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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
WAY-181187 (SAX187) is a novel, potent and selective 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY-181187 exhibits a full receptor agonist profile (WAY-EC50=6.6 nM, Emax=93%) and a high affinity binding (2.2 and 4.8 nM, respectively) at the human 5-HT6 receptor. Without affecting glutamate or norepinephrine levels, acute subcutaneous (s.c.) administration of WAY-181187 (3–30 mg/kg) markedly raised extracellular GABA concentrations in the rat frontal cortex.
Targets |
5-HT6 Receptor ( Ki = 2.2 nM ); 5-HT6 Receptor ( EC50 = 6.6 nM )
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ln Vitro |
WAY-181187 (1 and 10 μM) enhances ERK1/2 activation. WAY-181187 wood increases Fyn Manhattan activity[2]. Western Blot Analysis[2] Cell line: HEK/HA-5-HT6 receptor cell concentration: 1 and 10 μM Incubation time: 5 minutes of pretreatment Results: The activation of ERK1/2 increased at both 1 and 10 μM concentrations.
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ln Vivo |
Acute administration of WAY-181187 (3-30 mg/kg, sc) significantly increased extracellular GABA concentrations without altering glutamate or nordepine levels in the FX frontal lobes. Additionally, WAY-181187 (30 mg/kg, sc) modulates but significantly reduces cortical dopamine and 5-HT levels [1]. Animal model: Adult male Sprague-Dawley rat, body weight 280–350 g[1] Dosage: 3, 10 or 30 mg/kg Administration: Acute subcutaneous administration Results: Significant increase in extracellular GABA concentration without alteration Levels of glutamate or norepinephrine.
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Cell Assay |
Cell Line: HEK/HA-5-HT6 receptor cells
Concentration: 1 and 10 μM Incubation Time: Pretreatment 5 minutes Result: Increased activation of ERK1/2 both at 1 and 10 μM concentrations. |
Animal Protocol |
Adult male Sprague-Dawley rats weighing 280–350 g
3, 10, or 30 mg/kg Acute dministered by s.c. |
References |
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Molecular Formula |
C15H13CLN4O2S2
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Molecular Weight |
380.87232
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Exact Mass |
380.02
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CAS # |
554403-49-5
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Related CAS # |
WAY-181187 oxalate; 1883548-85-3; WAY-181187 hydrochloride; 554403-08-6
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Appearance |
Powder
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SMILES |
C1=CC=C2C(=C1)C(=CN2S(=O)(=O)C3=C(N=C4N3C=CS4)Cl)CCN
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InChi Key |
RYBOXBBYCVOYNO-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C15H13ClN4O2S2/c16-13-14(19-7-8-23-15(19)18-13)24(21,22)20-9-10(5-6-17)11-3-1-2-4-12(11)20/h1-4,7-9H,5-6,17H2
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Chemical Name |
2-[1-(6-chloroimidazo[2,1-b][1,3]thiazol-5-yl)sulfonylindol-3-yl]ethanamine
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Synonyms |
WAY-181187; WAY 181187; WAY181187; SAX187; SAX-187; SAX187
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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: ~100 mg/mL (~262.6 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.56 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 (6.56 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (6.56 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 | 2.6256 mL | 13.1278 mL | 26.2557 mL | |
5 mM | 0.5251 mL | 2.6256 mL | 5.2511 mL | |
10 mM | 0.2626 mL | 1.3128 mL | 2.6256 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.