAS # |
WAY-100635 maleate;1092679-51-0
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SMILES |
O=C(N(C1=NC=CC=C1)CCN2CCN(CC2)C3=CC=CC=C3OC)C4CCCCC4
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Synonyms |
WAY 100635 WAY100635 WAY-100635
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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 : ~66.67 mg/mL (~157.78 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.92 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 (5.92 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 (5.92 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 | 2.3665 mL | 11.8324 mL | 23.6647 mL | |
5 mM | 0.4733 mL | 2.3665 mL | 4.7329 mL | |
10 mM | 0.2366 mL | 1.1832 mL | 2.3665 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.