| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Calcitonin targets the calcitonin receptor (CTR). It binds to CTR2 with IC50 values of 8.5 nM. Receptor binding is modulated by receptor activity-modifying proteins (RAMPs). The hormone's activity is mediated through the modulation of the cAMP-PKA signaling pathway at the subcellular level. It acts primarily on osteoclasts to inhibit bone resorption.
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| ln Vitro |
Osteoclast-mediated bone resorption is potently inhibited by calcitonin [1].
In vitro, calcitonin has potent inhibitory effects on osteoclast-mediated bone resorption. It binds to the calcitonin receptor (CTR) with high affinity and stimulates cyclic nucleotide accumulation in human kidney cortex and medulla. The hormone's effects are mediated through the cAMP-PKA signaling pathway. Its activity is modulated by RAMPs. |
| ln Vivo |
One daily, 9-week infusion of cavogastric calcitonin (2 mg/kg) can block cartilage deterioration and prevent cartilage tracking [3].
In vivo, calcitonin lowers blood calcium levels and inhibits bone resorption. It opposes the effects of parathyroid hormone (PTH). The hormone is used in research on hypercalcemia and osteoporosis. It has been shown to decrease blood calcium and phosphate due to inhibition of resorption by osteoblasts and osteocytes. It can also be used as a carrier peptide to internalize fusion proteins. |
| Enzyme Assay |
For non-cellular assays, calcitonin is evaluated for its binding affinity to the calcitonin receptor using radioligand binding assays. Receptor binding is assessed using membrane preparations from cells expressing CTR. IC50 values are determined from competition binding experiments. The hormone's ability to stimulate cAMP production is assessed using biochemical assays with purified receptor preparations or membrane fractions.
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| Cell Assay |
In vitro cell culture experiments are performed using cells expressing the calcitonin receptor, such as osteoclasts, kidney cells, or CTR-transfected cell lines. Cells are treated with calcitonin at concentrations ranging from 0.1 nM to 1 μM. Endpoints include cAMP accumulation, PKA activation, osteoclast activity (resorption pit assays), and cellular signaling (Western blot for phosphorylated targets). The hormone's effects are compared to those of other calcitonin family peptides.
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| Animal Protocol |
Animal/Disease Models: Female SD (SD (Sprague-Dawley)) rat [3]
Doses: 2 mg/kg Route of Administration: po (oral gavage); 2 mg/kg; one time/day; 9 weeks Experimental Results: Ovariectomy-induced cartilage loss compared with vehicle control Degeneration was inhibited (P<0.001). Treatment with vehicle alone prevented cartilage erosion (P<0.01), and the extent of erosion was comparable to sham-operated animals. In vivo animal studies are conducted in rodent models. Calcitonin is administered subcutaneously, intravenously, or intraperitoneally. Endpoints include serum calcium and phosphate levels, bone mineral density (by DEXA or micro-CT), bone turnover markers (P1NP, CTX-1), and histomorphometric analysis of bone. The hormone's effects on calcium homeostasis and bone metabolism are assessed in models of osteoporosis, hypercalcemia, and other bone diseases. |
| ADME/Pharmacokinetics |
Calcitonin (human) has a molecular formula of C151H226N40O45S3 and a molecular weight of 3417.90 g/mol. It is a peptide hormone consisting of 32 amino acids. The peptide is typically stored as a lyophilized powder and reconstituted in appropriate buffers for experimental use. Pharmacokinetic properties are characteristic of peptides, with rapid clearance and limited oral bioavailability. It is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Toxicological profiles of calcitonin are well characterized from clinical use. The hormone is generally well-tolerated at therapeutic doses. Common adverse effects include nausea, vomiting, and local injection site reactions. Long-term use has been associated with a potential increased risk of cancer, although this remains controversial. Standard laboratory safety precautions should be followed during handling. The compound is for research use only.
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| References | |
| Additional Infomation |
Calcitonin (human) is a peptide hormone that lowers blood calcium and inhibits bone resorption. It targets the calcitonin receptor (CTR) and is modulated by RAMPs. The hormone stimulates cAMP accumulation and opposes PTH effects. It is used in research on hypercalcemia and osteoporosis. The compound is for research use only and is not intended for therapeutic applications without proper authorization.
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| Molecular Formula |
C151H226N40O45S3
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|---|---|
| Molecular Weight |
3417.846
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| Exact Mass |
3415.58
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| CAS # |
21215-62-3
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| PubChem CID |
129011830
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| Appearance |
White to off-white solid powder
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| LogP |
-11.6
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| Hydrogen Bond Donor Count |
47
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| Hydrogen Bond Acceptor Count |
50
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| Rotatable Bond Count |
103
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| Heavy Atom Count |
238
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| Complexity |
7950
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| Defined Atom Stereocenter Count |
34
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| SMILES |
CC[C@H](C)[C@@H](C(=O)NCC(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC4=CN=CN4)NC(=O)[C@H](CC5=CC=CC=C5)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CC6=CC=CC=C6)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC7=CC=C(C=C7)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CS)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)N)NC(=O)CNC(=O)[C@H](CS)N
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| InChi Key |
MYUAQRALWPOWGP-DSCKDRDKSA-N
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| InChi Code |
InChI=1S/C151H228N40O45S2/c1-18-75(10)118(143(228)163-66-113(205)182-116(73(6)7)142(227)162-63-111(203)165-77(12)150(235)190-50-30-39-105(190)124(158)209)185-125(210)76(11)166-145(230)120(79(14)194)186-130(215)92(46-48-108(155)200)169-141(226)106-40-31-51-191(106)151(236)102(57-85-36-26-21-27-37-85)179-148(233)122(81(16)196)188-138(223)98(58-87-62-159-70-164-87)174-132(217)95(54-83-32-22-19-23-33-83)172-128(213)90(38-28-29-49-152)168-135(220)100(60-110(157)202)175-133(218)96(55-84-34-24-20-25-35-84)173-136(221)101(61-115(207)208)176-129(214)91(45-47-107(154)199)170-147(232)121(80(15)195)187-137(222)97(56-86-41-43-88(198)44-42-86)178-146(231)119(78(13)193)183-114(206)65-161-127(212)93(52-71(2)3)177-144(229)117(74(8)9)184-140(225)104(69-238)181-149(234)123(82(17)197)189-139(224)103(67-192)180-131(216)94(53-72(4)5)171-134(219)99(59-109(156)201)167-112(204)64-160-126(211)89(153)68-237/h19-27,32-37,41-44,62,70-82,89-106,116-123,192-198,237-238H,18,28-31,38-40,45-61,63-69,152-153H2,1-17H3,(H2,154,199)(H2,155,200)(H2,156,201)(H2,157,202)(H2,158,209)(H,159,164)(H,160,211)(H,161,212)(H,162,227)(H,163,228)(H,165,203)(H,166,230)(H,167,204)(H,168,220)(H,169,226)(H,170,232)(H,171,219)(H,172,213)(H,173,221)(H,174,217)(H,175,218)(H,176,214)(H,177,229)(H,178,231)(H,179,233)(H,180,216)(H,181,234)(H,182,205)(H,183,206)(H,184,225)(H,185,210)(H,186,215)(H,187,222)(H,188,223)(H,189,224)(H,207,208)/t75-,76-,77-,78+,79+,80+,81+,82+,89-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,116-,117-,118-,119-,120-,121-,122-,123-/m0/s1
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| Chemical Name |
(3S)-4-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-5-amino-1-[[(2S,3R)-1-[[(2S)-1-[[(2S,3S)-1-[[2-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-5-amino-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[2-[[(2R)-2-amino-3-sulfanylpropanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-sulfanylpropanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-oxopentanoyl]amino]-4-oxobutanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~29.26 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2926 mL | 1.4629 mL | 2.9258 mL | |
| 5 mM | 0.0585 mL | 0.2926 mL | 0.5852 mL | |
| 10 mM | 0.0293 mL | 0.1463 mL | 0.2926 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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