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(Rac)-WAY-161503

Alias: (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
Cat No.:V40037 Purity: ≥98%
(Rac)-WAY-161503 is a potent, selective, high-affinity 5-HT2C receptor agonist (activator) with Ki of 4 nM and EC50 of 12 nM.
(Rac)-WAY-161503
(Rac)-WAY-161503 Chemical Structure CAS No.: 75704-24-4
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
Other Sizes

Other Forms of (Rac)-WAY-161503:

  • (Rac)-WAY-161503 hydrochloride
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
(Rac)-WAY-161503 is a potent, selective, high-affinity 5-HT2C receptor agonist (activator) with Ki of 4 nM and EC50 of 12 nM. (Rac)-WAY-161503 has higher affinity for HT2C than 5-HT2A and 5-HT2B receptors respectively. (Rac)-WAY-161503 has anti-obesity and antidepressant properties.
Biological Activity I Assay Protocols (From Reference)
Targets
5-HT2C Receptor (Ki = 4 nM); 5-HT2C Receptor (EC50 = 12 nM)
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].
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]
References

[1]. 5-HT(2A) and 5-HT(2C) receptors exert opposing effects on locomotor activity in mice. Neuropsychopharmacology. 2009 Jul;34(8):1958-67.

[2]. Synthesis and 5-hydroxytryptamine (5-HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines. Bioorg Med Chem Lett. 2000 Sep 4;10(17):1991-4.

Additional Infomation
8,9-dichloro-1,2,3,4,4a,6-hexahydropyrazino[1,2-a]quinoxalin-5-one is an amino acid amide.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C₁₁H₁₁CL₂N₃O
Molecular Weight
272.13
Exact Mass
307.005
Elemental Analysis
C, 48.55; H, 4.07; Cl, 26.05; N, 15.44; O, 5.88
CAS #
75704-24-4
Related CAS #
(Rac)-WAY-161503 hydrochloride;276695-22-8
PubChem CID
3906894
Appearance
Off-white to light yellow solid powder
Boiling Point
529ºC at 760 mmHg
Flash Point
273.7ºC
LogP
3.057
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
0
Heavy Atom Count
17
Complexity
328
Defined Atom Stereocenter Count
0
InChi Key
YPNWSZJDAKOUAW-UHFFFAOYSA-N
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
Chemical Name
8,9-dichloro-1,2,3,4,4a,6-hexahydropyrazino[1,2-a]quinoxalin-5-one;hydrochloride
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
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~367.47 mM)
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.

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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.
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 corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
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.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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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