Plerixafor (AMD3100) 普乐沙福

目录号 M1898 所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务

Plerixafor (AMD3100)是一种大环类化合物，同时也是CXCR4趋化因子受体的拮抗剂，可以作用于CXCR4和CXCL12调节趋化性，IC50分别为44 nM和5.7 nM。

别名：AMD3100; JM3100; ID791; AMD-3329

规格	价格	库存状态
Free Sample (0.5-1 mg)	¥ 0	中国库存现货
5mg	¥ 342	中国库存现货
10mg	¥ 585	中国库存现货
25mg	¥ 1035	中国库存现货
50mg	¥ 1755	中国库存现货
100mg	¥ 2970	中国库存现货

其他规格数量报价？

质量标准及产品资料

纯度： 99.24%
COA
MSDS
H-NMR
HPLC

产品信息

生物活性

Plerixafor (AMD3100)是一种CXCR4趋化因子受体拮抗剂，作用于CXCR4和CXCL12调节的趋化性，IC50分别为44 nM和5.7 nM。Plerixafor 是一种免疫刺激剂和造血干细胞动员剂，也是 CXCR7 的变构激动剂。Plerixafor 抑制 HIV-1 和 HIV-2 的复制，EC50 为 1-10 nM。

使用AbMole产品发表的文献

Biomaterials. 2023 Oct 17.

The genetic background determines material-induced bone formation through the macrophage-osteoclast axis
Plast Reconstr Surg. 2023 Jan 9.

Early angiogenesis dependent CXCL12 attracts Adipose-derived stem cells to promote the repair of fat grafting in a mice model
Front Pharmacol. 2022 Feb 1;792293.

Deletion of Wild-type p53 Facilitates Bone Metastatic Function by Blocking the AIP4 Mediated Ligand-Induced Degradation of CXCR4

产品使用成果展示

	数据来源	Tianjin Med J (2015). Figure 4. AMD3100 (Abmole Bioscience)
	方法	Caspase-3 Assay
	细胞系/动物模型	EPCs
	浓度	25 μmol/L
	处理时间	24、48、96 h
	实验结果	Compared with the control group, GLP-1 overexpression decreased Caspase-3 mRNA expression and Caspase-3 activity, both of which were significantly decreased after 48 h of GLP-1 treatment, and the most significant down-regulation trend was shown at 96 h (P<0.05). When the SDF-1/CXCR4 signaling pathway was blocked, the inhibitory effect of GLP-1 on Caspase-3 mRNA expression and Caspase-3 activity were significantly decreased (P <0.05). As shown in figure 4.

	数据来源	Tianjin Med J (2015). Figure 3. AMD3100 (Abmole Bioscience)
	方法	MTT
	细胞系/动物模型	EPCs
	浓度	25 μmol/L
	处理时间	24、48、96 h
	实验结果	Compared with the control group, GLP-1 overexpression significantly promoted cell proliferation (P<0.05). After blocking the SDF-1/CXCR4 signaling pathway with AMD3100 blocker, the proliferation effect of GLP-1 on EPCs was significantly decreased (P<0.05), as shown in Figure 3.

	数据来源	Tianjin Med J (2015). Figure 2. AMD3100 (Abmole Bioscience)
	方法	qPCR
	细胞系/动物模型	EPCs
	浓度
	处理时间	24、48、96 h
	实验结果	Compared with the control group, GLP-1 overexpression significantly increased the mRNA expressions of C/EBPα and PPARγ (P<0.05) in a time dependent manner. After the SDF-1/CXCR4 signaling pathway was blocked, GLP-1 significantly inhibited the mRNA expression of C/EBPα and PPARγ (P < 0.05), as shown in Figure 2.

	数据来源	Tianjin Med J (2015). Figure 1. AMD3100 (Abmole Bioscience)
	方法	western blot
	细胞系/动物模型	EPCs
	浓度	0、5、15 and 25 μmol/L
	处理时间	48h
	实验结果	Compared with the control group (0.465±0.085), CXCR4 protein expression was significantly decreased after treatment with different doses of AMD3100, and the effect of 25 μmol/L AMD3100 group (0.054±0.023) was the most significant (F=16.347, P < 0.05), see Figure 1. It was proved that 25 μmol/L AMD3100 had the best blocking effect and could be used for subsequent blocking experiments.

实验参考

体外实验*
细胞系	OS cell lines (LM8 and Dunn)
方法	MTT assay. The effects of CXCL12 and AMD3100 on the survival of two OS cell lines (LM8 and Dunn) were assessed using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cells were seeded in 96-well plates at 2×103/well in DMEM-h. After overnight growth, the cells were cultured for 7 days in FBS-free medium in the presence of 0 or 100 ng/ml CXCL12, 30 μM AMD3100 alone or 100 ng/ml CXCL12 with 10, 20 or 30 μM AMD3100. The FBS-free cells without 100 ng/ml CXCL12 or AMD3100 served as the control group. After the 7 day incubation, 20 μl MTT (5 mg/ml; Sigma, St. Louis, MO, USA) was added into each well and incubated for 4 h at 37°C. Culture medium was removed and 150 μl dimethylsulfoxide was added. The optical density (OD) was then measured using a model ELx800 microplate reader (Bio-Tech instruments inc.) at 490 nm. The cell viability was calculated using the equation: Cell viability (%) = (OD490nm of treatment/OD490nm of control) ×100%.
浓度	30 μM
处理时间	7 days

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
动物模型	orthotopic animal model of OS in Ten 4-week-old female C3H mice
配制	PBS
剂量	5 mg/kg every 2 days
给药处理	tail vein injection

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

化学性质

分子量	502.78
分子式	C28H54N8
CAS号	110078-46-1
溶解性（25°C）	Ethanol 50 mg/mL Water < 1 mg/mL
储存条件	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.9889 mL	9.9447 mL	19.8894 mL
5 mM	0.3978 mL	1.9889 mL	3.9779 mL
10 mM	0.1989 mL	0.9945 mL	1.9889 mL

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m²)	0.007	0.025	0.15	0.05	0.02	0.5
K_m 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Liao YX, et al. Oncol Rep. AMD3100 reduces CXCR4-mediated survival and metastasis of osteosarcoma by inhibiting JNK and Akt, but not p38 or Erk1/2, pathways in in vitro and mouse experiments.

[2] Kim JH, et al. Radiat Res. Plerixafor, a CXCR4 antagonist, mitigates skin radiation-induced injury in mice.

[3] Uy GL, et al. Expert Opin Biol Ther. Plerixafor, a CXCR4 antagonist for the mobilization of hematopoietic stem cells.

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