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编 号：F761773
分子式：C82H127N27O20S2
分子量：1875.18
分子式：C82H127N27O20S2
分子量：1875.18
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CAS No: 952295-80-6
产品详情
生物活性：
PL-3994 is a natriuretic peptide receptor-A (NPR-A) agonist that is resistant to neutral endopeptidase and acts as a bronchodilator. PL-3994 produces concentration-dependent relaxation of pre-contracted guinea-pig trachea with an IC50 value of 42.7 nM.
体内研究：
Intratracheal PL-3994 (1-1000 mg/kg; i.t.; single dose) produces a dose-dependent inhibition of the bronchoconstrictor response evoked by aerosolized methacholine, without significant effect on cardiovascular parameters.PL-3994 is resistant to degradation by human neutral endopeptidase (hNEP) (92% remaining after 2 h), whereas the natural ligands, ANP and CNP, are rapidly metabolized (≤1% remaining after 2 h).Animal Model:Guinea-pig model anaesthetized with urethane (1.75 g/kg, i.p.)
Dosage:1, 10, 100, 1000 mg/kg
Administration:Intrathecal; single dose
Result:Resulted a significant maximum inhibition of 43%, 63% and 70%, respectively, observed after 15-min pretreatment at doses of 10, 100 and 1000 mg/kg.
体外研究：
PL-3994 has high affinity for recombinant human, dog, or rat NPR-As with Ki values of 1 nM, 41 nM, 10 nM, respectively. And PL-3994 binds to hNPR-C with Ki of 7 nM, while there is no effect on cGMP generation in hNPR-B.PL-3994 induces dose-dependent cGMP generation in human, dog, and rat NPR-As with EC50s of 2 nM, 3 nM, and 14 nM, respectively.PL-3994 (0.1 nM-100 mM; 5-20 min) elicits a potent, concentration-dependent but small relaxation of pre-contracted human precision-cut lung slices (hPCLS).
PL-3994 is a natriuretic peptide receptor-A (NPR-A) agonist that is resistant to neutral endopeptidase and acts as a bronchodilator. PL-3994 produces concentration-dependent relaxation of pre-contracted guinea-pig trachea with an IC50 value of 42.7 nM.
体内研究：
Intratracheal PL-3994 (1-1000 mg/kg; i.t.; single dose) produces a dose-dependent inhibition of the bronchoconstrictor response evoked by aerosolized methacholine, without significant effect on cardiovascular parameters.PL-3994 is resistant to degradation by human neutral endopeptidase (hNEP) (92% remaining after 2 h), whereas the natural ligands, ANP and CNP, are rapidly metabolized (≤1% remaining after 2 h).Animal Model:Guinea-pig model anaesthetized with urethane (1.75 g/kg, i.p.)
Dosage:1, 10, 100, 1000 mg/kg
Administration:Intrathecal; single dose
Result:Resulted a significant maximum inhibition of 43%, 63% and 70%, respectively, observed after 15-min pretreatment at doses of 10, 100 and 1000 mg/kg.
体外研究：
PL-3994 has high affinity for recombinant human, dog, or rat NPR-As with Ki values of 1 nM, 41 nM, 10 nM, respectively. And PL-3994 binds to hNPR-C with Ki of 7 nM, while there is no effect on cGMP generation in hNPR-B.PL-3994 induces dose-dependent cGMP generation in human, dog, and rat NPR-As with EC50s of 2 nM, 3 nM, and 14 nM, respectively.PL-3994 (0.1 nM-100 mM; 5-20 min) elicits a potent, concentration-dependent but small relaxation of pre-contracted human precision-cut lung slices (hPCLS).
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