产品
编 号：F755671
分子式：C28H28ClFN6O3
分子量：551.01
分子式：C28H28ClFN6O3
分子量：551.01
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CAS No: 2762567-70-2
产品详情
生物活性：
APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease.
体内研究：
Assessment of Pharmacokinetics (PK) profile of APJ receptor agonist 4 (compound 21) in mouse.speciesratmonkeydogmax (ng/mL)
dose (mg/kg)1 (i.v. and p.o.)1 (i.v.) and 3 (p.o.)1 (i.v. and p.o.)
vehiclea FGG
CI (mL/min/kg)4.610.62.4
VSS (L/kg)1.60.20.2
T1/2 (h)4.01.32.5
Cmax (μM?h)2.21.46.5
AUC0-24 (μM?h)3.72.514.2
F (%)542776
a: Vehicle F: 5/5/90 v/v/v DMAC/Cremophor EL/sodium carbonate buffer, pH 9 and vehicle G: 10/40/50 v/v/v ethanol/PEG400/sodium carbonate buffer, pH 9.
APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease.
体内研究：
Assessment of Pharmacokinetics (PK) profile of APJ receptor agonist 4 (compound 21) in mouse.speciesratmonkeydogmax (ng/mL)
dose (mg/kg)1 (i.v. and p.o.)1 (i.v.) and 3 (p.o.)1 (i.v. and p.o.)
vehiclea FGG
CI (mL/min/kg)4.610.62.4
VSS (L/kg)1.60.20.2
T1/2 (h)4.01.32.5
Cmax (μM?h)2.21.46.5
AUC0-24 (μM?h)3.72.514.2
F (%)542776
a: Vehicle F: 5/5/90 v/v/v DMAC/Cremophor EL/sodium carbonate buffer, pH 9 and vehicle G: 10/40/50 v/v/v ethanol/PEG400/sodium carbonate buffer, pH 9.
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