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Aviptadil acetate

CAS No. : 1444827-29-5

MCE 站：Aviptadil acetate

产品活性：Aviptadil acetate 是一种模拟血管活性肠多肽 (VIP) 类似物，具有强的血管舒张 (vasodilatory) 效应。。Aviptadil acetate 诱导肺血管扩张，抑制血管 SMCs 增殖、血小板聚集。Aviptadil acetate 可用于肺纤维化、肺动脉高压 (PAH)、SARS-CoV-2 引起呼吸衰竭等的研究。

研究领域：Anti-infection

作用靶点：SARS-CoV

In Vitro: Aviptadil acetate inhibits the basal proliferation of pulmonary arterial smooth muscle cells (PASMC) ａnd the mobilization of intracellular free calcium concentration in these cells in a dose-dependent manner.
Aviptadil acetate (1 nM-10 μM) produces a concentration-dependent inhibition of CSE-induced cell death in L2 cells. At 10 μM, Aviptadil acetate reduces CSE-stimulated MMP activity ａnd caspase-3 activation in L2 cells.
Aviptadil acetate (10 nM-100 μM) attenuates lipopolisaccharide (LPS)-induced MMP-9 activity ａnd its expression by alveolar macrophages (AM) in rats.

In Vivo: Aviptadil acetate (1, 3 ａnd 10 mg/kg; intravenous bolus injection) is injected into a tail vein. No-effect dose level is 1 mg/kg. Dose level with first intolerance reactions 3 mg/kg, Lowest lethal dose level is >10 mg/kg. i.v. LD₅₀ of Aviptadil is >10 mg/kg in males, females ａnd male ａnd female combined after 24 hours ａnd 14 days.
Aviptadil acetate (intravenous bolus injection) at 3 mg causes slightly reduced motility, slight ataxia ａnd slight dyspnoea in all 5 male ａnd 5 female animals 15 to 30 minutes after administration. At 10 mg, Aviptadil reveals slightly reduced motility, slight ataxia, ａnd slight dyspnoea 15 to 60 minutes ａnd slightly reduces muscle tone 15 to 30 minutes after administration, respectively, in all male ａnd female animals.
Nose-only inhalation exposure of CD1 mice to aerosolized.
Aviptadil acetate at a dose of 1546 µg/kg/day is well tolerated ａnd produces no apparent changes in any of the parameters evaluated. No changes are observed after a single dose administration as high as 3920 µg/kg/day. The no-observable-adverse-effect level (NOAEL) is considered to be at least 3920 µg/kg/day fore an acute exposure ａnd 1546 µg/kg/day for a 10 day repeated exposure.

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