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40077-57-4

  • Product NameAviptadil
  • Molecular FormulaC147H238N44O42S
  • Molecular Weight3325.80
  • Purity99%
  • Appearancepowder
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  • CasNo: 40077-57-4
  • Molecular Formula: C147H238N44O42S
  • Appearance: powder
  • Purity: 99%

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  • Molecular Formula:C147H238N44O42S
  • Molecular Weight:3325.80
  • Appearance/Colour:powder 
  • PSA:1478.99000 
  • Density:1.47±0.1 g/cm3(Predicted) 
  • LogP:4.02270 

Aviptadil(Cas 40077-57-4) Usage

Discovery

VIP is a neuropeptide consisting of 28 aa residues, with wide distribution in the central and peripheral nervous systems. VIP has a broad spectrum of biologic actions, and acts as a neurotransmitter or neuromodulator and also as a hormone.?VIP was first discovered as a smooth muscle-relaxant vasodilator peptide in the lung; it was isolated from the porcine intestine in 1970. Its original label as a “candidate gastrointestinal hormone” was soon replaced by its new and apparently true identity as a neuropeptide with neurotransmitter and neuromodulator properties.

Structure

VIP possesses two segments of secondary structures: a random coil structure in the N-terminal region between positions 1 and 9, and a long α-helical structure in the C-terminal region stretching from position 10 to its C-terminus.?The primary structure of VIP is highly conserved in vertebrates with complete identity among mammals except for the guinea pig and opossum.?Mr 3326, pI >11. VIP is soluble in water to 20mg/mL.

Gene, mRNA, and precursor

The human VIP gene, VIP, location 6q25.2, contains seven exons. Each exon encodes a distinct functional domain of the VIP precursor. The VIP precursor polypeptide (preproVIP) contains several additional biologically active peptides, including peptide histidine isoleucine (PHI, found in nonhuman mammals), peptide histidine methionine (PHM, the human equivalent of PHI), and peptide histidine valine (PHV, a C-terminally extended form of PHI and PHM).

Synthesis and release

VIP gene expression is stimulated by dibutyryl cAMP and by increased PKC activity induced by tumorpromoting phorbol esters. When acting together, cAMP and phorbol esters synergistically stimulate VIP gene transcription via different sites on the gene.

Receptors

VIP and PACAP share a wide spectrum of biological activity as well as common receptors belonging to the class II of GPCR. Three VIP or PACAP receptor types, which are derived from different genes, are recognized, namely VPAC1, VPAC2, and PAC1. Two of these receptors, VPAC1 and VPAC2, share a high binding affinity in the nanomolar range for VIP and PACAP. A third receptor type, PAC1, has been characterized for its high affinity for PACAP, but low affinity for VIP.

Signal transduction pathway

By binding to VIP, VPAC acts on the Gs protein and activates PKA via elevation of AC activity and production of cAMP (cAMP-dependent pathway). PKA either inhibits phosphorylation of the downstream MAP/ERK kinase or promotes phosphorylation of cAMP response element binding protein (CREB), which finally leads to the inhibition of NF-κB. Meanwhile, studies have also identified a pathway that inhibits the nuclear entry of NF-κB through VPAC signaling, which inhibits IκB phosphorylation (cAMP-independent pathway).

Biological functions

Furthermore, VIP plays a role in the central nervous system, particularly in the hypothalamus and pituitary anterior lobe, regulating pituitary hormones. It is produced by lymphoid tissue, contributing to immunological functions and maintaining immune system homeostasis through various receptors in immunocompetent cells. Additionally, VIP acts as a growth factor, promoting proliferation in normal and cancer cells, potentially inhibiting apoptosis.

Clinical implications

Various diseases have been reported to involve VIP activity, including bronchial asthma, transmission of pain, cluster headaches, Alzheimer’s disease, Parkinson’s disease, and brain injury.

Uses

Aviptadil induces vessel dilation, leading to increased blood flow, reduced peripheral vascular resistance, and hypotension. VIP also affects smooth muscles, exerting relaxant effects on the lower esophageal sphincter, sphincter of Oddi, anal sphincter, and bronchial smooth muscle. In the small intestine, VIP facilitates electrolyte and aqueous liquid secretion, inhibits gastric secretion in the stomach, and aids in pancreatic bicarbonate and aqueous liquid secretion.

General Description

Aviptadil is an injectable synthetic formulation of human vasoactive intestinal peptide (VIP), discovered in 1970. VIP has been utilized to address various inflammatory conditions, including acute respiratory distress syndrome, asthma, and chronic obstructive pulmonary disease. It acts as a neurotransmitter and neuromodulator in both central and peripheral tissues, with its primary activity being vasodilatation.

Biochem/physiol Actions

VIP (Vasoactive intestinal peptide) possesses anti-inflammatory and immunomodulatory functions. It controls the pathogenesis of rheumatoid arthritis. It is also involved in neuroblastoma differentiation, and pancreatic insulin secretion. Vip exhibits its function through G-protein coupled receptors. Some of the other important actions of VIP is associated with the digestive, respiratory, cardiovascular and reproductive systems.

Clinical Use

Aviptadil, a 28-residue polypeptide structurally similar to secretin and glucagon, is widely distributed in the body, particularly in the gastrointestinal tract. It causes vasodilatation, enhances cardiac contractibility, stimulates bicarbonate secretion, relaxes gastrointestinal and other smooth muscles, stimulates glycogenesis, inhibits gastric acid secretion, and promotes insulin secretion. Aviptadil has been granted U.S. Food and Drug Administration (FDA) Fast Track Designation for the treatment of critical COVID-19 with respiratory failure, showcasing its potential therapeutic application in severe respiratory conditions.

InChI:InChI=1/C147H237N43O43S/c1-18-75(12)115(142(229)180-96(56-72(6)7)131(218)183-104(145(232)233)63-110(155)200)188-139(226)106(68-192)185-134(221)101(62-109(154)199)177-130(217)95(55-71(4)5)174-132(219)97(58-81-37-41-84(195)42-38-81)175-125(212)88(33-23-26-49-149)167-123(210)89(34-24-27-50-150)171-140(227)113(73(8)9)186-118(205)76(13)164-121(208)93(47-53-234-17)170-127(214)92(45-46-107(152)197)169-122(209)87(32-22-25-48-148)166-124(211)90(35-28-51-161-146(156)157)168-129(216)94(54-70(2)3)173-126(213)91(36-29-52-162-147(158)159)172-143(230)116(78(15)193)189-136(223)98(59-82-39-43-85(196)44-40-82)176-133(220)100(61-108(153)198)178-135(222)103(65-112(203)204)182-144(231)117(79(16)194)190-137(224)99(57-80-30-20-19-21-31-80)181-141(228)114(74(10)11)187-119(206)77(14)165-128(215)102(64-111(201)202)179-138(225)105(67-191)184-120(207)86(151)60-83-66-160-69-163-83/h19-21,30-31,37-44,66,69-79,86-106,113-117,191-196H,18,22-29,32-36,45-65,67-68,148-151H2,1-17H3,(H2,152,197)(H2,153,198)(H2,154,199)(H2,155,200)(H,160,163)(H,1

40077-57-4 Relevant articles

Effects Of Inhaled Aviptadil (Vasoactive Intestinal Peptide) In Patients With Pulmonary Arterial Hypertension (PAH)

Nazzareno Galie , Anco Boonstra , Ralf Ewert , Miguel A. Gomez-Sanchez , Joan A. Barbera , Adam Torbicki , Hinrich Bremer , Ardeschir Ghofrani , Robert Naeije , Ekkehard Gruenig , Hanno Leuchte , Gérald Simonneau , Hans Klose , Andrew Peacock , Heinrike Wilkens , Dorian Bevec , Vera Cavalli , Gerald Bacher , Lewis J. Rubin

, American Journal of Respiratory and Critical Care Medicine 2010;181:A2516

PAH is a condition characterized by increased pulmonary vascular resistance which leads to right ventricular failure and death. A double blind, placebo contrlled, dose finding, parallel group Phase II study has been performed to assess hemodynamic efcts, clinical efficacy, tolerbility and safety of Aviptadil, an endogenous vasodilatory peptide with immunomodulating and anti- proliferative properties, after single and repeated inhalation in patients with PAH receiving approved PDES inhibitors or endothelin receptor.

Effects of inhaled aviptadil (vasoactive intestinal peptide) in patients with pulmonary arterial hypertension (PAH): results from a phase II study

N Galie, D Badesch, T Fleming, G Simonneau

, European Heart Journal

VIP is a 28 aminoacid polypeptide and belongs to the glucagon-growth hormone releasing factor secretion superfamily (Identical peptide composition in many mammalian species • VIP is produced by neurons, endocrine cell, T-cells, B-cells.

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