| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| Other Sizes |
|
Purity: ≥98%
Amifostine trihydrate (WR2721), a phosphorylated aminosulfhydryl compound, is the first approved radioprotective drug, it is used to decrease the risk of kidney problems caused by treatment with cisplatin. After dephosphorylation of amifostine by alkaline phosphatase to an active free sulfhydryl (thiol) metabolite, the thiol metabolite binds to and detoxifies cytotoxic platinum-containing metabolites of cisplatin and scavenges free radicals induced by cisplatin and ionizing radiation.
| Targets |
hypoxia-inducible factor-α1 (HIF-α1); p53
|
|---|---|
| ln Vitro |
Amifostine (0.78125-100 μM, 24 h) trihydrate dramatically lowers H9c2 cell apoptosis at a concentration of 100 μM and decreases tert-butyl hydroperoxide (TBHP)-induced cell damage in a dose-dependent manner [5].
|
| ln Vivo |
Male C57BL/6 mice that have myocardial I/R injury are protected against it by amifostine (intravenous injection, 400 mg/kg, 4 h) trihydrate [5].
|
| Enzyme Assay |
We used TBHP, a more stable chemical than H2O2, to induce oxidative stress. For measurement of ROS of the H9c2 cells, cells were incubated with 10 μmol/L ROS sensitive dye 2′,7′-dichloruoresceindiacetate (DCFH-DA) at 37°C for 20 min. ROS was detected by a flow cytometry sorter (BD Biosciences, San Jose, CA, USA) and quantified by BD FACS software. The above experiments were repeated three times. ΔΨm was measured using JC-1 staining; cells were seeded into Petri dishes. After treatment, the dishes were incubated in JC-1 staining solution (5 mg/ml) at 37°C for 20 min. Subsequently the staining cells were washed twice with JC-1 staining buffer; images were taken by a confocal laser scanning microscopy.[5]
|
| Cell Assay |
H9c2 cells were seeded into 96-well plates at a concentration of 5000 cells per well. The cells were pretreated with amifostine (0.78125, 1.5625, 3.125, 6.25, 12.5, 25, 50, and 100 μM) for 30 min before being exposure to tert-Butyl hydroperoxide (TBHP) for 12 h. The number of viable cells was evaluated by MTT assay. Briefly, MTT dye solution was added to each well and incubated for 4 h. The number of viable cells was measured by evaluating Absorbance at 490 nm. The MTT assay was repeated three times for consistency.[5]
|
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice with myocardial I/R injury [5]
Doses: 400 mg/kg Route of Administration: intravenous (iv) injection; 4 hrs (hours)) Experimental Results: Attenuated cardiomyocyte apoptosis and diminished I/R-induced ROS production. Dramatically diminished the expression of cleaved caspase 3 and Bax, while enhancing the expression of SOD1, SOD2 and Bcl2. SOD activity was Dramatically increased and MDA levels were diminished. |
| References |
[1]. D Maurici, et al. Amifostine (WR2721) restores transcriptional activity of specific p53 mutant proteins in a yeast functional assay. Oncogene. 2001 Jun 14;20(27):3533-40.
[2]. Efstathia Giannopoulou, et al. Amifostine inhibits angiogenesis in vivo. J Pharmacol Exp Ther. 2003 Feb;304(2):729-37. [3]. Michael I Koukourakis, et al. Amifostine induces anaerobic metabolism and hypoxia-inducible factor 1 alpha. Cancer Chemother Pharmacol. 2004 Jan;53(1):8-14. [4]. John R Kouvaris, et al. Amifostine: the first selective-target and broad-spectrum radioprotector. Oncologist. 2007 Jun;12(6):738-47. [5]. Shao-Ze Wu, et al. Amifostine Pretreatment Attenuates Myocardial Ischemia/Reperfusion Injury by Inhibiting Apoptosis and Oxidative Stress. Oxid Med Cell Longev. 2017;2017:4130824. |
| Molecular Formula |
C5H15N2O3PS.3H2O
|
|
|---|---|---|
| Molecular Weight |
268.27
|
|
| Exact Mass |
268.085794
|
|
| Elemental Analysis |
C, 22.39; H, 7.89; N, 10.44; O, 35.78; P, 11.55; S, 11.95
|
|
| CAS # |
112901-68-5
|
|
| Related CAS # |
20537-88-6 (free); 112901-68-5 (trihydrate); 59178-37-9 (sodium); 63717-27-1 (monohydrate)
|
|
| Appearance |
White to off-white solid powder
|
|
| tPSA |
124Ų
|
|
| SMILES |
S(C([H])([H])C([H])([H])N([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])P(=O)(O[H])O[H].O([H])[H].O([H])[H].O([H])[H]
|
|
| InChi Key |
TXQPXJKRNHJWAX-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C5H15N2O3PS.3H2O/c6-2-1-3-7-4-5-12-11(8,9)10;;;/h7H,1-6H2,(H2,8,9,10);3*1H2
|
|
| Chemical Name |
S-(2-((3-aminopropyl)amino)ethyl) O,O-dihydrogen phosphorothioate trihydrate
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|---|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7276 mL | 18.6379 mL | 37.2759 mL | |
| 5 mM | 0.7455 mL | 3.7276 mL | 7.4552 mL | |
| 10 mM | 0.3728 mL | 1.8638 mL | 3.7276 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA