SK609 hydrochloride
Based on 1 Customer Validation
SK609 hydrochloride is a dopamine D3 receptor (D3R) selective agonist with an EC50 of 1109 nM. SK609 hydrochloride has the potential for parkinson research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.83%
- CAS. Nr.: 1092797-77-7
- Formel: C10H15Cl2N
- Molecular Weight:220.14
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biologische Aktivität
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Dopamine D3 receptor 1109 nM (EC50) |
In a Competitive inhibition affinity assay by SK609 hydrochloride to D3R, SK609 exhibits an EC50 value of 1109 nM at D3R[1].
SK609 hydrochloride activates Gi/o proteins and downstream ERK1/2 signaling but have no effects on D2R/ERK1/2. SK609 exhibits EC50 values of 1.1 μM, 50.2 nM, and 14.4 μM for [35S]GTPγS binding, ERK1/2 phosphorylation, and β-Arrestin recruitment respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SK609 hydrochloride shows the maximum tolerated dose of SK609 hydrochloride is 30mg/kg in safety toxicology study within the no-observed-adverse-effect level of SK609 hydrochloride[2].
In the cynomolgus macaques PK study, oral administration of SK609 hydrochloride (0.5, 2 and 4 mg/kg) is associated with mean Cmax values of 13.7, 69.3 and 218 ng/ml respectively, occurring at (Tmax) 4.1, 6.4 and 5.0 hours following administration and with corresponding AUC(0-t) values of 171, 904 and 2938 h.ng/ml respectively[3].Following intravenous administration (2 mg/kg), SK609 hydrochloride has a mean terminal half-life of 7.9 h in plasma. SK609 hydrochloride (i.p.; 2, 4, 6, 8, 10, 20 mg/kg) significantly improves the performance of the impaired paw and also normalized the bilateral asymmetry associated with the hemiparkinson rat[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1092797-77-7
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Appearance Solid
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Molecular Weight 220.14
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Formel C10H15Cl2N
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Color Off-white to light brown
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SMILES
CC(CCC1=CC=CC=C1Cl)N.Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (567.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 100 mg/mL (454.26 mM; Need ultrasonic)
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
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- Español - ES (393 KB)
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- Italian - IT (393 KB)
- Korean - KR (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Wei Xu, et al. Functional Characterization of a Novel Series of Biased Signaling Dopamine D3 Receptor Agonists. ACS Chem Neurosci. 2017 Mar 15;8(3):486-500. [Content Brief]
[2]. Jay S Schneider, et al. A novel dopamine D3R agonist SK609 with norepinephrine transporter inhibition promotes improvement in cognitive task performance in rodent and non-human primate models of Parkinson's disease. Exp Neurol. 2021 Jan;335:113514 [Content Brief]
[3]. Sherise L Simms, et al. In vivo characterization of a novel dopamine D3 receptor agonist to treat motor symptoms of Parkinson's disease . Neuropharmacology. 2016 Jan;100:106-15. [Content Brief]
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 and light). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 4.5426 mL | 22.7128 mL | 45.4256 mL | 113.5641 mL |
| 5 mM | 0.9085 mL | 4.5426 mL | 9.0851 mL | 22.7128 mL | |
| 10 mM | 0.4543 mL | 2.2713 mL | 4.5426 mL | 11.3564 mL | |
| 15 mM | 0.3028 mL | 1.5142 mL | 3.0284 mL | 7.5709 mL | |
| 20 mM | 0.2271 mL | 1.1356 mL | 2.2713 mL | 5.6782 mL | |
| 25 mM | 0.1817 mL | 0.9085 mL | 1.8170 mL | 4.5426 mL | |
| 30 mM | 0.1514 mL | 0.7571 mL | 1.5142 mL | 3.7855 mL | |
| 40 mM | 0.1136 mL | 0.5678 mL | 1.1356 mL | 2.8391 mL | |
| 50 mM | 0.0909 mL | 0.4543 mL | 0.9085 mL | 2.2713 mL | |
| 60 mM | 0.0757 mL | 0.3785 mL | 0.7571 mL | 1.8927 mL | |
| 80 mM | 0.0568 mL | 0.2839 mL | 0.5678 mL | 1.4196 mL | |
| 100 mM | 0.0454 mL | 0.2271 mL | 0.4543 mL | 1.1356 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
SK609 hydrochloride Related Classifications
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