SK609 hydrochloride

Name: SK609 hydrochloride
Brand: MedChemExpress
SKU: HY-117059
Rating: 4.5 (1 reviews)

Cat. No.: HY-117059 Purity: 99.83%: FAQs
Data Sheet SDS COA Handling Instructions

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SK609 hydrochloride is a dopamine D3 receptor (D3R) selective agonist with an EC₅₀ of 1109 nM. SK609 hydrochloride has the potential for parkinson research.

For research use only. We do not sell to patients.

SK609 hydrochloride Chemical Structure

CAS No. : 1092797-77-7

Size	Price	Stock	Quantity
5 mg	USD 238	In-stock	Estimated Time of Arrival: December 31
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50 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

SK609 hydrochloride is a dopamine D3 receptor (D3R) selective agonist with an EC₅₀ of 1109 nM. SK609 hydrochloride has the potential for parkinson research^[1].

IC₅₀ & Target^[1]

Dopamine D3 receptor

1109 nM (EC₅₀)

In Vitro

In a Competitive inhibition affinity assay by SK609 to D3R, SK609 exhibits an EC₅₀ value of 1109 ± 273 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 ± 0.2 μM, 50.2 ± 5.9 nM, and 14.4 ± 2.7 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.

In Vivo

Safety toxicology studies of SK609 in rats have shown the maximum tolerated dose of SK609 is 30mg/kg and all the doses used in this study are well within the no-observed-adverse-effect level of SK609^[1].
SK609 shows the maximum tolerated dose of SK609 is 30mg/kg in safety toxicology study within the no-observed-adverse-effect level of SK609^[2].
In the cynomolgus macaques PK study, oral administration of SK609 (0.5, 2 and 4 mg/kg) is associated with mean C_max values of 13.7, 69.3 and 218 ng/ml respectively, occurring at (T_max) 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 had a mean terminal half-life of 7.9 h in plasma. SK609 (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.

Molecular Weight

220.14

Formula

C₁₀H₁₅Cl₂N

CAS No.

1092797-77-7

Unlabeled CAS

Appearance

Solid

Color

Off-white to light brown

SMILES

CC(CCC1=CC=CC=C1Cl)N.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.5426 mL	22.7128 mL	45.4256 mL
5 mM	0.9085 mL	4.5426 mL	9.0851 mL
10 mM	0.4543 mL	2.2713 mL	4.5426 mL

View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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Dosing volume
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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.83%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (250 KB) HNMR (266 KB) LCMS (86 KB)

Handling Instructions (2659 KB)

References

[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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

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