Plerixafor-AMD-3100-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPlerixaforCat. No.: HY-10046CAS No.: 110078-46-1Synonyms: AMD 3100; JM3100; SID791分式: CHN分量: 502.78作靶點: CXCR作通路: GPCR/G Protein; Immunology/Inflammation儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體

2、外實驗 Ethanol : 166.66 mg/mL (331.48 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.9889 mL 9.9447 mL 19.8894 mL5 mM 0.3978 mL 1.9889 mL 3.9779 mL10 mM 0.1989 mL 0.9945 mL 1.9889 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 Plerixafor (AMD3100) is

3、 prepared in vehicle (normal saline)5. Plerixafor (AMD3100) is dissolved in DMSOand in sterile PBS for animal administration6.BIOLOGICAL ACTIVITY物活性 Plerixafor (AMD 3100)是選擇性的 CXCR4 拮抗劑，IC50值為44 nM。1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEIC50 & Target 125I-CXCL12-CXCR444 nM (IC50)體外研究 The C

4、XCR4 inhibitor Plerixafor (AMD3100) is a potent inhibitor of CXCL12-mediated chemotaxis (IC50, 5.7nM) with a potency slightly better than its affinity for CXCR4. Treating the cells with CCX771 or CXCL11 hasno effect on CXCL12-mediated MOLT-4 or U937 TEM. In contrast, 10 M Plerixafor inhibits CXCL12-

5、mediated TEM in both cells lines 1. Plerixafor (10 M)-treated cells show a moderate reduction in cellproliferation compared to CXCL12-stimulated cells, which do not reach statistical significance 2.體內(nèi)研究 Plerixafor (2 mg/kg) administration to UUO mice exacerbates renal interstitial T cell infiltratio

6、n, resulting inincreased production of the pro-inflammatory cytokines IL-6 and IFN- and decreased expression of the anti-inflammatory cytokine IL-10 3. Both perivascular and interstitial fibrosis are significantly reduced by theCXCR4 antagonist, Plerixafor (AMD3100) at 8 weeks 4. LD50, mouse, SC: 16

7、.3 mg/kg; LD50, rat, SC: 50mg/kg; LD50, mouse and rat, IV injection: 5.2 mg/kg.PROTOCOLCell Assay 2 U87MG cells are seeded in 96-well plates at the density of 6103 cells in 200 L/well and treated withCXCL12, Plerixafor or with peptide R. MTT (5 g/mL) is added at each time point (24, 48, 72 h) during

8、 thefinal 2 h of treatment. After removing cell medium, 100 L DMSO are added and optical densities measuredat 595 nm with a LT-4000MS Microplate Reader. Measurements are made in triplicates from threeindependent experiments 2.MCE has not independently confirmed the accuracy of these methods. They ar

9、e for reference only.Animal Mice 3Administration 34 Male C57bl/6 mice (6-7 weeks old, weighing 20 g) are used. The animals are acclimated to the housingenvironment, which is SPF and had a temperature of 22C and a 12h/12h light/dark cycle for a week. Then,they are randomly divided into following expe

10、rimental groups, with 8 mice in each group: normal (no specificintervention), UUO+AMD3100 (mice received UUO surgery and 2 mg/kg AMD3100), and UUO+PBS (micereceived UUO surgery and the same volume of PBS). AMD3100 and PBS are administered viaintraperitoneal injection every day until sacrifice.Rats 4

11、The CXCR4 antagonist, AMD3100 dissolved in H2O, is delivered in the type 2 diabetic sand rat model at adose of 6 mg/kg per day for 8 weeks. In complementary studies, the effect of CXCR4 antagonism (AMD31006mg/kg/d) on regulatory T cell numbers is examined. For these studies, AMD3100 or vehicle is de

12、livered viaminipump for a period of one week.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Mol Immunol. 2019 Jul 18. Oncogene. 2019 Jun;38(25):5021-5037. Brain Behav Immun. 2017 Jan;59:322-332.2/3 Master of Small Molecules 您邊的抑制劑師www.

13、MedChemE Cell Death Dis. 2017 Jan 19;8(1):e2560. Cells. 2019 Jul 22;8(7). pii: E761.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Zabel BA, et al. Elucidation of CXCR7-mediated signaling events and inhibition of CXCR4-mediated tumor cell transendothelialmigration by CXCR7 lig

14、ands. J Immunol. 2009 Sep 1;183(5):3204-11.2. Mercurio L, et al. Targeting CXCR4 by a selective peptide antagonist modulates tumor microenvironment and microglia reactivity in ahuman glioblastoma model. J Exp Clin Cancer Res. 2016 Mar 25;35:55.3. Yang J, et al. Continuous AMD3100 Treatment Worsens R

15、enal Fibrosis through Regulation of Bone Marrow Derived Pro-AngiogenicCells Homing and T-Cell-Related Inflammation. PLoS One. 2016 Feb 22;11(2):e0149926.4. Chu PY, et al. CXCR4 Antagonism Attenuates the Development of Diabetic Cardiac Fibrosis. PLoS One. 2015 Jul 27;10(7):e0133616.5. He G, et al. SDF-1 in Mammary Fibroblasts of Bovine with Mastitis Induces EMT and Inflammatory Response of Epithelial Cells. Int JBiol Sci. 2017 May 5;13(5):604-614.6. Wei He, et al. Targeting CXC motif chemokine receptor 4 inhibits the proliferation, migration and angiogenesis of lung cancer cell