| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In primary rat and human hepatocytes, azathioprine (0-50 μM, 48 hours) sodium causes substantial intracellular GSH depletion at relevant doses [2].
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|---|---|
| ln Vivo |
Azathioprine (oral gavage, 25-400 mg/kg, daily, 10 days) sodium can alter associated parameters such as bone marrow cells, red blood cells, and peripheral blood cytokines in a dose-dependent manner, and can induce apoptosis of female CD-cells. 1 mice and ICR mice [3].
|
| Cell Assay |
Cell viability assay [2]
Cell Types: rat hepatocytes, human hepatocytes Tested Concentrations: 0-50 μM Incubation Duration: 24-48 hrs (hours) Experimental Results: It shows that the cell viability and intracellular GSH level of rat hepatocytes diminished at a low concentration of 0.5 μM , but not diminished. In human hepatocytes, cell viability was Dramatically diminished at concentrations below 50 μM, and GSH depletion was clearly noted at concentrations as low as 1 μM. |
| Animal Protocol |
Animal/Disease Models: outbred female CD-1 mice, female ICR mice [3]
Doses: 25-400 mg/kg Route of Administration: po (oral gavage); every day; 10 days Experimental Results: Result in red blood cell related parameters and white blood cell related parameters. diminished in a dose-dependent manner. fms-like tyrosine kinase 3 (FLT-3) induced bone marrow cell reduction by 52.4%, 35.4%, 17.9%, 16.1% and 15.2% ligand at concentrations of 40, 60, 80, 100 and 120 mg/kg, respectively ( FL) related cytokines increased. Increased induction of apoptosis. |
| References |
[1]. SoniaChavez-Alvarez, et al. Azathioprine: its uses in dermatology. An Bras Dermatol. 2020 Nov-Dec;95(6):731-736.
[2]. Yue-Ting Wu, et al. Azathioprine hepatotoxicity and the protective effect of liquorice and glycyrrhizic acid. Phytother Res. 2006 Aug;20(8):640-5. doi: 10.1002/ptr.1920. [3]. Gemma Molyneux, et al. The haemotoxicity of azathioprine in repeat dose studies in the female CD-1 mouse. Int J Exp Pathol. 2008 Apr;89(2):138-58. |
| Additional Infomation |
Azathioprine Sodium is the sodium salt form of azathioprine, a pro-drug of purine analogue with immunosuppressive activity. Azathioprine is converted in vivo to its active metabolite 6-mercaptopurine (6-MP), which substitutes for the normal nucleoside and mistakenly gets incorporated into DNA sequences. This leads to inhibition of DNA, RNA, and protein synthesis. As a result, cell proliferation may be inhibited, particularly in lymphocytes and leukocytes.
An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed) See also: Azathioprine (broader). |
| Molecular Formula |
C9H7N7O2S.NA+
|
|---|---|
| Exact Mass |
299.02
|
| CAS # |
55774-33-9
|
| Related CAS # |
Azathioprine;446-86-6
|
| PubChem CID |
11529527
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
20
|
| Complexity |
354
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN1C=NC(=C1SC2=NC=NC3=C2N=C[N-]3)[N+](=O)[O-].[Na+]
|
| InChi Key |
WISNYKIQFMKSDQ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C9H6N7O2S.Na/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;/q-1;+1
|
| Chemical Name |
sodium;6-(3-methyl-5-nitroimidazol-4-yl)sulfanylpurin-9-ide
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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.
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