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PL-3994

CAS No. : 952295-80-6

MCE 站：PL-3994

产品活性：PL-3994 是一种利钠肽受体 NPR-A 激动剂，对中性肽酶具有耐药性，并是一种支气管扩张剂。PL-3994 对预收缩豚鼠气管产生浓度依赖性弛豫，IC₅₀ 为 42.7 nM。

研究领域：Others

作用靶点：Others

In Vitro: PL-3994 has high affinity for recombinant human, dog, or rat NPR-As with K_i values of 1 nM, 41 nM, 10 nM, respectively. And PL-3994 binds to hNPR-C with K_i 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).

In Vivo: 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).

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