Ixekizumab (Synonyms:伊西贝单抗; LY2439821)
目录号 : KM14718 CAS No. : 1143503-69-8

Ixekizumab 是一种人源化 IgG4 单克隆抗体,可选择性结合和中和白细胞介素 IL-17A (KD<3 pM)。Ixekizumab 直接阻断 IL-17A 与 IL-17RA 的结合,但不与其他 IL-17 家族成员结合。Ixekizumab 用于中重度斑块型银屑病的研究。

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生物活性

Ixekizumab (LY2439821) is a humanized IgG4 monoclonal antibody that selectively binds and neutralizes interleukin IL-17A (KD<3 pM). Ixekizumab directly blocks IL-17A binding to IL-17RA (IL-17A receptor) but does not bind to other IL-17 family members. Ixekizumab is used for the research of moderate-to-severe plaque psoriasis.

体外研究

The equilibrium KD of Ixekizumab for human and cynomolgus monkey IL-17A were 1.8 pM and 0.8 pM, respectively. Ixekizumab also bound to rabbit IL-17A, but the affinity was lower, and the binding was heterogeneous (KD of 1.3 nM and 14 nM). Ixekizumab shows no binding to either mouse or rat IL-17A.
Ixekizumab (0.1-10000 pM) inhibits human IL-17A- or human IL-17A/F heterodimer-induced growth-regulated oncogene (GRO)α secretion from HT-29 cells in a dose-dependent fashion. Ixekizumab inhibits cynomolgus monkey IL-17A-induced GROα secretion from HT-29 cells in a dose-dependent fashion.

体内研究

Ixekizumab (0.001-1 mg/kg; i.v.) is able to decrease human IL-17A-induced keratinocyte chemoattractant (KC) secretion in the plasma of the C57BL/6 mice in a dose-dependent manner.
In male cynomolgus monkeys, following IV administration of 1 mg/kg, Ixekizumab is eliminated with a mean half-life of 6.5 days. After SC administration of 1 mg/kg, Ixekizumab reaches an average maximal plasma concentration of 11.1 µg/mL ~72 hours postdose. The mean elimination half-life following the SC injection was 10.3 days.

Animal Model: C57BL/6 mice
Dosage: 1 mg/kg, 0.1 mg/kg, 0.01 mg/kg, or 0.001 mg/kg (corresponding to 20 µg, 2 µg, 0.2 µg, and 0.02 µg per mouse, respectively)
Administration: I.v.;
Result: Decrease human IL-17A-induced KC secretion in the plasma of the C57BL/6 mice in a dose-dependent manner.
CAS号
1143503-69-8
中文名称
伊西贝单抗
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

临床试验
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