Bindarit-d5 (AF2838-d5) is the deuterium labeled Bindarit. Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8, and no effect on other CC and CXC chemokines such as MIP-1α/CCL3, MIP-1β/CCL4, MIP-3/CCL23. Bindarit also has anti-inflammatory activity[1].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
329.40
Formula
C19H15D5N2O3
中文名称
宾达利 d5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. 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.
[3]. Zoja C, Bindarit retards renal disease and prolongs survival in murine lupus autoimmune disease. Kidney Int. 1998 Mar;53(3):726-34.
Bindarit-d5 (AF2838-d5) is the deuterium labeled Bindarit. Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8, and no effect on other CC and CXC chemokines such as MIP-1α/CCL3, MIP-1β/CCL4, MIP-3/CCL23. Bindarit also has anti-inflammatory activity[1].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
329.40
Formula
C19H15D5N2O3
中文名称
宾达利 d5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. 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.
[3]. Zoja C, Bindarit retards renal disease and prolongs survival in murine lupus autoimmune disease. Kidney Int. 1998 Mar;53(3):726-34.
Bindarit-d5 (AF2838-d5) is the deuterium labeled Bindarit. Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8, and no effect on other CC and CXC chemokines such as MIP-1α/CCL3, MIP-1β/CCL4, MIP-3/CCL23. Bindarit also has anti-inflammatory activity[1].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
329.40
Formula
C19H15D5N2O3
中文名称
宾达利 d5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. 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.
[3]. Zoja C, Bindarit retards renal disease and prolongs survival in murine lupus autoimmune disease. Kidney Int. 1998 Mar;53(3):726-34.
Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8, and no effect on other CC and CXC chemokines such as MIP-1α/CCL3, MIP-1β/CCL4, MIP-3/CCL23. Bindarit also has anti-inflammatory activity[1].
IC50 & Target
MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8[1]
体外研究 (In Vitro)
Bindarit (10-300 μM; 48 hours) at 100 µM and 300 µM significantly inhibits platelet derived growth factor-BB (PDGF-BB)-induced rat VSMCs proliferation by 27% and 42%, respectively[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
VSMC cells
Concentration:
10 μM, 30 μM, 100 μM, 300 μM
Incubation Time:
48 hours
Result:
Inhibited PDGF-BB-induced rat VSMCs proliferation.
体内研究 (In Vivo)
Bindarit (50 mg/kg; oral administration; every day; for 4 months, 6 months, 8 months; NZB/W F1 female mice) delays the onset of proteinuria and significantly protects from renal function impairment. Bindarit completely prevents monocyte chemoattractant protein (MCP-1) up-regulation[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
NZB/W F1 female mice ( two months of age)[2]
Dosage:
50 mg/kg
Administration:
Oral administration; every day; for 4 months, 6 months, 8 months
Result:
Delayed the onset of proteinuria and significantly protected from renal function impairment.
Clinical Trial
分子量
324.37
Formula
C19H20N2O3
CAS 号
130641-38-2
中文名称
宾达利
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. 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.
