Adrenomedullin (AM) (1-12), human, is a peptide with the sequence Tyr-Arg-Gln-Ser-Met-Asn-Asn-Phe-Gln-Gly-Leu-Arg. Adrenomedullin (AM) (1-12), human, was initially identified as a vasodilator, and as such, it has the ability to relax vascular tone. Other
Adrenomedullin (AM) (22-52), human [22-52-Adrenomedullinhuman], TFA, is a C-terminal truncated analogue of adrenomedullin and acts as an adrenomedullin receptor antagonist.
Adrenomedullin (13-52) is a 40 amino acid peptide with one intramolecular disulfide bridge, Adrenomedullin (13-52) is a high affinity ligand for the adrenomedullin receptor.
Adrenomedullin (22-52) is a C-terminal fragment of adrenomedullin (1-52) . In vitro, adrenomedullin (22-52) reduces basal corticosterone production in a mixture of rat adrenocortical and adrenomedulllary cells. It also reverses increases in ACTH-stimulated corticosterone production induced by adrenomedullin (1-52). Adrenomedulin (22-52) (0.5 and 5 μg/kg/min) has no effect on basal regional cerebral blood flow but reverses increases in regional cerebral blood flow induced by rat adrenomedullin in rats. Unlike adrenomedullin (1-52), adrenomedullin (22-52) has no effect on mesenteric arterial perfusion pressure in cats.
Adrenomedullin (13-52) is a truncated form of adrenomedullin (1-52) . It induces nitric oxide-dependent relaxation of and inhibits release of angiotensin II and endothelin-1 from isolated rat aorta. In vivo, adrenomedullin (13-52) decreases mean arterial pressure (MAP) in spontaneously and renal hypertensive rats in a dose-dependent manner. Adrenomedullin (13-52) (10-3,000 ng per animal) reverses increases in lobar arterial pressure induced by U-46619 in a dose-dependent manner in cats but has no effect on basal lobar arterial pressure or systemic arterial pressure. It also potentiates inflammatory edema and neutrophil accumulation in rats.
Pro-Adrenomedullin(153-185),human, (C143H224N42O43), a peptide with the sequence H2N-SLPEAGPGRTLVSSKPQAHGAPAPPSGSAPHFL-OH, MW= 3219.6. Adrenomedullin (AM) is a ubiquitously expressed peptide initially isolated from phaechromyctoma in 19931. AM was initially identified as a vasodilator, some have cited this as the most potent endogenous vasodilatory peptide found in the body2. Differences in opinion regarding the ability of AM to relax vascular tone arises from the differences in the model system used3. Other effects of AM include increasing the tolerance of cells to oxidative stress and hypoxic injury and angiogenesis. AM is seen as a positive influence in diseases such as hypertension, myocardial infarction, chronic obstructive pulmonary disease and other cardiovascular diseases, whereas it can be seen as a negative factor in potentiating the potential of cancerous cells to extend their blood supply and cause cell proliferation.
Adrenomedullin (AM) (1-52), human (TFA), is an NH2-terminal truncated adrenomedullin analogue that influences cell proliferation and angiogenesis in cancer.
Calcitonin is a peptide hormone that lowers blood calcium level and inhibits bone resorption. It belongs to the calcitonin family of peptides, which also includes amylin , calcitonin gene-related peptide , and adrenomedullin. The binding of salmon calcitonin to the human calcitonin receptor (CTR) is not modulated by receptor activity-modifying proteins (RAMPs), which influence affinity of human calcitonin to CTR. Salmon calcitonin binds to human CTR2 with IC50 values of 0.933, 0.224, 0.134, and 0.317 nM alone and with RAMP1, 2, or 3, respectively. It induces cAMP accumulation in COS-7 cells transfected with CTR2 (EC50 = 0.166 nM). Salmon calcitonin inhibits bone resorption by osteoclasts in a pit formation assay using rat bone slices (ID50 = 0.003 pg/mL) and lowers calcium level in vivo in a bioassay of hypocalcemia in rats (ED15 = 33.9 mg/kg). Formulations containing salmon calcitonin have been used to treat hypercalcemia, bone destruction by osteoporosis, and Paget's disease.
KRH102140 is a potent activator of PHD2. KRH102140, which has a structure similar to KRH102053. KRH102140 more efficiently suppressed HIF-1α than KRH102053 in human osteosarcoma cells under hypoxia. Furthermore, KRH102140 decreased the mRNA levels of HIF-regulated downstream target genes associated with angiogenesis and energy metabolism such as vascular endothelial growth factor, adrenomedullin, Glut1, aldolase A, enolase 1 and monocarboxylate transporter 4. KRH102140 also inhibited tube formation in human umbilical vein endothelium cells. The results suggest that KRH102140 has potential therapeutic effects in alleviating various diseases associated with HIFs.