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Merck
CN

L5025

来氟米特

≥98% (TLC), T cell proliferation inhibitor, powder

别名:

5-甲基异恶唑-4-(4-三氟甲基)羧基苯胺

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关于此项目

经验公式(希尔记法):
C12H9F3N2O2
化学文摘社编号:
分子量:
270.21
UNSPSC Code:
12352202
PubChem Substance ID:
NACRES:
NA.77
MDL number:
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产品名称

来氟米特, Immunosuppressant

SMILES string

Cc1oncc1C(=O)Nc2ccc(cc2)C(F)(F)F

InChI key

VHOGYURTWQBHIL-UHFFFAOYSA-N

InChI

1S/C12H9F3N2O2/c1-7-10(6-16-19-7)11(18)17-9-4-2-8(3-5-9)12(13,14)15/h2-6H,1H3,(H,17,18)

assay

≥98% (TLC)

form

powder

mp

166.5 °C

solubility

methanol: 19.60-20.40 mg/mL, clear, colorless to faintly yellow

mode of action

enzyme | inhibits

storage temp.

2-8°C

Quality Level

Gene Information

human ... DHODH(1723)

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Application

由于其免疫抑制作用,来氟米特被发现可用于器官移植 、类风湿关节炎 和其他自身免疫性疾病的治疗。

Biochem/physiol Actions

免疫抑制;抑制 T、B 细胞增殖。活性主要归因于其代谢产物丙二腈衍生物,后者被认为抑制二氢乳清酸脱氢酶(在 新生 嘧啶合成途径中)以及几种蛋白酪氨酸激酶。

pictograms

Skull and crossbones

signalword

Danger

Hazard Classifications

Acute Tox. 3 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

target_organs

Respiratory system

存储类别

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Faceshields, Gloves


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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T R Brazelton et al.
Current opinion in immunology, 8(5), 710-720 (1996-10-01)
Among all the new immunosuppressive molecules being investigated either preclinically or clinically, four stand out: tacrolimus (FK506), sirolimus (rapamycin), mycophenolate mofetil and leflunomide (and its malononitriloamide analogs). Each drug has distinct mechanisms of immunosuppressive action, and in the past year
X Xu et al.
Biochemical pharmacology, 52(4), 527-534 (1996-08-23)
Previous studies have demonstrated that the active metabolite of leflunomide, A77 1726 [N-(4-trifluoromethylphenyl-2-cyano-3-hydroxycrotoamide)], is capable of inhibiting the activities of tyrosine kinases and dihydroorotate dehydrogenase (DHO-DHase). In the present study, we define the relative contribution of these activities to the
J M Kremer et al.
Clinical and experimental rheumatology, 22(5 Suppl 35), S95-100 (2004-11-24)
Leflunomide was first shown to have disease-modifying properties in a rat model of adjuvant-induced arthritis. Leflunomide has been subsequently used with success in several animal models of tissue and organ allograft and of autoimmune disease including collagen- and adjuvant-induced arthritis
K F Siemasko et al.
Transplantation, 61(4), 635-642 (1996-02-27)
Leflunomide is an immunosuppressive drug capable of inhibiting cellular and humoral mediated responses in vivo. The mechanism responsible for suppression of B cell antibody responses in vivo has not been identified. In this study we demonstrate that leflunomide functions to
Nicolae Leca
Current opinion in organ transplantation, 14(4), 370-374 (2009-06-11)
Leflunomide has been used off-label in renal transplantation because of the attractive combination of antiviral and immunosuppressive effects. This study intends to review the clinical applications of leflunomide with interest to transplantation. In renal transplantation, particularly in BK nephropathy, the

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