40077-57-4
基本信息
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
VIP【pig】
Apidodil
AVIPTADIL
aviptidal
VIP PORCINE
VIP【rabbit】
VIP USP/EP/BP
Aviptadil Acetate
Aviptadil impurity
物理化學(xué)性質(zhì)
常見問題列表
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。
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。
GPR14
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.
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.