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上海源葉生物科技有限公司
主營產(chǎn)品： S30260異硫氰酸胍,30259鹽酸胍,嗜熱菌蛋白酶 |
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15921386130
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- 聯(lián)系人：
- 何小姐
- 電話：
- 86-021-61559134
- 手機：
- 15921386130
- 傳真：
- 86-021-55068248
- 地址：
- 上海市松江區(qū)長塔路465號6幢
- 郵編：
- 200433
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- www.shyuanye.com
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更新時間：2025-05-15 21:32:47瀏覽次數(shù)：144
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- 產(chǎn)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
- 靶點： 125I-CXCL12-CXCR4:44 nM (IC50);125I-CXCL12-CXCR7;HIV-1:1-10 nM (EC50);HIV-2:1-10 nM (EC50)
- 體內(nèi)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.
- 參考文獻：
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.
- 溶解度： 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)
- 保存條件： -20℃
- 配置溶液濃度參考：
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：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的性，僅供客戶參考交流研究之用。
