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40077-57-4

中文名稱 醋酸阿肽地爾
英文名稱 VIP
CAS 40077-57-4
分子式 C147H238N44O42S
分子量 3325.8
MOL 文件 40077-57-4.mol
更新日期 2024/10/29 09:41:23
40077-57-4 結(jié)構(gòu)式 40077-57-4 結(jié)構(gòu)式

基本信息

中文別名
阿肽地爾
血管活性腸肽
醋酸阿肽地爾
阿肽地爾雜質(zhì)
利尿肽II,鼠
血管活性腸肽(抗體)
血管活性腸肽/阿肽地爾
血管活性腸肽(人,豬,鼠)
阿肽地爾, ≥95% (HPLC)
醋酸阿肽地爾 40077-57-4
英文別名
VIP
VIP【pig】
Apidodil
AVIPTADIL
aviptidal
VIP PORCINE
VIP【rabbit】
VIP USP/EP/BP
Aviptadil Acetate
Aviptadil impurity
所屬類別
生物化工:多肽

物理化學(xué)性質(zhì)

密度1.47±0.1 g/cm3(Predicted)
儲存條件−20°C
儲存條件−20°C
溶解度1%醋酸:可溶0.1%,澄清,無色
形態(tài)powder
顏色White to off-white
水溶解性Soluble to 1 mg/ml in water
序列His-Ser-Asp-Ala-Val-Phe-Thr-Asp-Asn-Tyr-Thr-Arg-Leu-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Asn-Ser-Ile-Leu-Asn-NH2
InChIKeyHEOYHMUESMJFDC-RIWXPGAOSA-N

安全數(shù)據(jù)

WGK Germany3
WGK Germany3

常見問題列表

概述

醋酸阿肽地爾是一種活性多肽為從小腸粘膜提取的一種直鏈肽。由28個氨基酸殘基組成,其排列為一部分胰高血糖素(glucagon)和催胰液素(secretin),具有可使血管舒張降低血壓的作用。從肝動脈開始,對內(nèi)臟血管具有較強(qiáng)的作用能力,但對股動脈則全無作用。對腸液的分泌具有很強(qiáng)的促進(jìn)作用,但對胰腺的分泌其促進(jìn)作用很弱,對胃液的分泌可起抑制作用,對消化道平滑肌的收縮產(chǎn)生抑制作用。

應(yīng)用

醋酸阿肽地爾為Mondobiotech AG和Biogen Idec公司開發(fā)出來,是由28個氨基酸組成的線性肽,主要用于急性呼吸窘迫綜合癥和特發(fā)性肺纖維化治療,其效果較好且副作用小,是一種很有市場前景的多肽藥物。

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

GPR14

體外研究

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.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.Aviptadil (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 (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 (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 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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