Azathioprine

Catalog No.S1721

Azathioprine Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
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Biological Activity

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.
Targets
Rac1 [1]
In vitro

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. [1] Azathioprine-generated 6-Thio-GTP thus prevents the development of an effective immune response via blockade of Vav activity on Rac proteins. [2] 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. [3] 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. [4]

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. [5]

Protocol

Solubility (25°C)

In vitro DMSO 54 mg/mL (194.76 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 277.26
Formula

C9H7N7O2S

CAS No. 446-86-6
Storage powder
Synonyms N/A

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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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Rho Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID