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

Aviptadil acetate;(Synonyms: 醋酸阿肽地尔; Vasoactive Intestinal Peptide acetate salt (human, rat, mouse, rabbit, canine, porcine)) 纯度: 99.09%

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。

Aviptadil acetateamp;;(Synonyms: 醋酸阿肽地尔; Vasoactive Intestinal Peptide acetate salt (human, rat, mouse, rabbit, canine, porcine))

Aviptadil acetate Chemical Structure

CAS No. : 1444827-29-5

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生物活性

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

体外研究
(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[3].
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[1].
Aviptadil acetate (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 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[3].
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[3].
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[3].

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

Clinical Trial

分子量

3385.90

Formula

C147H238N44O42S.C2H4O2

CAS 号

1444827-29-5

Sequence Shortening

HSDAVFTDNYTRLRKQMAVKKYLNSILN-NH2

中文名称

醋酸阿肽地尔;醋酸阿维他定

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro:;

H2O : 100 mg/mL (29.53 mM; Need ultrasonic)

DMSO : 100 mg/mL (29.53 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.2953 mL 1.4767 mL 2.9534 mL
5 mM 0.0591 mL 0.2953 mL 0.5907 mL
10 mM 0.0295 mL 0.1477 mL 0.2953 mL

*

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 (sealed storage, away from moisture and light)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂:;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.5 mg/mL (0.74 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (0.74 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂:;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (0.74 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (0.74 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂:;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (0.74 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (0.74 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
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