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Calcitonin, eel (Thyrocalcitonin eel) Sale

(Synonyms: 降钙素,Thyrocalcitonin eel) 目录号 : GC30291

A peptide hormone

Calcitonin, eel (Thyrocalcitonin eel) Chemical Structure

Cas No.:57014-02-5

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1mg
¥1,607.00
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5mg
¥4,820.00
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10mg
¥8,122.00
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产品描述

Calcitonin is a 32-amino acid peptide hormone that lowers blood calcium levels and inhibits bone resorption.1,2 The amino acid sequence of eel calcitonin varies from salmon and human calcitonin at 3 and 16 positions, respectively.3 Calcitonin (eel) binds to calcitonin receptor 2 (CTR2) with higher affinity than human, porcine, or rat calcitonin (Kis = 0.01, 2.95, 0.44, and 5.89 nM, respectively, in radioligand binding assays). It inhibits gastric emptying in conscious dogs more potently than human calcitonin when administered at a dose of 10 ?g/kg.3,4 Calcitonin (eel) increases the paw withdrawal threshold in a mouse model of carrageenan-induced inflammation when administered at a dose of 0.2 ?g/paw.5

1.Foster, G.V.Calcitonin. A review of experimental and clinical investigationsPostgrad. Med. J.44(511)411-422(1968) 2.Chesnut, C.H., III, Azria, M., Silverman, S., et al.Salmon calcitonin: A review of current and future therapeutic indicationsOsteoporos. Int.19(4)479-491(2008) 3.Chen, W.-J., Armour, S., Way, J., et al.Expression cloning and receptor pharmacology of human calcitonin receptors from MCF-7 cells and their relationship to amylin receptorsMol. Pharmacol.52(6)1164-1175(1997) 4.Nakamura, H., Asano, T., and Takeda, K.Gastrointestinal motor inhibition by exogenous human, salmon, and eel calcitonin in conscious dogsCan. J. Physiol. Pharmacol.73(1)43-49(1995) 5.Guidobono, F., Netti, C., Villani, P., et al.Antinociceptive activity of eel calcitonin, injected into the inflamed paw in ratsNeuropharmacology30(12A)1275-1278(1991)

Chemical Properties

Cas No. 57014-02-5 SDF
别名 降钙素,Thyrocalcitonin eel
Canonical SMILES Cys-Ser-Asn-Leu-Ser-Thr-Cys-Val-Leu-Gly-Lys-Leu-Ser-Gln-Glu-Leu-His-Lys-Leu-Gln-Thr-Tyr-Pro-Arg-Thr-Asp-Val-Gly-Ala-Gly-Thr-Pro-NH2 (Disulfide bridge: Cys1-Cys7)
分子式 C146H241N43O47S2 分子量 3414.91
溶解度 Water: 10 mg/ml 储存条件 Store at -20°C
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1 mM 0.2928 mL 1.4642 mL 2.9283 mL
5 mM 0.0586 mL 0.2928 mL 0.5857 mL
10 mM 0.0293 mL 0.1464 mL 0.2928 mL
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Research Update

Efficacy of calcitonin for treating acute pain associated with osteoporotic vertebral compression fracture: an updated systematic review

Objective: Acutely painful osteoporotic vertebral compression fractures are associated with hospitalization and mortality in older adults. Calcitonin may be an alternative to opioid or nonopioid analgesia for treating acute compression fracture pain in emergency and primary care settings. This review summarizes pain, function, and adverse events associated with calcitonin. Methods: We searched MEDLINE, EMBASE, The Cochrane Library, clinical trials registries, and reference lists of included studies. Eligible studies evaluated the effect of synthetic calcitonins (salmon, eel, and human) on pain scores in adults ≥60 years old with a recent atraumatic compression fracture. Two reviewers screened studies, extracted data, and allocated bias in duplicate. A random effects meta-analysis evaluated standard mean difference (SMD) and heterogeneity (I2). Results: Of 1,198 articles screened, 11 were included (9 in the meta-analysis). Treatment lasted from 14 days to 6 months. Pain was lower in the salmon calcitonin group (100-200 IU IM or NAS, daily) than the control group with high certainty of evidence at week 1 (SMD, -1.54; 95% confidence interval [CI], -2.02 - -1.06; I2 = 52%), representing a number needed to treat of two. The analgesic efficacy of salmon calcitonin at 4 weeks was unclear due to substantial heterogeneity. There was low certainty evidence that calcitonin did not increase the overall risk of adverse events, including nausea and vomiting (risk ratio, 2.10; 95% CI, 0.87-5.08; I2 = 47%). Conclusions: Calcitonin is beneficial and appears safe for treating acute pain associated with compression fractures. Further studies may improve the certainty of evidence.

Comparative effects of eel calcitonin, salmon calcitonin and [Asu1,7]eel calcitonin on hypophyseal and osteoblastic function

Three different calcitonins: salmon calcitonin, eel calcitonin and the semi-synthetic analog [Asu1,7]eel calcitonin have been evaluated for their ability to affect phosphoinositide hydrolysis in primary cultures of anterior pituitary cells and in the osteoblast-like UMR-106 cells. In both cellular systems a repeated treatment with any form of calcitonin induced an inhibition of inositol phospholipid turnover. Eel calcitonin and its analog were always more potent than salmon calcitonin, but the efficacy of the three polypeptides was comparable. In cultured anterior pituitary cells, the inhibitory effect on phosphoinositide hydrolysis observed after chronic treatment with calcitonin was accompanied by a reduction of prolactin release. In contrast, a single treatment of cultured anterior pituitary cells with eel calcitonin or its analog [Asu1,7]eel calcitonin induced an increase of inositol phosphate accumulation, while salmon calcitonin was inactive. Accordingly, eel and [Asu1,7]eel calcitonin, but not salmon calcitonin, induced a slight but significant stimulation of prolactin secretion. In UMR-106 cells, the three calcitonins exhibited similar potency and efficacy in reducing parathyroid hormone-stimulated 4 beta[3H]-phorbol-12,13-dibutyrate ([3H]PdBu) binding, an indirect index of protein kinase C activation. Taken together, these results suggest that, either at the pituitary or in osteoblast-like cells, some of the effects exerted by calcitonin may be ascribed to an interference with the intracellular events initiated by modulation of phosphoinositide turnover.

[Calcitonin]

Calcitonin is a potent inhibitor of osteoclastic bone resorption and has been widely used for the treatment of osteoporosis. Nasal calcitonin, instead of injectable form, is more popular in Europe and United States, while only injectable form has been approved in Japan. The regimen, dose, frequency is remarkably different from study to study, and the standard regimen has not been established for osteoporosis. Fifty to 100 units of salmon calcitonin has been used daily intramuscularly in Europe. Recent trial using nasal calcitonin has shown the similar effects on the bone as the injectable form although the actual resorptionis not so high. In Japan, once weekly 20 units if eel calcitonin analogue injection has been approved for osteoporosis. After administration in the form of either nasal or injectable preparation, peak serum concentration reaches more than 100 pg/ml, far exceeding 10(-11) M, at which level osteoclast bone resorption is rapidly impaired with disappearance of actin ring formation. It is reflected by the decrease of urinary pyridinoline cross-links excretion. Consecutive treatment with calcitonin reduces the calcitonin receptors on the surface of osteoclasts as well as osteoclast precursors, while they are still TRAP positive, suggesting that they retain bone resorbing activity. That may be one of the mechanisms of escape phenomenon. We are not sure whether daily administration of calcitonin can avoid the escape phenomenon and can maintain the bone volume. The standard preparation should be determined by the longer clinical trials with new bone markers and bone mass measurement as the endpoints.

Stability of [Asu1,7]-eel calcitonin and eel calcitonin in vitro and in vivo

Stability of [Asu1,7]-eel calcitonin was compared with that of eel calcitonin by the radioimmunoassay method. [Asu1,7]-Eel calcitonin cross-reacted with anti-eel calcitonin antisera. [Asu1,7]-Eel calcitonin was as stable as eel calcitonin in rabbit liver or rabbit kidney extracts when incubated at 37 degrees C. Disappearance curves from the plasma of [Asu1,7]-eel calcitonin and eel calcitonin following iv injection in rabbits were quite similar.

Stability and the biological activity of eel calcitonin in rats

Hypocalcemic effect in rats of eel calcitonin was more persistent that that of porcine calcitonin and it was as persistent as that of salmon calcitonin I. Eel calcitonin was more stable than porcine or salmon calcitonin I when incubated in vitro with rat or human serum. Incubation in vitro with rat kidney or liver extract for 1 hour at 37 degrees C caused an almost complete inactivation of porcine calcitonin. On the other hand, both eel and salmon calcitonin I were inactivated less markedly and in the similar manner. The relationship between the hypocalcemic effect of calcitonins and the inactivation is discussed.