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• 产品描述： 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

• 靶点： 125I-CXCL12-CXCR4:44 nM (IC50);125I-CXCL12-CXCR7;HIV-1:1-10 nM (EC50);HIV-2:1-10 nM (EC50);VirusProtease;HIVProtease;CXCR

• 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.

• 参考文献：
  1. Yang J, et al. Continuous AMD3100 Treatment Worsens Renal Fibrosis through Regulation of Bone Marrow Derived Pro-Angiogenic Cells Homing and T-Cell-Related Inflammation. PLoS One. 2016 Feb 22;11(2):e0149926.2. Seki JT, et al. Chemical Stability of Plerixafor after Opening of Single-Use Vial. Can J Hosp Pharm. 2017 Jul-Aug;70(4):270-275. 3. Zabel BA, et al. Elucidation of CXCR7-mediated signaling events and inhibition of CXCR4-mediated tumor cell transendothelial migration by CXCR7 ligands. J Immunol. 2009 Sep 1;183(5):3204-11. 4. De Clercq E, et al. Mozobil® (Plerixafor, AMD3100), 10 years after its approval by the US Food and Drug Administration. Antivir Chem Chemother. 2019 Jan-Dec;27:2040206619829382. 5. Mercurio L, et al. Targeting CXCR4 by a selective peptide antagonist modulates tumor microenvironment and microglia reactivity in a human glioblastoma model. J Exp Clin Cancer Res. 2016 Mar 25;35:55. 6. Chu PY, et al. CXCR4 Antagonism Attenuates the Development of Diabetic Cardiac Fibrosis. PLoS One. 2015 Jul 27;10(7):e0133616. 7. Schols D, et al. HIV co-receptor inhibitors as novel class of anti-HIV drugs. Antiviral Res. 2006 Sep;71(2-3):216-26. 8. Zheng J, et al. Toward Normalization of the Tumor Microenvironment for Cancer Therapy. Integr Cancer Ther. 2019;18:1534735419862352.

• 溶解性： Ethanol  :  50  mg/mL  (99.45  mM;  Need  ultrasonic)    DMF  :  1  mg/mL  (1.99  mM;  Need  ultrasonic)    H2O  :  1  mg/mL  (1.99  mM;  Need  ultrasonic)    DMSO  :  1  mg/mL  (1.99  mM;  ultrasonic  and  warming  and  heat  to  60°C)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.989 ml	9.945 ml	19.889 ml
  5 mM	0.398 ml	1.989 ml	3.978 ml
  10 mM	0.199 ml	0.994 ml	1.989 ml
  50 mM	0.04 ml	0.199 ml	0.398 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *