SYD5115
Based on 1 Customer Validation
SYD5115 is an orally available TSH-R antagonist.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.69%
- CAS. Nr.: 3043770-26-6
- Formel: C22H32F2N4O3
- Molecular Weight:438.51
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biologische Aktivität
SYD5115 (0.1 nM-10 μM) blocks M22-induced cAMP production with IC50s of 22 nM in rat FRTL5 and HEK293-hTSHR cells, respectively[1] .
Note: M22 is a stimulating autoantibody to the human monoclonal TSH receptor (TSHR), and another autoantibody is K1-70 (blocking) [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS. Nr. 3043770-26-6
-
Appearance Solid
-
Molecular Weight 438.51
-
Formel C22H32F2N4O3
-
Color White to off-white
-
SMILES
O=C(O[C@H](C(C)(C)C)C)NC1=NC=C(N(C(C)=O)C2(C)C)C(C32CCC(F)(F)CC3)=N1
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (228.04 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 5 mg/mL (11.40 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Reinheit & Dokumentation
-
Data Sheet (275 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. Karstens WFJ, et al. Discovery of SYD5115, a novel orally active small molecule TSH-R antagonist. Bioorg Med Chem. 2023 Apr 15;84:117258. [Content Brief]
[2]. Furmaniak J, et al. In vivo effects of a human thyroid-stimulating monoclonal autoantibody (M22) and a human thyroid-blocking autoantibody (K1-70). Auto Immun Highlights. 2011 Sep 14;3(1):19-25. [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 | 2.2804 mL | 11.4022 mL | 22.8045 mL | 57.0112 mL |
| 5 mM | 0.4561 mL | 2.2804 mL | 4.5609 mL | 11.4022 mL | |
| 10 mM | 0.2280 mL | 1.1402 mL | 2.2804 mL | 5.7011 mL | |
| 15 mM | 0.1520 mL | 0.7601 mL | 1.5203 mL | 3.8007 mL | |
| 20 mM | 0.1140 mL | 0.5701 mL | 1.1402 mL | 2.8506 mL | |
| 25 mM | 0.0912 mL | 0.4561 mL | 0.9122 mL | 2.2804 mL | |
| 30 mM | 0.0760 mL | 0.3801 mL | 0.7601 mL | 1.9004 mL | |
| 40 mM | 0.0570 mL | 0.2851 mL | 0.5701 mL | 1.4253 mL | |
| 50 mM | 0.0456 mL | 0.2280 mL | 0.4561 mL | 1.1402 mL | |
| 60 mM | 0.0380 mL | 0.1900 mL | 0.3801 mL | 0.9502 mL | |
| 80 mM | 0.0285 mL | 0.1425 mL | 0.2851 mL | 0.7126 mL | |
| 100 mM | 0.0228 mL | 0.1140 mL | 0.2280 mL | 0.5701 mL |