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Azathioprine(BW 57-322)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Azathioprine(BW 57-322)图片
CAS NO:446-86-6
规格:≥98%
包装与价格:
包装价格(元)
1g电议
2g电议
5g电议
10g电议
50g电议
100g电议

产品介绍
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 acts by inhibiting purine synthesis and GTP-binding protein Rac1 activation. 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.
理化性质和储存条件
Molecular Weight (MW)277.26
FormulaC9H7N7O2S
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)

Chemical Name: 6-((1-methyl-4-nitro-1H-imidazol-5-yl)thio)-7H-purine

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)

SMILES Code: O=[N+](C1=C(SC2=C3NC=NC3=NC=N2)N(C)C=N1)[O-]

Synonyms

BW57-322; BW-57-322; Azathioprine; BW 57-322; BW 57 322; trade name: Imuran; Azasan; Imurel. Abbreviations: AZA. AZTP.

实验参考方法
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.

In VivoAzathioprine 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 modelMouse-rat brain xenograft
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.