Synonym
SK-609; SK 609; SK609
IUPAC/Chemical Name
4-(2-Chlorophenyl)butan-2-amine hydrochloride
InChi Key
JPYONMJJWKTSBP-UHFFFAOYSA-N
InChi Code
InChI=1S/C10H14ClN/c1-8(12)6-7-9-4-2-3-5-10(9)11/h2-5,8H,6-7,12H2,1H3
SMILES Code
CC(CCC1=CC=CC=C1Cl)N
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
Biological target:
SK609 is a dopamine D3 receptor (D3R) selective agonist with a bias towards the G-protein-dependent pathway and an EC50 value of 113.9 nM for activation of ERK1/2 phosphorylation. It does not induce desensitization of D3R.
In vivo activity:
SK609 has the potential to treat sustained attention deficits without affecting dopamine transporter activity, unlike amphetamines and methylphenidate. In naïve rats, systemic SK609 dosing led to a 300% rise in norepinephrine and a 160% increase in dopamine. Notably, cognitive improvement was more pronounced in low-performing animals, and doses associated with this enhancement did not elevate spontaneous locomotor activity, indicating potential absence of side effects related to dopamine transporter activity.
Reference: Neuropharmacology. 2019 Apr;148:178-188. https://pubmed.ncbi.nlm.nih.gov/30633928/
Preparing Stock Solutions
The following data is based on the
product
molecular weight
183.68
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Marshall CA, Brodnik ZD, Mortensen OV, Reith MEA, Shumsky JS, Waterhouse BD, España RA, Kortagere S. Selective activation of Dopamine D3 receptors and norepinephrine transporter blockade enhances sustained attention. Neuropharmacology. 2019 Apr;148:178-188. doi: 10.1016/j.neuropharm.2019.01.003. Epub 2019 Jan 8. PMID: 30633928; PMCID: PMC6424628.
2. Simms SL, Huettner DP, Kortagere S. In vivo characterization of a novel dopamine D3 receptor agonist to treat motor symptoms of Parkinson's disease. Neuropharmacology. 2016 Jan;100:106-15. doi: 10.1016/j.neuropharm.2015.04.004. Epub 2015 Apr 18. PMID: 25896768.
In vivo protocol:
1. Marshall CA, Brodnik ZD, Mortensen OV, Reith MEA, Shumsky JS, Waterhouse BD, España RA, Kortagere S. Selective activation of Dopamine D3 receptors and norepinephrine transporter blockade enhances sustained attention. Neuropharmacology. 2019 Apr;148:178-188. doi: 10.1016/j.neuropharm.2019.01.003. Epub 2019 Jan 8. PMID: 30633928; PMCID: PMC6424628.
2. Simms SL, Huettner DP, Kortagere S. In vivo characterization of a novel dopamine D3 receptor agonist to treat motor symptoms of Parkinson's disease. Neuropharmacology. 2016 Jan;100:106-15. doi: 10.1016/j.neuropharm.2015.04.004. Epub 2015 Apr 18. PMID: 25896768.
1: Lei J, Tang LL, Jing R, You HJ. Antinociceptive role of the thalamic dopamine D3 receptor in descending modulation of intramuscular formalin-induced muscle nociception in a rat model of Parkinson's disease. Exp Neurol. 2024 Sep;379:114846. doi: 10.1016/j.expneurol.2024.114846. Epub 2024 Jun 13. PMID: 38879111.
2: Xu W, Bearoff F, Kortagere S. G-protein biased signaling agonists of Dopamine D3 receptor promote distinct activation patterns of ERK1/2. Pharmacol Res. 2022 May;179:106223. doi: 10.1016/j.phrs.2022.106223. Epub 2022 Apr 14. PMID: 35429668.
3: Schneider JS, Marshall CA, Keibel L, Snyder NW, Hill MP, Brotchie JM, Johnston TH, Waterhouse BD, Kortagere S. 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. doi: 10.1016/j.expneurol.2020.113514. Epub 2020 Oct 22. PMID: 33141071; PMCID: PMC7750278.
4: Marshall CA, Brodnik ZD, Mortensen OV, Reith MEA, Shumsky JS, Waterhouse BD, España RA, Kortagere S. Selective activation of Dopamine D3 receptors and norepinephrine transporter blockade enhances sustained attention. Neuropharmacology. 2019 Apr;148:178-188. doi: 10.1016/j.neuropharm.2019.01.003. Epub 2019 Jan 8. PMID: 30633928; PMCID: PMC6424628.
5: Xu W, Wang X, Tocker AM, Huang P, Reith ME, Liu-Chen LY, Smith AB 3rd, Kortagere S. Functional Characterization of a Novel Series of Biased Signaling Dopamine D3 Receptor Agonists. ACS Chem Neurosci. 2017 Mar 15;8(3):486-500. doi: 10.1021/acschemneuro.6b00221. Epub 2016 Nov 23. PMID: 27801563; PMCID: PMC5813806.
6: Simms SL, Huettner DP, Kortagere S. In vivo characterization of a novel dopamine D3 receptor agonist to treat motor symptoms of Parkinson's disease. Neuropharmacology. 2016 Jan;100:106-15. doi: 10.1016/j.neuropharm.2015.04.004. Epub 2015 Apr 18. PMID: 25896768.
