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Plerixafor (AMD-3329) 是一种趋化因子受体拮抗剂,可阻断基质细胞衍生因子与细胞受体 CXCR4 的结合。它也是 CXCR7 的变构激动剂,是免疫刺激剂和造血干细胞动员剂,还抑制HIV-1和HIV-2的复制,EC50为 1-10 nM。
Plerixafor (AMD-3329) 是一种趋化因子受体拮抗剂,可阻断基质细胞衍生因子与细胞受体 CXCR4 的结合。它也是 CXCR7 的变构激动剂,是免疫刺激剂和造血干细胞动员剂,还抑制HIV-1和HIV-2的复制,EC50为 1-10 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 163 | 现货 | |
5 mg | ¥ 343 | 现货 | |
10 mg | ¥ 572 | 现货 | |
25 mg | ¥ 982 | 现货 | |
50 mg | ¥ 1,680 | 现货 | |
100 mg | ¥ 2,960 | 现货 | |
200 mg | ¥ 4,280 | 现货 | |
500 mg | ¥ 6,550 | 现货 |
产品描述 | Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4. |
靶点活性 | CXCL12:5.7 nM, CXCR4:44 nM |
体外活性 | Plerixafor以略优于其对CXCR4亲和力的效力,抑制了CXCL12介导的趋化作用。[1] Plerixafor还以IC50为651 nM对SDF-1/CXCL12配体结合产生拮抗作用。对于SDF-1介导的GTP结合、SDF-1介导的钙流和SDF-1刺激的趋化作用,Plerixafor的IC50分别为27 nM、572 nM和51 nM。Plerixafor不抑制表达CXCR3、CCR1、CCR2b、CCR4、CCR5或CCR7的细胞在其相应配体刺激下的钙流,也不抑制LTB4的受体结合。Plerixafor本身不在表达多种GPCRs(包括CXCR4、CCR4和CCR7)的CCRF-CEM细胞中诱导钙流。[2] |
体内活性 | 单次局部施用Plerixafor能通过增加细胞因子产生、动员骨髓EPCs、增强成纤维细胞和单核细胞/巨噬细胞的活性,从而促进糖尿病小鼠的伤口愈合,同时增加血管生成和血管形成。[3] 小鼠连续五天被给予PBS、IGF1、PDGF、SCF或VEGF,并在第5天给予Plerixafor。与PDGF、SCF和VEGF处理组相比,IGF1加Plerixafor注射的小鼠群体中,克隆的数量和大小最大。[4] |
激酶实验 | In vitro biochemical assays against histone acetylases: GSK503 is profiled to assess inhibition against a panel of histone acetylases. GSK503 is dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM, with a final DMSO concentration of 2%. Anacardic Acid is used as positive control for CBP, GCN5, and pCAF and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Curcumin is used as positive control for KAT5, MYST2/KAT7, MYST4/KAT6B, and p300, and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Reactions are carried out at 3.08 μM Acetyl-CoA. For CBP, GCN5, MYST2/KAT7, pCAF, and p300, the substrate used is histone H3. For KAT5 and MYST4/KAT6B the substrates used are histone H2A and histone H4, respectively. |
细胞实验 | Plerixafor is dissolved in DMSO and then diluted with appropriate medium[2]. U87 mg cells are seeded in 96-well plates at the density of 6×103 cells in 200 μL/well and treated with CXCL12, Plerixafor or with peptide R, as described in the previous "Treatments" section. MTT (5 μg/mL) is added at each time point (24, 48, 72 h) during the final 2 h of treatment. After removing cell medium, 100 μL DMSO are added and optical densities measured at 595 nm with a LT-4000MS Microplate Reader. Measurements are made in triplicates from three independent experiments[2]. |
别名 | 普乐沙福, JM3100, AMD-3329, AMD 3100 |
分子量 | 502.78 |
分子式 | C28H54N8 |
CAS No. | 110078-46-1 |
Smiles | C(N1CCCNCCNCCCNCC1)c1ccc(CN2CCCNCCNCCCNCC2)cc1 |
密度 | 0.962 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||
溶解度信息 | PBS: 1 mg/mL (1.98 mM), Sonication is recommended. Ethanol: 50 mg/mL, Sonication is recommended. DMSO: < 1 mg/mL (insoluble), Sonication is recommended. H2O: Insoluble | ||||||||||
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