RPI-GLYT2-82
Based on 1 Customer Validation
RPI-GLYT2-82 is a reversible, blood-brain barrier-permeable allosteric inhibitor of GlyT2 with an IC50 value of 554 nM. RPI-GLYT2-82 also exhibits inhibitory activity against 5-HT2AR and SERT, with IC50 values of 1.9 μM and 4.7 μM, respectively. RPI-GLYT2-82 inhibits pain signals and alleviates allodynia, shows no target-related side effects at the maximum analgesic dose, and has no addictive potential. RPI-GLYT2-82 can be used for the research of neuropathic pain.
For research use only. We do not sell to patients.
- Purity : 99.12%
- Formula: C24H30ClN3O3
- Molecular Weight:443.97
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
GlyT2 544 nM (IC50) |
5-HT2A Receptor 1.9 μM (IC50) |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, female, 6 weeks old at arrival); C57BL/6J (male, 8-12 weeks old, conditioned place preference model)[1]
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Dosage:50 mg/kg; 100 mg/kg; 250 mg/kg; 150 mg/kg (CPP)
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Administration:i.p.; single dose
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Result:Produced dose-dependent anti-hyperalgesia effect without on-target side effects at therapeutic doses (50 mg/kg, 100 mg/kg) and showed no addiction liability up to 150 mg/kg
Chemical Information
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Appearance Solid
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Molecular Weight 443.97
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Formula C24H30ClN3O3
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Color Off-white to light yellow
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SMILES
O=C(C1=CC2=C(N(C(C3=CC=CC=C3)=O)CC2)C=C1)NCC4(N(C)C)CCOCC4.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 25 mg/mL (56.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.2524 mL | 11.2620 mL | 22.5240 mL | 56.3101 mL |
| 5 mM | 0.4505 mL | 2.2524 mL | 4.5048 mL | 11.2620 mL | |
| 10 mM | 0.2252 mL | 1.1262 mL | 2.2524 mL | 5.6310 mL | |
| 15 mM | 0.1502 mL | 0.7508 mL | 1.5016 mL | 3.7540 mL | |
| 20 mM | 0.1126 mL | 0.5631 mL | 1.1262 mL | 2.8155 mL | |
| 25 mM | 0.0901 mL | 0.4505 mL | 0.9010 mL | 2.2524 mL | |
| 30 mM | 0.0751 mL | 0.3754 mL | 0.7508 mL | 1.8770 mL | |
| 40 mM | 0.0563 mL | 0.2816 mL | 0.5631 mL | 1.4078 mL | |
| 50 mM | 0.0450 mL | 0.2252 mL | 0.4505 mL | 1.1262 mL |
RPI-GLYT2-82 Related Classifications
HY-181977 Related Classifications
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