产品
编 号：F743564
分子式：C49H63FN10O9
分子量：955.08
分子式：C49H63FN10O9
分子量：955.08
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 1254036-23-1
产品详情
生物活性：
JPE-1375 is a complement C5a receptor 1 (C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 μM) and reduces TNF levels (EC50=4.5 μM) in mice. JPE-1375 can be used in studies of autoimmune and inflammatory diseases.
体内研究：
JPE-1375 (0.3, 1.0, 3.0 mg/kg; i.v.; single) inhibits PMN (polymorphonuclear leukocytes) mobilization and TNF with EC50 values of 6.9 and 4.5 μM, respectively.JPE-1375 (1 mg/kg; i.v.; single) demonstrates a rapid distribution in the plasma, followed by elimination in mice.JPE-1375 (1 mg/kg; i.v.; single) shows a strong negative correlation between PMN mobilization and TNF production with plasma concentrations.Animal Model:C57BL/6J wild-type (10 to 12-week-old; C5a pharmacodynamic model).
Dosage:0.3, 1.0, 3.0 mg/kg
Administration:Intravenous injection; single.
Result:Significantly decreased C5a-mediated PMN mobilization at 1 and 3 mg/kg doses, while no effect was observed at a 0.3 mg/kg dose.Showed a significant reduction in TNF plasma levels at 1 and 3 mg/kg dose with both compounds reducing C5a-mediated TNF by about 90%.
Animal Model:C57BL/6J wild-type mice(10 to 12-week-old).
Dosage:1 mg/kg
Administration:Intravenous injection; single.
Result:1.19Pharmacokinetic Parameters of JPE-1375 in C57BL/6J wild-type mice.IV (1 mg/kg)
T1/2 (h)0.13
Cmax (μg/mL)7.18
AUC0-t (μg/mL?h)2.40
AUC0-inf, obs (μg/mL?h)2.41
AUC0-t/0-inf, obs (μg/mL?h)1.00
AUMC0-inf, obs (μg/mL?h2)0.13
MRT0-inf, obs (h)0.05
Vz, obs ((μg)/(μg/mL))2.38
CL, obs ((μg)/(μg/mL)/h)12.47
Vss, obs ((μg)/(μg/mL))0.66
JPE-1375 is a complement C5a receptor 1 (C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 μM) and reduces TNF levels (EC50=4.5 μM) in mice. JPE-1375 can be used in studies of autoimmune and inflammatory diseases.
体内研究：
JPE-1375 (0.3, 1.0, 3.0 mg/kg; i.v.; single) inhibits PMN (polymorphonuclear leukocytes) mobilization and TNF with EC50 values of 6.9 and 4.5 μM, respectively.JPE-1375 (1 mg/kg; i.v.; single) demonstrates a rapid distribution in the plasma, followed by elimination in mice.JPE-1375 (1 mg/kg; i.v.; single) shows a strong negative correlation between PMN mobilization and TNF production with plasma concentrations.Animal Model:C57BL/6J wild-type (10 to 12-week-old; C5a pharmacodynamic model).
Dosage:0.3, 1.0, 3.0 mg/kg
Administration:Intravenous injection; single.
Result:Significantly decreased C5a-mediated PMN mobilization at 1 and 3 mg/kg doses, while no effect was observed at a 0.3 mg/kg dose.Showed a significant reduction in TNF plasma levels at 1 and 3 mg/kg dose with both compounds reducing C5a-mediated TNF by about 90%.
Animal Model:C57BL/6J wild-type mice(10 to 12-week-old).
Dosage:1 mg/kg
Administration:Intravenous injection; single.
Result:1.19Pharmacokinetic Parameters of JPE-1375 in C57BL/6J wild-type mice.IV (1 mg/kg)
T1/2 (h)0.13
Cmax (μg/mL)7.18
AUC0-t (μg/mL?h)2.40
AUC0-inf, obs (μg/mL?h)2.41
AUC0-t/0-inf, obs (μg/mL?h)1.00
AUMC0-inf, obs (μg/mL?h2)0.13
MRT0-inf, obs (h)0.05
Vz, obs ((μg)/(μg/mL))2.38
CL, obs ((μg)/(μg/mL)/h)12.47
Vss, obs ((μg)/(μg/mL))0.66
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