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1444827-29-5

中文名稱 醋酸阿肽地爾
英文名稱 Aviptadil acetate
CAS 1444827-29-5
1444827-29-5 結(jié)構(gòu)式 1444827-29-5 結(jié)構(gòu)式

基本信息

英文別名
Vasoactive Intestinal Peptide acetate salt
所屬類別
生物化工:多肽

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C, protect from light
溶解度DMSO: 100 mg/mL (29.53 mM)
形態(tài)Solid
顏色White to off-white
水溶解性Water: < 0.1 mg/mL (insoluble)

常見問題列表

生物活性
Aviptadil acetate 是一種模擬血管活性腸多肽 (VIP) 類似物,具有強(qiáng)的血管舒張 (vasodilatory) 效應(yīng)。。Aviptadil acetate 誘導(dǎo)肺血管擴(kuò)張,抑制血管 SMCs 增殖、血小板聚集。Aviptadil acetate 可用于肺纖維化、肺動(dòng)脈高壓 (PAH)、SARS-CoV-2 引起呼吸衰竭等的研究。
體外研究

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.

體內(nèi)研究

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. LD 50 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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