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）。
| 生物活性 | 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]. |
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体外研究
(In Vitro) | 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. |
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体内研究
(In Vivo) | 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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| 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. |
