GENZ-882706 (RA03546849)

目录号: GC31842纯度: >98%同义词: RA03546849
GENZ-882706 (RA03546849) 是一种有效的集落刺激因子-1 受体 (CSF-1R) 抑制剂,提取自专利 WO 2017015267A1。

GENZ-882706 (RA03546849)
Cas No.: 2070864-35-4
规格价格库存数量操作
5mg¥4,909.00现货
1
10mg¥7,854.00现货
1
25mg¥16,779.00现货
1
50mg¥25,704.00现货
1

文献被引

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产品描述 Description

GENZ-882706 is a potent colony stimulating factor-1 receptor (CSF-1R) Inhibitor extracted from patent WO 2017015267A1.

Genz-882706 induces an increased level of proliferative activity on unstimulated cells 48 hours post treatment and the reason for this effect is unclear[1].

Daily treatment with Genz-882706 significantly reduces experimental autoimmune encephalomyelitis. Treatment with Genz-882706 in experimental autoimmune encephalomyelitis (EAE) mice results in significant decreases in MCP-1, IL-6, IL-Ιβ and IP-10 levels in spinal cord homogenates when compared to Vehicle treated animals. Treatment with Genz-882706 shows a significant increase in TNF-a levels in the spinal cord when compared to the vehicle treated group. Genz-882706 at both the 30 mg/kg and the 100 mg/kg dose significantly reduces the number of microglia and monocytes/macrophages in the brain and spinal cord compared to the vehicle and LPS controls. Treatment with Genz-882706 modestly reduces CD80 expression on monocytes/macrophages in the brain[1].

[1]. Kane, et al. Colony Stimulating Factor-1 Receptor (CSF-1R) Inhibitors. WO 2017015267A1

实验参考方法 Experimental Reference Method

Cell experiment:

To determine the effect of GENZ-882706 on the proliferation of primary murine microglial cells following LPS or CSF-1 stimulation, GENZ-882706 (500 nM) is added to appropriate assay wells. 25 μL medium are also added to all cells only wells at this time. 25 μL of LPS at 10 ng/mL or 100 ng/mL or CSF-1 at 100 ng/mL are then added to appropriate wells. 25 μL of medium are added to wells not receiving LPS or CSF-1 to bring the final volume of all assay wells to 150uL[1].

Animal experiment:

Mice[1]Mycobacterium tuberculosis is induced in a secondary progressive experimental autoimmune encephalomyelitis (EAE) model in NOD mice with an emulsion of MOG 35-55 and CFA. Therapeutic treatment with Genz-882706 (25mg/kg/day) or vehicle control is started on Day 27 post-disease induction when mice began to enter the progressive stage of disease. Inflammatory/neurotoxic mediators in the CNS are measured through protein analysis in homogenate and gene expression[1].

References:

[1]. Kane, et al. Colony Stimulating Factor-1 Receptor (CSF-1R) Inhibitors. WO 2017015267A1

产品文档 Product Documents

化学性质Chemical Properties

CAS 号
2070864-35-4
同义词
RA03546849
SMILES
COC1=CC=C([C@@H]2OC(C=CC(CN3C4=NC=C(C#CC(N)(C)C)C=C4N=C3)=C5)=C5OC2)C=N1
分子式
C26H25N5O3
分子量
455.51 g/mol
溶解性
Soluble in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol