ST 1535
Based on 1 Customer Validation
ST 1535 is a potent and orally active A2A adenosine receptor antagonist. ST 1535 shows antiparkinsonian activity and antitremorigenic effects. ST 1535 has the potential for the research of Parkinson’s disease.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.80%
- No. CAS: 496955-42-1
- Fòrmula: C12H16N8
- Peso molecular:272.31
-
Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
HY-19533
SCH 58261A2A Receptor Antagonist -
HY-10995
TozadenantAdenosine Receptor Antagonist -
HY-19533R
SCH 58261 (Standard)A2A Receptor Antagonist -
HY-119486
TavapadonDopamine D1/D5 Receptor Agonist -
HY-124729
BL-918ULK1 Activator -
HY-111954
(+)-Erinacin AAnticancer Agent -
HY-129393
EtrumadenantA2aR/A2bR Antagonist -
HY-103169
SCH442416A2AR Antagonist -
HY-101980
ImaradenantA2AR Antagonist -
HY-102024
A2A receptor antagonist 1Adenosine A2A-R Antagonist -
HY-10857
VipadenantAdenosine Receptor Antagonist -
HY-103170
LUF5834A2A/A2B Receptor Agonist
Ver todos los productos específicos de isoformas Adenosine Receptor
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
A2a adenosine receptor |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
430 nM
Compound: 1, ST1535
|
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
|
[PMID: 23789814] |
In Vitro
In Vivo
ST 1535 (10, 20, 40 mg/kg; i.p.) increases the number of contralateral turns induced by l-DOPA (HY-N0304) in rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:5-6 weeks CD1 male mice[1]
-
Dosage:0, 5, 10 mg/kg
-
Administration:P.o.
-
Result:Antagonized catalepsy induced by i.c.v. administration with the A2A adenosine agonist CGS 21680.
-
Animal Model:Male Sprague Dawley rats[2]
-
Dosage:10, 20, 40 mg/kg
-
Administration:I.p.
-
Result:Significantly increased the number of contralateral turns induced by l-DOPA (3 mg/kg i.p.) at 20 and 40 mg/kg.
Chemical Information
-
No. CAS 496955-42-1
-
Appearance Solid
-
Peso molecular 272.31
-
Fòrmula C12H16N8
-
Color White to off-white
-
SMILES
CN1C(N2N=CC=N2)=NC3=C1N=C(CCCC)N=C3N
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (183.61 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. 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. 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (279 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. Stasi MA, et al. ST 1535: a preferential A2A adenosine receptor antagonist. Int J Neuropsychopharmacol. 2006 Oct;9(5):575-84. [Content Brief]
[2]. Tronci E, et al. Characterization of the antiparkinsonian effects of the new adenosine A2A receptor antagonist ST1535: acute and subchronic studies in rats. Eur J Pharmacol. 2007 Jul 2;566(1-3):94-102. [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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6723 mL | 18.3614 mL | 36.7229 mL | 91.8071 mL |
| 5 mM | 0.7345 mL | 3.6723 mL | 7.3446 mL | 18.3614 mL | |
| 10 mM | 0.3672 mL | 1.8361 mL | 3.6723 mL | 9.1807 mL | |
| 15 mM | 0.2448 mL | 1.2241 mL | 2.4482 mL | 6.1205 mL | |
| 20 mM | 0.1836 mL | 0.9181 mL | 1.8361 mL | 4.5904 mL | |
| 25 mM | 0.1469 mL | 0.7345 mL | 1.4689 mL | 3.6723 mL | |
| 30 mM | 0.1224 mL | 0.6120 mL | 1.2241 mL | 3.0602 mL | |
| 40 mM | 0.0918 mL | 0.4590 mL | 0.9181 mL | 2.2952 mL | |
| 50 mM | 0.0734 mL | 0.3672 mL | 0.7345 mL | 1.8361 mL | |
| 60 mM | 0.0612 mL | 0.3060 mL | 0.6120 mL | 1.5301 mL | |
| 80 mM | 0.0459 mL | 0.2295 mL | 0.4590 mL | 1.1476 mL | |
| 100 mM | 0.0367 mL | 0.1836 mL | 0.3672 mL | 0.9181 mL |
ST 1535 Related Classifications
HY-105003 Related Classifications
Powered by Bioz