calcitonin (human)

Endogenous calcitonin receptor agonist. Lowers systemic blood calcium levels and inhibits bone resorption.

Calcitonin (human) acetate (21215-62-3, free base) is a synthetic polypeptide hormone composed of 32 amino acids. As an endogenous calcitonin receptor agonist, it inhibits bone resorption and lowers serum calcium levels. It is commonly used in the study of the mechanisms underlying osteoporosis, hypercalcemia, and Paget’s disease of bone.

Adrenomedullin (AM) (22-52), human acetate is an antagonist of calcitonin generelated peptide receptor in the hindlimb vascular bed of the cat and an adrenomedullin receptor.

Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a selective calcitonin gene-related peptide 1 (CGRP1) receptor antagonist with an IC50=0.03 nM and Ki=14.4 pM.

Olcegepant (BIBN-4096) is an effective and selective non-peptide calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP).

MK-3207 is a highly potent and orally bioavailable small molecule antagonist of the calcitonin gene-related peptide (CGRP) receptor, demonstrating an in vitro IC50 of 0.12 nM and a Ki of 0.024 nM for the human receptor with exceptional selectivity over the related human AM1, AM2, CTR, and AMY3 receptors, though it exhibits lower affinity for CGRP receptors from other species such as canine and rodent; in vitro studies confirm its potent antagonism of human and rhesus monkey CGRP receptors (K(i) = 0.024 nM), and in vivo models show it produces a concentration-dependent inhibition of dermal vasodilation, requiring plasma concentrations of 0.8 nM and 7 nM to block 50% and 90% of the blood flow increase, respectively.

SUN B8155 is a calcitonin (CT) receptor agonist that selectively mimics the biological effects of calcitonin and induces cAMP formation in cells expressing recombinant human CT receptor.

Tyr-α-CGRP is an N-terminal extended tyrosinated analogue of α-calcitonin gene-related peptide . It binds to amylin receptors AMY1 and AMY3 in COS-7 cells expressing the human receptors (IC50s = 141 and 1.86 nM, respectively). Tyr-α-CGRP also binds to and stimulates cAMP accumulation in rat L6 myocytes (IC50 = 4 nM; EC50 = 12 nM). It also binds to rat brain and spleen membrane preparations (IC50s = 0.2 and 0.5 nM, respectively), induces positive chronotropic and inotropic effects in isolated right and left guinea pig atria (EC50s = 282 and 74 nM, respectively), and inhibits the twitch response in rat vas deferens (EC50 = 1.9 nM).

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.

Eptinezumab is a humanised monoclonal antibody targeting CGRP (calcitonin gene-related peptide), which prevents CGRP binding to its receptor and may be used for migraine prevention.

Fremanezumab (TEV-48125) is a humanised monoclonal antibody targeting CGRP, capable of neutralising human (IC50=7.94 nM), mouse (IC50=19.6 nM) and rat CGRP, and is indicated for the prevention of migraine. Fremanezumab inhibits CGRP's vasodilatory effects in the basilar artery constriction segment and suppresses activation of A-δ and high-threshold (HT) neurons in the meningeal nociceptive system triggered by cortical spreading depression (CSD) in rats. In vitro, Fremanezumab counteracts CGRP's immunosuppressive effects on microglia and lymphocytes.

Erenumab is a whole-human monoclonal antibody. Erenumab inhibits calcitonin gene-related peptide (CGRP) receptors. Erenumab can be used to prevent migraine attacks.

β-CGRP, human ,a 37-amino acid peptide,is the beta form of Calcitonin-gene-related peptide (β-CGRP), involved extensively in regulation of the cardiovascular and nervous systems. β-CGRP contains a disulphide bridge at the N-terminus, a C-terminal phenylal

β-CGRP,human tissue is one of the calcitonin peptide, through complex behavior of calcitonin receptor like receptor (CRLR) - and receptor activity - modifying proteins (increased), and 1 and 300 - nM CRLR IC50s/RAMP1 and CRLR/RAMP2 cells.

HCGRP-(8-37) acetate is a human calcitonin gene-related peptide (hCGRP) fragment acetate and also an antagonist of CGRP receptor.

Endogenous peptide product of human prepro-VIP and analog of porcine PHI-27; potent agonist for the human calcitonin receptor (EC50 = 11 nM). Transgenic mice expressing the human VIP/PHM 27 gene in pancreatic β-islets display enhanced glucose-induced insu

PHM-27 (human) acetate is the endogenous peptide product of prepro-VIP (human), an agonist of the calcitonin receptor (EC 50 = 11 nM). Transgenic mice overexpressing PHM-27 (human) acetate in pancreatic β-islets exhibited enhanced glucose-induced insulin secretion.

β-CGRP, human acetate is one of calcitonin peptides and acts via the complex of receptor-activity-modifying protein (RAMP) and calcitonin-receptor-like receptor (CRLR) (IC50s: 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells).

Intermedin1-53 (Human) is a 53-amino acid peptide from the human calcitonin family that reduces the vulnerability of atherosclerotic plaques by inhibiting CHOP-mediated macrophage apoptosis and inflammasome activity.