Aviptadil(Synonyms: 阿肽地尔 Vasoactive Intestinal Peptide (human, rat, mouse, rabbit, canine, porcine))

Aviptadil;(Synonyms: 阿肽地尔; Vasoactive Intestinal Peptide (human, rat, mouse, rabbit, canine, porcine))

Aviptadil 是一种血管活性肠多肽 (VIP) 类似物,具有强的血管舒张 (vasodilatory) 作用。Aviptadil 诱导肺血管扩张,抑制血管 SMCs 增殖、血小板聚集。Aviptadil 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。

Aviptadil (Synonyms: 阿肽地尔; Vasoactive Intestinal Peptide (human, rat, mouse, rabbit, canine, porcine))

Aviptadil Chemical Structure

CAS No. : 40077-57-4

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1 mg ¥1200 In-stock
5 mg ¥2500 In-stock
10 mg ¥3500 In-stock
50 mg ¥6500 In-stock
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生物活性

Aviptadil is an analog vasoactive intestinal polypeptide (VIP) with potent vasodilatory effects. Aviptadil induces pulmonary vasodilation and inhibits vascular SMCs proliferation, platelet aggregation. Aviptadil can be used for the research of pulmonary fibrosis, pulmonary arterial hypertension (PAH) and SARS-CoV-2 caused respiratory failure, et al[1][2].

体外研究
(In Vitro)

Aviptadil 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[3].
Aviptadil (1 nM-10 μM) produces a concentration-dependent inhibition of CSE-induced cell death in L2 cells. At 10 μM, Aviptadil reduces CSE-stimulated MMP activity and caspase-3 activation in L2 cells[3].
Aviptadil (10 nM-100 μM) attenuates lipopolisaccharide (LPS)-induced MMP-9 activity and its expression by alveolar macrophages (AM) in rats[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Aviptadil (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[3].
Aviptadil (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[3].
Nose-only inhalation exposure of CD1 mice to aerosolized.
Aviptadil 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

3325.80

Formula

C147H238N44O42S

CAS 号

40077-57-4

Sequence Shortening

HSDAVFTDNYTRLRKQMAVKKYLNSILN-NH2

中文名称

阿肽地尔

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro:;

H2O : 33.33 mg/mL (10.02 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.3007 mL 1.5034 mL 3.0068 mL
5 mM 0.0601 mL 0.3007 mL 0.6014 mL
10 mM 0.0301 mL 0.1503 mL 0.3007 mL

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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Intravenous Aviptadil for Critical COVID-19 With Respiratory Failure (COVID-AIV)

    [2]. Jian Hu, et al. Novel Targets of Drug Treatment for Pulmonary Hypertension. Am J Cardiovasc Drugs

    [3]. INVESTIGATOR’S BROCHURE Sponsor: NeuroRx, Inc