| Company Name: |
Shanghai Huzhen Industrial Co., LTD
|
| Tel: |
021-60345367 13916550749 |
| Email: |
sales@shzbio.com |
| Products Intro: |
Product Name:Apelin
Purity:> 99% Package:50ul/RMB 1098;100ul/RMB 1880;200ul/RMB 2900 Remarks:AGTRL1 ligand; APEL; APEL_HUMAN; Apelin-13; Apelin13; Apelin 13; APJ endogenous ligand; Apln; XNPEP2.
|
|
| Product Name: | apelin | | Synonyms: | apelin | | CAS: | | | MF: | | | MW: | 0 | | EINECS: | | | Product Categories: | | | Mol File: | Mol File | ![apelin Structure]() |
| | apelin Chemical Properties |
| | apelin Usage And Synthesis |
| Gene, mRNA, and precursor | The human APLN gene, location Xq25–26.1, consists of
three exons. Human APLN mRNA has 3238 bp nucleotides that encode a preproprotein of 77 aa. Cleavage of
the proprotein by subtilisin/kexin 3 (PCSK3 or furin)
probably produces APLN-13 (aa 65–77), the mature
APLN peptide exerting biological activities. In mammals, the expression of APLN mRNA is seen in
the heart, lung, kidney, liver, adipose tissue, intestine,
vasdeferens, mammary gland, pituitary, adrenal gland,
endothelium, and brain. | | Synthesis and release | Hypoxia, diabetic retinopathy, angiopoetin, and FGF2
induce APLN expression. In human adipocytes, APLN
expression and secretion are strongly induced under
hypoxic conditions, whereas those are decreased by
aldosterone. | | Receptors | The APLN receptor, APJ, is the seven-transmembrane
GPCR. The human APJ consists of 380 aa residues. Although human APJ shows high homology with the
human angiotensin receptor 1 (AT-1; 30% in total aa
and 54% in transmembrane regions), angiotensin II does
not bind APJ. The binding activity of mammalian APLN
to AJP: Kd=4.45 nM. The Gi/Go protein is coupled and APLN inhibits the
production of cAMP in target cells. The activation of
APJ is also mediated by the Akt/mTOR/p70S6 pathway. | | Agonists and Antagonists | APLN proprotein (55 aa residues), APLN-36, and
APLN-13 (mature apelin). (Ala13)-APLN-13 (functional antagonist). | | Biological functions | APLN binds to APJ, located on the cell membrane of
various tissues. APLN induces a wide range of biological
effects, such as the hypotensive effect through nitric oxide
(NO) release, angiogenesis, the stimulation of cardiac
contractility, and water intake and diuretic effect. APLN inhibits HIV infection by blocking
the HIV coreceptor APJ. Apln-deficient mice are viable, fertile, and showed normal development,whereasApj-deficientmice are not born
in the expected Mendelian ratio, and many show cardiovascular developmental defects. Apln-knockout mice show
impaired retinal vascularization and ocular development. The APLN-induced hypotensive effect is abolished in Apjdeficient mice. Apj-deficient mice also show increased
vasopressor response to the vasoconstrictor angiotensin II.
The baseline blood pressure of double mutant mice homozygous for the deletion of both Apj and At1 is significantly
higher than that in mice deficient of At1 alone. | | Description | Apelin (APLN) is secreted from various tissues in the
cardiovascular, digestive, urinary, and CNS, and regulates
a wide range of physiological/pathophysiological functions,
including cardiovascular function, blood pressure, angiogenesis, and drinking behavior. In 1998, APLN was isolated and characterized from
bovine stomach extracts as an endogenous ligand for
an orphan GPCR, APJ (putative receptor protein related
to the angiotensin receptor, AT1). The peptide sequences
of bovine APLN and bovine cDNA encoding preproAPLN were used to identify human APLN. | | Clinical Use | The down regulation of APJ is suggested to be a possible cause for the development of heart failure. APLN is
indicated to present a future drug target for the treatment
of hypertension and heart failure. APJ agonists are
expected to be blockers of HIV infection. | | Structure and conformation | The human APLN gene encodes a preproprotein of
77 aa residues, containing a signal peptide of 22 aa residues. After cleavage of the signal peptide, the proprotein
of 55 aa residues generates several active fragments,
including APLN-36 (aa 42–77), APLN-17 (aa 61–77),
and APLN-13 (aa 65–77). The APLN-13 is highly active
and responsible for the APJ binding and biological activities of mature APLN. So far, 46 different APLN peptides
ranging from APLN-55 to APLN-12 have been identified
in the bovine colostrum, including C-terminal truncated
isoforms. APLN has been identified in mammals, birds, reptiles,
amphibians, and teleosts. Mr 8569 (Human preproAPLN), 4195.87 (Human
APLN-36), 1550.84 (Human APLN-13). The mature
APLN, APLN-13, contains no cysteine or N-glycosylation
site. It is soluble in water and physiological saline solution. APLN is a specific substrate of angiotensinconverting enzyme 2 (ACE2).
 |
| | apelin Preparation Products And Raw materials |
|