Amustaline dihydrochloride
Based on 1 Customer Validation
Amustaline (S-303) dihydrochloride, a nucleic acid-targeted alkylator, is an efficient pathogen inactivation agent for blood components containing red blood cells. Amustaline dihydrochloride has three components: an acridine anchor (an intercalator that targets nucleic acids non-covalently), an effector (a bis-alkylator group that reacts with nucleophiles), and a linker (a small flexible carbon chain containing a labile ester bond that hydrolyzes at neutral pH to yield non-reactive breakdown products).
For research use only. We do not sell to patients.
- Purity: 95.0%
- CAS No.: 210584-54-6
- Formula: C22H27Cl4N3O2
- Molecular Weight:507.28
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
S‐303 (200 μM; 20 h) and glutathione (GSH; 20 mM) inactivates high titres of Chikungunya virus (CHIKV) in red blood cells (RBCs)[1].
S-303 (200 μM; 20 h) and GSH (2 mM) inactivates >6.5 logs of HIV, >5.7 logs of Bluetongue virus, >7.0 logs of Yersinia enterocolitica, 4.2 logs of Serratia marcescens, and 7.5 logs of Staphylococcus epidermidis in whole blood experiments[2].
S-303 (200 μM; 20 h) and GSH (20 mM) inactivates approximately 5 logs or greater of Y. enterocolitica, E. coli, S. marcescens, S. aureus, HIV, bovine viral diarrhoea virus, bluetongue virus and human adenovirus 5 in RBC[2].
S-303 (200 μM; 20 h) retains in vitro parameters of RBC function and physiology (including total ATP, extracellular potassium, hemolysis, glucose consumption, lactate production, and pH at 37 °C) compared to conventional RBC[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
S‐303 RBCs (repeated transfusions) is well tolerated in rats (10 μmol/kg) and dogs (10 μmol/kg) with no histopathologic evidence of organ toxicity[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 210584-54-6
-
Appearance Oil
-
Molecular Weight 507.28
-
Formula C22H27Cl4N3O2
-
Color Yellow to brown
-
SMILES
O=C(CCNC1=C2C=CC=CC2=NC3=CC=CC=C31)OCCN(CCCl)CCCl.[H]Cl.[H]Cl
-
Synonyms
S-303 dihydrochloride
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (197.13 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
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 (4.93 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
-
Data Sheet (271 KB)
-
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
-
Handling Instructions (2659 KB)
References
[1]. Aubry M, et, al. Amustaline (S-303) treatment inactivates high levels of Chikungunya virus in red-blood-cell components. Vox Sang. 2018 Apr;113(3):232-241. [Content Brief]
[2]. Mufti NA, et, al. Treatment of whole blood (WB) and red blood cells (RBC) with S-303 inactivates pathogens and retains in vitro quality of stored RBC. Biologicals. 2010 Jan;38(1):14-9. [Content Brief]
[3]. North A, et, al. Preclinical pharmacokinetic and toxicology assessment of red blood cells prepared with S-303 pathogen inactivation treatment. Transfusion. 2011 Oct;51(10):2208-18. [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 (sealed storage, away from moisture). 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 | 1.9713 mL | 9.8565 mL | 19.7130 mL | 49.2824 mL |
| 5 mM | 0.3943 mL | 1.9713 mL | 3.9426 mL | 9.8565 mL | |
| 10 mM | 0.1971 mL | 0.9856 mL | 1.9713 mL | 4.9282 mL | |
| 15 mM | 0.1314 mL | 0.6571 mL | 1.3142 mL | 3.2855 mL | |
| 20 mM | 0.0986 mL | 0.4928 mL | 0.9856 mL | 2.4641 mL | |
| 25 mM | 0.0789 mL | 0.3943 mL | 0.7885 mL | 1.9713 mL | |
| 30 mM | 0.0657 mL | 0.3285 mL | 0.6571 mL | 1.6427 mL | |
| 40 mM | 0.0493 mL | 0.2464 mL | 0.4928 mL | 1.2321 mL | |
| 50 mM | 0.0394 mL | 0.1971 mL | 0.3943 mL | 0.9856 mL | |
| 60 mM | 0.0329 mL | 0.1643 mL | 0.3285 mL | 0.8214 mL | |
| 80 mM | 0.0246 mL | 0.1232 mL | 0.2464 mL | 0.6160 mL | |
| 100 mM | 0.0197 mL | 0.0986 mL | 0.1971 mL | 0.4928 mL |