1、Product Data SheetBindaritCat. No.: HY-B0498CAS No.: 130641-38-2分式: CHNO分量: 324.37作靶點(diǎn): CCR作通路: GPCR/G Protein; Immunology/Inflammation儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 46 mg/mL (141.81 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 m

2、g 10 mgConcentration制備儲(chǔ)備液1 mM 3.0829 mL 15.4145 mL 30.8290 mL5 mM 0.6166 mL 3.0829 mL 6.1658 mL10 mM 0.3083 mL 1.5414 mL 3.0829 mL請(qǐng)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(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊?qǐng)先按照 In

3、 Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.67 mg/mL (8.23 mM); Clear solution此案可獲得 2.67 mg/mL (8.23 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L

4、26.7 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.67 mg/mL (8.23 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.67 mg/mL (8.23 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 26.7 mg/mL 的澄 DMSO 儲(chǔ)備液加到 90

5、0 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.67 mg/mL (8.23 mM); Clear solution; Need warming此案可獲得 2.67 mg/mL (8.23 mM) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 26.7 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Bindarit (AF2838)單核細(xì)胞趨化蛋 MCP-1/CCL2，MCP-3

6、/CCL7 和 MCP-2/CCL8 的選擇性抑制劑，對(duì)其他趨化因如 MIP-1/CCL3，MIP-1/CCL4，MIP-3/CCL23 抑制作。Bindarit 還具有抗炎作。IC & Target MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL81體外研究 Bindarit (10-300 M; 48 hours) at 100 M and 300 M significantly inhibits platelet derived growth factor-BB (PDGF-BB)-induced rat VSMCs proliferation by 27%

7、and 42%, respectively1.Cell Viability Assay1Cell Line: VSMC cellsConcentration: 10 M, 30 M, 100 M, 300 MIncubation Time: 48 hoursResult: Inhibited PDGF-BB-induced rat VSMCs proliferation.體內(nèi)研究 Bindarit (50 mg/kg; oral administration; every day; for 4 months, 6 months, 8 months; NZB/W F1 female mice)

8、delaysthe onset of proteinuria and significantly protects from renal function impairment. Bindarit completely preventsmonocyte chemoattractant protein (MCP-1) up-regulation2.Animal Model: NZB/W F1 female mice ( two months of age)2Dosage: 50 mg/kgAdministration: Oral administration; every day; for 4

9、months, 6 months, 8 monthsResult: Delayed the onset of proteinuria and significantly protected from renal functionimpairment.REFERENCES1. Grassia, G., et al., The anti-inflammatory agent bindarit inhibits neointima formation in both rats and hyperlipidaemic mice. Cardiovasc Res, 2009. 84(3):p. 485-93.2. Zoja C, Bindarit retards renal disease and prolongs survival in murine lupus autoimmune disease. Kidney Int. 1998 Mar;53(3):726-34.McePdfHeightPage 2 of 3 www.MedChemECaution: Product has not been fully validated for medical applicati