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Laquinimod(ABR-215062)
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。
Laquinimod(ABR-215062)图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Laquinimod (ABR-215062) (ABR-215062) 是一种可口服的羧酰胺衍生物,是一种有效的免疫调节剂,可防止中枢神经系统的神经变性和炎症。

Cell experiment:

Purified CD11b+ cells from laquinimod- or vehicle-treated mice are cultured with naive CD4+ cells isolated from laquinimod- or vehicle-treated 2D2 mice and antigen (MOG p35-55, 20 μg/mL). Cells are cultured in 96-well microtitre plates at a concentration of 0.25×106 cells/mL. Culture medium consisted of RPMI 1640 supplemented with L-glutamine (2 mM), sodium pyruvate (1 mM), penicillin (100 U/mL), streptomycin (0.1 mg/mL), 2-mercaptoethanol (5×10-5 M) and 10% (v/v) fetal bovine serum. Cells are incubated for 48 h and pulsed for 18 h with 1 μCi per well of [3H]-thymidine before harvesting.

Animal experiment:

Seven to 10-week-old female C57BL/6, DBA/1 or SJL/J mice are injected subcutaneously with 50 μg MOG p35-55, 50 μg rMOG or 100 μg PLP p139-151, respectively, in complete Freund's adjuvant. After immunization and 2 days later, mice receive 200 ng (C57BL/6) or 100 ng (SJL/J) pertussis toxin intraperitoneally (i.p.). For adoptive transfer, donor SJL/J mice are immunized as described above and treated daily with laquinimod or vehicle. 10 days later, cells from draining lymph nodes and spleen are isolated, re-stimulated for 48 h (20 μg/mL PLP p139-151), and injected i.p. into naive SJL/J recipients (107 cells per mouse). Animals are observed daily and clinical scores are assessed as follows: 0, no signs; 1, decreased tail tone; 2, mild monoparesis or paraparesis; 3, severe paraparesis; 4, paraplegia and/or quadraparesis; and 5, moribund or death.

产品描述

ABR-215062 is an orally active immunoregulator. Experimental autoimmune encephalomyelitis (EAE) is an inflammatory autoimmune disease of the CNS that can be elicited in rodents and represents the major animal model for the study of multiple sclerosis (MS).

In vitro: ABR-215062 was shown to completely inhibit the development of murine acute experimental autoimmune encephalomyelitis (EAE) [1].

In vivo: ABR-215062 dose-dependently inhibited disease and showed better disease inhibitory effects as compared to roquinimex (Linomide). Furthermore, ABR-215062 inhibited the inflammation of both CD4+ T cells and macrophages into central nervous tissues [2].

Clinical trial: Randomized, controlled clinical trials in relapsing MS demonstrate a dose–response effect of ABR-215062 on disease activities, indicated by reduced clinical relapse rate, number of brain MRI active lesions, and sustained disability and brain atrophy [3].

References:
[1] Brunmark C, Runstrom A, Ohlsson L, Sparre B, Brodin T, Astrom M, Hedlund G.  The new orally active immunoregulator laquinimod (ABR-215062) effectively inhibits development and relapses of experimental autoimmune encephalomyelitis. J Neuroimmunol. 2002 Sep;130(1-2):163-72.
[2] Yang JS, Xu LY, Xiao BG, Hedlund G, Link H.  Laquinimod (ABR-215062) suppresses the development of experimental autoimmune encephalomyelitis, modulates the Th1/Th2 balance and induces the Th3 cytokine TGF-beta in Lewis rats. J Neuroimmunol. 2004 Nov;156(1-2):3-9.
[3] Haggiag S, Ruggieri S, Gasperini C.  Efficacy and safety of laquinimod in multiple sclerosis: current status. Ther Adv Neurol Disord. 2013 Nov;6(6):343-52.