| Size | Price | Stock | Qty |
|---|---|---|---|
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| 10g |
|
||
| 50g |
|
||
| 100g |
|
||
| Other Sizes |
|
Purity: ≥98%
Azathioprine (BW-57322; BW 57-322; Imuran; Azasan; Imurel; AZA; AZTP) is an approved immunosuppressive drug (prodrug of 6-MP) used in the treatment of organ transplantation and autoimmune diseases. It functions by preventing purine synthesis and GTP-binding protein Rac1 from being activated. The active metabolite 6-mercaptopurine (6-MP), which acts as a stand-in for a normal nucleoside and inadvertently incorporates itself into DNA sequences, must be produced in vivo from the prodrug azathioprine. DNA, RNA, and protein synthesis are inhibited as a result. In particular, this may prevent leukocytes and lymphocytes from proliferating.
| Targets |
Rac1
|
|
|---|---|---|
| ln Vitro |
|
|
| ln Vivo |
|
|
| Cell Assay |
Cell Line: Rat hepatocytes, Human hepatocytes
Concentration: 0-50 μM Incubation Time: 24-48 hours Result: Showed the decrease in cell viability and intracellular GSH levels in rat hepatocytes as low concentration of 0.5 μM but no significant decrease in cell viability at concentrations below 50 μM as well as GSH depletion was obviously noted at a concentration as low as 1 μM in human hepatocytes. |
|
| Animal Protocol |
Outbred female CD-1 mice, Female ICR mice
25-400 mg/kg Oral gavage; everyday; 10days |
|
| References |
| Molecular Formula |
C9H7N7O2S
|
|---|---|
| Molecular Weight |
277.26
|
| Exact Mass |
277.04
|
| Elemental Analysis |
C, 38.99; H, 2.54; N, 35.36; O, 11.54; S, 11.56
|
| CAS # |
446-86-6
|
| Related CAS # |
Azathioprine-d3;2702733-53-5;Azathioprine sodium;55774-33-9;Azathioprine-13C4;1346600-71-2
|
| Appearance |
Solid powder
|
| SMILES |
CN1C=NC(=C1SC2=NC=NC3=C2NC=N3)[N+](=O)[O-]
|
| InChi Key |
LMEKQMALGUDUQG-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C9H7N7O2S/c1-15-4-14-7(16(17)18)9(15)19-8-5-6(11-2-10-5)12-3-13-8/h2-4H,1H3,(H,10,11,12,13)
|
| Chemical Name |
6-(3-methyl-5-nitroimidazol-4-yl)sulfanyl-7H-purine
|
| Synonyms |
BW57-322; BW-57-322; Azathioprine; BW 57-322; BW 57 322; trade name: Imuran; Azasan; Imurel. Abbreviations: AZA; AZTP
|
| 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 |
| 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) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6067 mL | 18.0336 mL | 36.0672 mL | |
| 5 mM | 0.7213 mL | 3.6067 mL | 7.2134 mL | |
| 10 mM | 0.3607 mL | 1.8034 mL | 3.6067 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04737343 | Recruiting | Drug: Azathioprine Tablets Drug: Leflunomide |
ANCA Associated Vasculitis Maintenance Therapy |
Chinese SLE Treatment And Research Group |
June 30, 2021 | Not Applicable |
| NCT04160325 | Recruiting | Drug: azathioprine Other: normal diet |
Crohn Disease | Zhu Weiming | January 1, 2018 | Not Applicable |
| NCT05321485 | Recruiting | Other: MedicijnWijs | Crohn Disease Ulcerative Colitis |
Maxima Medical Center | March 16, 2022 | Not Applicable |
| NCT05040464 | Recruiting | Drug: AZA capsules Drug: MTX |
Azathioprine Methotrexate |
Centre Hospitalier Universitaire, Amiens |
August 26, 2021 | Phase 3 |
| NCT05349006 | Not yet recruiting | Drug: Azathioprine Other: Placebo |
Central Nervous System Inflammation MOG-IgG Associated Disease |
Hospices Civils de Lyon | January 1, 2023 | Phase 3 |
|
|---|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
