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)。
Cas No. | 1448221-67-7 |
别名 | RG 7155; RO 5509554 |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | IC50: 0.2 nM (CSF-1R)[2] Emactuzumab(RG 7155) is a specificmonoclonal antibodythat inhibits colonystimulating factor 1 receptor(CSF1R)activation. Emactuzumab has high affinity for CSF-1R withKivalue 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 IC50of 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 monkeysMacaca 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. |
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