Human Calcitonin (hCT) is a 32-amino acid hormone peptide belonging to the Calcitonin/Calcitonin-gene related peptide (CGRP) family,that also comprises amylin,adrenomedullin (AM) and adrenomedullin2/intermedin (AM2/IMD). Calcitonin is characterized by a N-terminal disulfide bond that forms a 7 amino acid ring structure,a region with a α-helix tendency and an amidated C-terminus 1.
Calcitonin peptide is produced by C cells of the thyroid gland and binds preferentially to the G-protein coupled receptor,calcitonin receptor (CTR)1. Calcitonin receptor signals through activated Gs protein and the production of cAMP second messenger molecules by adenylyl cyclase 1. The dissociation constant (Kd) of calcitonin receptors expressed by a human ovarian small cell carcinoma line is approximately 4.6 nM for human Calcitonin2.
Calcitonin is involved in the homeostasis of calcium and phosphorus,and the regulation of bone dynamics. At the basal state,calcitonin secretion reduces plasma calcium and phosphorus levels,and promote bone formation. In Calca -/- mice,a murin particle-induced osteolysis model,Calcitonin peptide has been used as a test compound for studying the effects of calcitonin deficiency. It has been shown that artificial calcitonin subsitution inhibits bone resorption by reducing the formation of osteoclasts and thereby the resulting osteolytic reaction 3. The Hypocalcemic Human calcitonin was also used as a positive control to monitor changes in serum calcium levels in HHD transgenic mice vaccinated with Parathyroid hormone-related protein (PTH-rP)-derived peptides in the context of anti-cancer immunotherapy study 4. Moreover,it has been reported that calcitonin peptide is a potent stimulator of uncapacitated mouse spermatozoa by regulating a specific isoform of adenylyl cyclase and the production of cAMP,which plays a pivotal role in mammalian sperm function 5.
Sequence : CGNLSTCMLGTYTQDFNKFHTFPQTAIGVGAP-NH2
MW : 3 417.85 Da (C 151 H 226 N 40 O 45 S 3)
Purity : > 95%
Disulfide bonds : Cys1-Cys7
Counter-Ion : TFA Salts(see option TFA removal)
Delivery format : Freeze dried in propylene 2mL microtubes
Other names : 21215-62-3,Calcihexal,Calcimar,calcitonin salmon,Forcaltonin,Fortical,Miacalcic,Salcatonin
Peptide Solubility Guideline
Bulk peptide quantities available
Update on the pharmacology of calcitonin/CGRP family of peptides: IUPHAR Review 25
The calcitonin/CGRP family of peptides includes calcitonin,α and β CGRP,amylin,adrenomedullin (AM) and adrenomedullin 2/intermedin (AM2/IMD). Their receptors consist of one of two GPCRs,the calcitonin receptor (CTR) or the calcitonin receptor-like receptor (CLR). Further diversity arises from heterodimerization of these GPCRs with one of three receptor activity-modifying proteins (RAMPs). This gives the CGRP receptor (CLR/RAMP1),the AM1 and AM2 receptors (CLR/RAMP2 or RAMP3) and the AMY1,AMY2 and AMY3 receptors (CTR/RAMPs1-3 complexes,respectively). Apart from the CGRP receptor,there are only peptide antagonists widely available for these receptors,and these have limited selectivity,thus defining the function of each receptor in vivo remains challenging. Further challenges arise from the probable co-expression of CTR with the CTR/RAMP complexes and species-dependent splice variants of the CTR (CT(a) and CT(b) ). Furthermore,the AMY1(a) receptor is activated equally well by both amylin and CGRP,and the preferred receptor for AM2/IMD has been unclear. However,there are clear therapeutic rationales for developing agents against the various receptors for these peptides. For example,many agents targeting the CGRP system are in clinical trials,and pramlintide,an amylin analogue,is an approved therapy for insulin-requiring diabetes. This review provides an update on the pharmacology of the calcitonin family of peptides by members of the corresponding subcommittee of the International Union of Basic and Clinical Pharmacology and colleagues.
Cloning,characterization,and expression of a human calcitonin receptor from an ovarian carcinoma cell line
A human ovarian small cell carcinoma line (BIN-67) expresses abundant calcitonin (CT) receptors (CTR) (143 ,000 per cell) that are coupled,to adenylate cyclase. The dissociation constants (Kd) for the CTRs on these BIN-67 cells is approximately 0.42 nM for salmon CT and approximately 4.6 nM for human CT. To clone a human CTR (hCTR),a BIN-67 cDNA library was screened using a cDNA probe from a porcine renal CTR (pCTR) that we recently cloned. One positive clone of 3 ,588 bp was identified. Transfection of this cDNA into COS cells resulted in expression of receptors with high affinity for salmon CT (Kd = approximately 0.44 nM) and for human CT (Kd = approximately 5.4 nM). The expressed hCTR was coupled to adenylate cyclase. Northern analysis with the hCTR cDNA probe indic
