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Emactuzumab Sale

(Synonyms: RG 7155; RO 5509554) 目录号 : GC66380

Emactuzumab (RG 7155) 是一种特异性单克隆抗体,可抑制集落刺激因子 1 受体 (CSF1R) 的激活。Emactuzumab 对 CSF-1R 具有高亲和力,Ki 值为 0.2 nM,可阻断 CSF-1R 二聚化。Emactuzumab 可用于多种疾病的研究,如弥漫型腱鞘巨细胞瘤(dt-GCT)。

Emactuzumab Chemical Structure

Cas No.:1448221-67-7

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Sample solution is provided at 25 µL, 10mM.

Description

IC50: 0.2 nM (CSF-1R)[2]

Emactuzumab(RG 7155) is a specific monoclonal antibody that inhibits colonystimulating factor 1 receptor (CSF1R) activation. Emactuzumab has high affinity for CSF-1R with Ki value of 0.2 nM to blocks CSF-1R dimerization. Emactuzumab can be used for the research of several diseases, such as diffuse-type tenosynovial giant cell tumour (dt-GCT) [1][2].

Emactuzumab (RG 7155) binds to human and cynomolgus CSF-1R with high affinity (Kd = 0.2 nM) to blocks CSF-1R dimerization[2].
RG7155 (0-10 μg/mL, 7 days) potently inhibited the viability of CSF-1-differentiated macrophages with an IC50 of 0.3 nM by inducing cell death[2].
RG7155 (30 μg/mL, 6 days) induces cell death of in vitro-differentiated human M2-like macrophages[2].

Cell Viability Assay[2]

Cell Line: CSF-1 and/or GM-CSF Macrophages
Concentration: 0-10 μg/mL
Incubation Time: 7 days
Result: Resulted cell death of CSF-1-differentiated macrophages.

Emactuzumab(RG 7155) (i.v.; 0.1、1、10、30 and 100 mg/kg; once) increases CSF-1 concentration in nonhuman primates' peripheral blood[2].
RG7155 (i.v.; 0, 30, and 100 mg/kg; once weekly; for 2 weeks) depletes CSF-1R+CD163+ macrophages in vivo[2].

Animal Model: cynomolgus monkeys Macaca fascicularis[2]
Dosage: 0.1, 1, 10, 30 and 100 mg/kg (male cynomolgus monkeys)
0, 30, and 100 mg/kg (male and female cynomolgus)
Administration: i.v., once (male cynomolgus monkeys)
i.v., once weekly, for 2 weeks(male and female cynomolgus)
Result: Increased CSF-1 concentration in serum.
Efficiently reduced CSF-1R and CD68+163+ macrophages in the liver (Kupffer cells) and colon of cynomologus monkeys.

化学性质

Cas No. 1448221-67-7 SDF Download SDF
别名 RG 7155; RO 5509554
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