product name Azathioprine
Description: Azathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, it is used in the treatment of organ transplantation and autoimmune diseases. Azathioprine is a prodrug that has to be 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.
References: J Clin Invest. 2003 Apr;111(8):1133-45; J Immunol. 2006 Jan 1;176(1):640-51; Exp Brain Res. 1995;106(2):181-6.
277.26
Formula
C9H7N7O2S
CAS No.
446-86-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 54 mg/mL (194.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Azathioprine suppresses the activation of Rac1 target genes such as mitogen-activated protein kinase kinase (MEK), NF-kappaB, and bcl-x(L), leading to a mitochondrial pathway of apoptosis in primary human CD4+ T lymphocytes. Azathioprine thus converts a costimulatory signal into an apoptotic signal by modulating Rac1 activity. Azathioprine-generated 6-Thio-GTP thus prevents the development of an effective immune response via blockade of Vav activity on Rac proteins. Azathioprine (1 mM) restores ATP levels and arrests cell injury, while culture in glucose-enriched media augments ATP levels and ameliorates cell death. Azathioprine reduces viability 5-34% at day 1 and 42-92% by day 4. Azathioprine decreases the viability of hepatocytes and induces the following events in primary culture of isolated rat hepatocytes: intracellular reduces glutathione (GSH) depletion, metabolic activity reduction, and lactate dehydrogenase release. Azathioprine effect on hepatocytes is associated with swelling and increased oxygen consumption of intact isolated rat liver mitochondria. Kinase Assay: Cell Assay: |
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| In Vivo | Azathioprine combined with cyclosporin A and prednisolone has resulted in survival of 14 out of 15 grafts (93%), compared with 11 out of 14 (79%) in the group treated with cyclosporin A alone in mouse-rat brain xenograft. |
| Animal model | |
| Formulation & Dosage | |
| References | J Clin Invest. 2003 Apr;111(8):1133-45; J Immunol. 2006 Jan 1;176(1):640-51; Exp Brain Res. 1995;106(2):181-6. |
