Plerixafor (AMD3100, JM 3100, SID791)是一种趋化因子受体拮抗剂，作用于CXCR4和CXCL12介导的趋化性，无细胞试验中IC50分别为44 nM和5.7 nM。Plerixafor 可抑制human immunodeficiency virus (HIV)复制。
| CAS No. | 110078-46-1 |
| 生物活性 | Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM. |
| 分子式 | C28H54N8 |
| 分子量 | 502.78 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -20°C 3 years |
| 溶解性数据 | Ethanol : 50 mg/mL (99.45 mM; Need ultrasonic) DMSO : 1.92 mg/mL (3.82 mM; ultrasonic and warming and adjust pH to 7 with 1 M HCL and heat to 60°C) H2O : < 0.1 mg/mL (ultrasonic) (insoluble) |
| 体内研究 | Plerixafor (2 mg/kg) administration to UUO mice exacerbates renal interstitial T cell infiltration, resulting in increased production of the pro-inflammatory cytokines IL-6 and IFN-γ and decreased expression of the anti-inflammatory cytokine IL-10. Both perivascular and interstitial fibrosis are significantly reduced by the CXCR4 antagonist, Plerixafor (AMD3100) at 8 weeks. LD50, mouse, SC: 16.3 mg/kg; LD50, rat, SC: >50 mg/kg; LD50, mouse and rat, IV injection: 5.2 mg/kg. |
| 体外研究 | The CXCR4 inhibitor Plerixafor (AMD3100) is a potent inhibitor of CXCL12-mediated chemotaxis (IC50, 5.7 nM) with a potency slightly better than its affinity for CXCR4. Plerixafor interferes with the interaction of CXCR4 with its natural ligand, SDF-1 (CXCL12). Treating the cells with CCX771 or CXCL11 has no effect on CXCL12-mediated MOLT-4 or U937 TEM. In contrast, 10 μM Plerixafor inhibits CXCL12-mediated TEM in both cells lines . Plerixafor prevents the infiltration of tumor-associated macrophages (TAMs) into the tumor tissues. |
| 纯度及产品资料 | ≥98% |
邮箱：info@TianyaBio.com
电话：020-3107 8154
地址：广州市番禺区兴业大道东路1078号2-50
微信公众号
微信客服
