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描述 | Bindarit (AF2838) selectively inhibits monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8, without affecting other CC and CXC chemokines such as MIP-1α/CCL3, MIP-1β/CCL4, and MIP-3/CCL23. It also exhibits anti-inflammatory properties[1]. |
体内研究 | Administered orally at 50 mg/kg daily for varying durations (4, 6, and 8 months) to NZB/W F1 female mice, Bindarit delays the onset of proteinuria and significantly protects against renal function impairment while completely preventing monocyte chemoattractant protein (MCP-1) up-regulation[2]. |
体外研究 | At concentrations of 100 µM and 300 µM, Bindarit significantly reduces platelet-derived growth factor-BB (PDGF-BB)-induced proliferation of rat vascular smooth muscle cells (VSMCs) by 27% and 42%, respectively, after 48 hours[1]. |
Dose | Rat: 12.5 mg/kg[2] (p.o.), 200 mg/kg[3] (p.o.) |
Administration | p.o. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01269242 | Coronary Restenosis | Phase 2 | Completed | - | Italy ... 展开 >> Fondazione S.Raffaele del Monte Tabor - UO Emodinamica e Cardiologia Interventistica Milan, Italy, 20132 收起 << |
NCT01109212 | Diabetic Nephropathy | Phase 2 | Completed | - | Italy ... 展开 >> The Mario Negri Institute for Pharmacological Research- Clinical Research Center for Rare Diseases Ranica, Bergamo, Italy, 24020 Azienda Ospedaliera di Treviglio-Caravaggio - Unità Operativa Malattie Metaboliche e Diabetologia Treviglio, Bergamo, Italy, 24047 Azienda Ospedaliera OO.RR. Bergamo - Unità Operativa Diabetologia Bergamo, Italy, 24128 IRCCS Fondazione Centro S. Raffaele del Monte Tabor- Unità Operativa Medicina Generale Milano, Italy, 20132 Ist. Patologia Medica e metodologia Clinica - Università di Sassari Sassari, Italy, 7100 Slovenia University Medical Center Dpt Endocrinology Diabetes and Metabolic Diseases- Diabetology Unit Ljubljana, Slovenia, 1000 收起 << |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.08mL 0.62mL 0.31mL |
15.41mL 3.08mL 1.54mL |
30.83mL 6.17mL 3.08mL |
CAS号 | 130641-38-2 |
分子式 | C19H20N2O3 |
分子量 | 324.37 |
SMILES Code | CC(OCC1=NN(CC2=CC=CC=C2)C3=C1C=CC=C3)(C)C(O)=O |
MDL No. | MFCD00866723 |
别名 | AF2838 |
运输 | 蓝冰 |
InChI Key | MTHORRSSURHQPZ-UHFFFAOYSA-N |
Pubchem ID | 71354 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, 2-8°C |
溶解方案 |
DMSO: 45 mg/mL(138.73 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
|
动物实验配方 |
IP 2% DMSO+2% Tween80+40% PEG300+water 7 mg/mL clear PO 0.5% CMC-Na 38 mg/mL suspension |