ST4206 |
| Catalog No.GC31256 |
ST4206 is a potent and orally active adenosine A2A receptor antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1246018-36-9
Sample solution is provided at 25 µL, 10mM.
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ST4206 is a potent adenosine A2A antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively.
ST4206 inhibits agonist-induced cAMP accumulation with an IC50 of 990 nM[1].
ST4206 (10, 20, and 40 mg/kg, p.o.) antagonizes haloperidol-induced catalepsy, and increases motor activity in a dose dependent manner in mice. ST4206 (20 and 40 mg/kg) significantly increases the number of contralateral turns induced by l-DOPA in rats[1]. ST4206 is orally active at concentrations of 10, 20, and 40 mg/kg in haloperidol-induced catalepsy in mice[2].
[1]. Stasi MA, et al. Animal models of Parkinson?s disease: Effects of two adenosine A2A receptor antagonists ST4206 and ST3932, metabolites of 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535). [2]. de Lera Ruiz M, et al. Adenosine A2A receptor as a drug discovery target. J Med Chem. 2014 May 8;57(9):3623-50.
Animal experiment: | Mice[1]Catalepsy is induced by haloperidol (2 mg/kg) injected intraperitoneally (i.p.) 2.5 h before oral administration of 10, 20, and 40 mg/kg ST1535, ST3932, ST4206 or vehicle. An additional group without haloperidol (control group) with only vehicle is administered. At time 0 min, successful induction of catalepsy in all animals is checked before compounds administration, then, catalepsy is scored every 60 min for 3 h. Each mouse is gently placed by its forepaws on a wire at a height of 4.5 cm. The catalepsy is measured as the time necessary for the animal to step down with at least one forepaw with a cut off time for each animal of 60 s; after this time the mouse is gently removed from the wire. Catalepsy is recorded using a video-camera and by an observer who is unaware of the treatment. Rats[1] Two weeks after the unilateral 6-OHDA-lesion, rats are screened on the basis of their contralateral rotation in response to l-DOPA (50 mg/kg i.p.)+benserazide (30 mg/kg i.p.). Rats not showing at least 200 contralateral rotations during 3 h testing period are eliminated from the study. One week later, rats are administered with the threshold dose of l-DOPA (3 mg/kg i.p.)+benserazide (6 mg/kg i.p.) in combination with vehicle (10% sucrose and 0.3% Tween 80 in sterile water i.p.) or with ST1535, ST3932 and ST4206 respectively (10, 20 and 40 mg/kg i.p.). l-DOPA is administered 5 min after vehicle or molecules in study, whereas benserazide is administered 30 min before l-DOPA injection. Contralateral rotations are measured every 10 min for 2 h by Rotameter system. |
References: [1]. Stasi MA, et al. Animal models of Parkinson׳s disease: Effects of two adenosine A2A receptor antagonists ST4206 and ST3932, metabolites of 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535). | |
| Cas No. | 1246018-36-9 | SDF | |
| Canonical SMILES | CC(CCC1=NC(N)=C2N=C(N3N=CC=N3)N(C)C2=N1)=O | ||
| Formula | C12H14N8O | M.Wt | 286.29 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.493 mL | 17.4648 mL | 34.9296 mL |
| 5 mM | 0.6986 mL | 3.493 mL | 6.9859 mL |
| 10 mM | 0.3493 mL | 1.7465 mL | 3.493 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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