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L5025

Sigma-Aldrich

来氟米特

Immunosuppressant

同義詞:

5-甲基异恶唑-4-（4-三氟甲基）羧基苯胺

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About This Item

經驗公式（希爾表示法）:
C12H9F3N2O2
CAS號碼:
75706-12-6
分子量：:
270.21
MDL號碼:
MFCD00867593
分類程式碼代碼:
12352202
PubChem物質ID:
24278516
NACRES:
NA.77
暫時無法取得訂價和供貨情況

品質等級

200

化驗

≥98% (TLC)

形狀

powder

mp

166.5 °C

溶解度

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

作用方式

enzyme | inhibits

儲存溫度

2-8°C

SMILES 字串

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

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)

InChI 密鑰

VHOGYURTWQBHIL-UHFFFAOYSA-N

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本產品
1356960PHR1378Y0000674
来氟米特 Immunosuppressant

L5025

来氟米特

来氟米特 United States Pharmacopeia (USP) Reference Standard

1356960

来氟米特

来氟米特 Pharmaceutical Secondary Standard; Certified Reference Material

PHR1378

来氟米特

来氟米特 European Pharmacopoeia (EP) Reference Standard

Y0000674

来氟米特

Gene Information

human ... DHODH(1723)

Gene Information

human ... DHODH(1723)

Gene Information

human ... DHODH(1723)

Gene Information

human ... DHODH(1723)

Quality Level

200

Quality Level

-

Quality Level

300

Quality Level

-

form

powder

form

-

form

-

form

-

storage temp.

2-8°C

storage temp.

-

storage temp.

2-8°C

storage temp.

-

solubility

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

solubility

-

solubility

-

solubility

-

應用

由于其免疫抑制作用，来氟米特被发现可用于器官移植 [1]、类风湿关节炎 [2] 和其他自身免疫性疾病的治疗。

生化／生理作用

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。

象形圖

Skull and crossbones
GHS06

訊號詞

Danger

危險分類

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

標靶器官

Respiratory system

儲存類別代碼

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

水污染物質分類（WGK）

WGK 1

閃點（°F）

Not applicable

閃點（°C）

Not applicable

個人防護裝備

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

  • 規格表

    • 從最近期的版本中選擇一個：

    分析證明 (COA)

    Lot/Batch Number
    039M4044V
    13180905
    107M4010V
    038M4149V
    13180109

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    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
    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
    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
    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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