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Teriflunomide

特立氟胺
Catalog No.
B1850
二氢乳清酸脱氢酶的抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 454.00
现货
10mg
¥ 272.00
现货
100mg
¥ 818.00
现货

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A

背景

Teriflunomide (also known as A77 1726), the active metabolite of an approved antirheumatic drug Leflunomide, is an emerging oral therapy for multiple sclerosis (MS). Teriflunomide has demonstrated anti-inflammatory, antiproliferative and immunosuppressive

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt270.21
Cas No.108605-62-5
FormulaC12H9F3N2O2
Solubilityinsoluble in H2O; ≥13.5 mg/mL in DMSO; ≥2.54 mg/mL in EtOH with gentle warming and ultrasonic
Chemical Name(Z)-2-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]but-2-enamide
SDFDownload SDF
Canonical SMILESCC(=C(C#N)C(=O)NC1=CC=C(C=C1)C(F)(F)F)O
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试验操作

Cell experiment:[1]

Cell lines

Human synoviocytes

Reaction Conditions

10-7 ~ 10-4 M teriflunomide for 50 h incubation

Applications

Teriflunomide inhibited the production of prostaglandin E2 in TNF-α- or IL-1α-stimulated isolated human synoviocytes (IC50s = 7 and 3 μM, respectively). At higher concentrations (> 10 μM), teriflunomide also reduced the production of matrix metalloproteinase 1 and IL-6 due to the known inhibitory effect of teriflunomide on pyrimidine synthesis, which could be reversed by the addition of uridine.

Animal experiment:[2]

Animal models

Male Dark Agouti (DA) rat, 6-week old

Dosage form

3 and 10 mg/kg

Once daily by oral route

Applications

Teriflunomide (3 and 10 mg/kg) delayed disease onset and decreased neurological deficits in a rat model of experimental autoimmune encephalomyelitis induced by complete Freund’s adjuvant and Mycobacterium tuberculosis.

Note

The technical data provided above is for reference only.

References:

1. Burger D, Begué-Pastor N, Benavent S, et al. The active metabolite of leflunomide, A77 1726, inhibits the production of prostaglandin E(2), matrix metalloproteinase 1 and interleukin 6 in human fibroblast-like synoviocytes. Rheumatology (Oxford), 2003, 42(1): 89-96.

2. McMonagle-Strucko K. Teriflunomide reduces behavioral, electrophysiological, and histopathological deficits in the Dark Agouti rat model of experimental autoimmune encephalomyelitis. Journal of Neurology, 2009, 256(1): 89-103.

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