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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:
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。
signalword
Danger
hcodes
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
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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