| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
5-HT2C Receptor (Ki = 4 nM); 5-HT2C Receptor (EC50 = 12 nM)
(Rac)-WAY-161503 targets the serotonin 5-HT2C receptor as a high-affinity agonist. It has a Ki of 4 nM and an EC50 of 12 nM. It displays higher affinity for 5-HT2C than for 5-HT2A and 5-HT2B receptors. It also has Ki values of 50 nM for rat 5-HT2C and 100 nM for human 5-HT2C. |
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| ln Vitro |
(Rac)-WAY-161503 is a potent and selective 5-HT2C receptor agonist with a Ki of 4 nM and an EC50 of 12 nM. It displays higher affinity for 5-HT2C than for 5-HT2A and 5-HT2B receptors. Its activity makes it a valuable tool for studying 5-HT2C receptor function and its role in appetite regulation and mood.
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| ln Vivo |
(Rac)-WAY-161503 (3-30 mg/kg; intraperitoneal injection; male C57BL/6J mice) reduces locomotor activity in a dose-dependent manner; the 5-HT2C/2B antagonist SER-082 blocks this effect[1].
(Rac)-WAY-161503 has anti-obesity and antidepressant effects. As a selective 5-HT2C agonist, it can be administered to animal models of obesity and depression. Its ability to activate 5-HT2C receptors translates to in vivo efficacy in reducing food intake and body weight, as well as antidepressant-like effects. |
| Enzyme Assay |
In vitro receptor binding assays for (Rac)-WAY-161503 involve measuring its affinity for 5-HT2C, 5-HT2A, and 5-HT2B receptors. Radioligand binding studies using ³H-mesulergine or other 5-HT2 ligands are performed on membranes from cells expressing the receptors. Ki values of 4 nM for 5-HT2C are determined. Functional assays measure its ability to activate 5-HT2C-mediated signaling pathways.
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| Cell Assay |
For in vitro cell-based assays, cells expressing 5-HT2C receptors are cultured and treated with (Rac)-WAY-161503 at various concentrations. Receptor activation is measured by quantifying intracellular calcium mobilization using fluorescent calcium indicators. Cell viability is assessed by standard assays. Its selectivity is confirmed by testing against cells expressing 5-HT2A and 5-HT2B receptors.
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| Animal Protocol |
Animal/Disease Models: Male C57BL/6J mice Hallucinogen 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) [1]
Doses: 3mg/kg, 10mg/kg, 30. mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Locomotor activity was diminished in a dose-dependent manner, and this effect could be blocked by the 5-HT2C/2B antagonist SER-082. WAY 161,503 was dissolved in saline containing 2.5% Tween 80. DOI and WAY 161,503 were administered intraperitoneally at a volume of 5 ml/kg body weight. [1] Animals were placed in the mouse BPM chambers 15 min after treatment with DOI, or 10 min after treatment with WAY 161,503. In experiment 1, mice (n=10–11, 63 total) were treated with vehicle, 0.625, 1.25, 2.5, 5.0, or 10 mg/kg DOI. In experiment 2, the 5-HT2A cohort consisted of 14 WT and 13 KO male mice, and 13 WT and 5 KO female mice. The mice were tested in a three-way crossover design with 1 week between tests. Each animal received vehicle as well as 1.0 and 10 mg/kg DOI in a semi-randomized, counterbalanced order, to complete a within-subject design. In experiment 3, mice (n=10, 60 total) were treated with SER-082 (vehicle or 1.0 mg/kg) 15 min before administration of DOI (vehicle, 1.0, or 10 mg/kg). In experiment 4, mice (n=8–10, 38 total) were treated with vehicle or 3, 10, or 30 mg/kg WAY 161,503. In experiment 5, mice (n=8–10, 38 total) were treated with SER-082 (vehicle or 1.0 mg/kg) 20 min before administration of WAY 161,503 (vehicle, 1, or 10 mg/kg). In experiment 6, a new 5-HT2A cohort consisted of 8 WT and 10 KO male mice, and 9 WT and 11 KO female mice. WT and KO mice were injected with either vehicle or WAY 161,503 (10 mg/kg) in a between subjects design.[1] In vivo animal studies with (Rac)-WAY-161503 are conducted in models of obesity and depression. The compound is administered orally or intraperitoneally to rodents. Food intake, body weight, and metabolic parameters are monitored. Antidepressant-like effects are assessed using behavioral tests such as the forced swim test or tail suspension test. |
| ADME/Pharmacokinetics |
(Rac)-WAY-161503 (CAS: 75704-24-4) has a molecular weight of 284.74 g/mol and a molecular formula of C12H16ClN3O. Appearance: solid powder. Purity: ≥98%. Solubility: DMSO. Storage: -20°C. The compound is a potent and selective 5-HT2C receptor agonist.
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| Toxicity/Toxicokinetics |
(Rac)-WAY-161503 is a research compound and is not approved for human therapeutic use. In preclinical studies, it has shown a manageable safety profile. As a 5-HT2C agonist, it may have effects on appetite, mood, and metabolism. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
8,9-Dichloro-1,2,3,4,4a,6-hexahydropyrazino[1,2-a]quinoxaline-5-one is an amino acid amide.
(Rac)-WAY-161503 is a potent, selective, high-affinity agonist of the 5-HT2C receptor with a Ki of 4 nM and an EC50 of 12 nM. It exhibits anti-obesity and antidepressant effects. It is not FDA-approved and is intended for research use only. |
| Molecular Formula |
C₁₁H₁₁CL₂N₃O
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| Molecular Weight |
272.13
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| Exact Mass |
307.005
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| Elemental Analysis |
C, 48.55; H, 4.07; Cl, 26.05; N, 15.44; O, 5.88
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| CAS # |
75704-24-4
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| Related CAS # |
(Rac)-WAY-161503 hydrochloride;276695-22-8
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| PubChem CID |
3906894
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| Appearance |
Off-white to light yellow solid powder
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| Boiling Point |
529ºC at 760 mmHg
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| Flash Point |
273.7ºC
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| LogP |
3.057
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
17
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| Complexity |
328
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YPNWSZJDAKOUAW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H11Cl2N3O.ClH/c12-6-3-8-9(4-7(6)13)16-2-1-14-5-10(16)11(17)15-8;/h3-4,10,14H,1-2,5H2,(H,15,17);1H
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| Chemical Name |
8,9-dichloro-1,2,3,4,4a,6-hexahydropyrazino[1,2-a]quinoxalin-5-one;hydrochloride
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| Synonyms |
(Rac)WAY161503; WAY 161503 hydrochloride; 276695-22-8; 75704-24-4; 8,9-DICHLORO-2,3,4,4A-TETRAHYDRO-1H-PYRAZINO[1,2-A]QUINOXALIN-5(6H)-ONE HYDROCHLORIDE; (Rac)-WAY-161503 (hydrochloride); 8,9-dichloro-1,2,3,4,4a,6-hexahydropyrazino[1,2-a]quinoxalin-5-one;hydrochloride; 8,9-dichloro-2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5(6H)-one hydrochloride salt; WAY161503 hydrochloride; (Rac) WAY 161503
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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 (~367.47 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.19 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 (9.19 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 (9.19 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 | 3.6747 mL | 18.3736 mL | 36.7471 mL | |
| 5 mM | 0.7349 mL | 3.6747 mL | 7.3494 mL | |
| 10 mM | 0.3675 mL | 1.8374 mL | 3.6747 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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