Molecular Weight(MW): 277.26
Azathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.
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|Description||Azathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.|
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. 
|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. |
-  Tiede I, et al. J Clin Invest, 2003, 111(8), 1133-1145.
-  Poppe D, et al. J Immunol, 2006, 176(1), 640-651.
-  Tapner MJ, et al. J Hepatol, 2004, 40(3), 454-463.
|In vitro||DMSO||54 mg/mL (194.76 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02936375||Not yet recruiting||Lupus Nephritis||RenJi Hospital||March 2017||Phase 2|
|NCT02900443||Recruiting||Autoimmune Hepatitis||Radboud University|Leiden University Medical Center||January 2017||Phase 4|
|NCT02939573||Recruiting||Primary Cutaneous Vasculitis|Cutaneous Polyarteritis Nodosa|IgA Vasculitis|Henoch-Schönlein Purpura||University of Pennsylvania|National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS)|National Center for Advancing Translational Science (NCATS)|Office of Rare Diseases (ORD)||January 2017||Phase 2|
|NCT02994927||Recruiting||ANCA-Associated Vasculitis||ChemoCentryx||December 2016||Phase 3|
|NCT02998827||Enrolling by invitation||Crohn Disease||Sixth Affiliated Hospital, Sun Yat-sen University||November 2016||--|
|NCT02852694||Not yet recruiting||Crohns Disease||PIBD-Net|European Commission||September 2016||Phase 4|
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