| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Amylin Receptor (AMY1, AMY2, AMY3 subtypes). Calcitonin (8-32), salmon acts as a competitive antagonist at amylin receptors, which are heterodimers of the calcitonin receptor and receptor activity-modifying proteins (RAMPs). It equipotently blocks CT(a), AMY1(a), and AMY3(a) receptors with a pKB of approximately 8. Unlike irreversible agonists, it is a rapidly reversible antagonist, allowing complete washout between treatments-a feature essential for repeated drug addition protocols in CT/AMY-expressing cells. The compound does not activate calcitonin receptors due to the absence of the N-terminal residues 1-7 required for receptor activation.
|
|---|---|
| ln Vitro |
In vitro, Calcitonin (8-32), salmon functions as a competitive antagonist at amylin and calcitonin-family receptors. It exhibits potent inhibition of amylin-induced signaling in receptor-expressing cell lines, effectively blocking amylin-mediated cAMP accumulation and downstream effects. The compound demonstrates high selectivity for amylin receptors over other calcitonin-family receptors, making it a valuable tool for distinguishing amylin-specific responses from those mediated by calcitonin or CGRP receptors. Its reversible binding kinetics allow for precise pharmacological characterization in receptor binding and functional assays.
|
| ln Vivo |
In vivo, Calcitonin (8-32), salmon has been studied in rat models for its effects on pancreatic hormone secretion. In the perfused rat pancreas, this amylin antagonist was shown to reverse amylin-induced inhibition of insulin secretion, achieving approximately 80% reversal. The compound has also been used to investigate the role of amylin in glucose homeostasis, calcium metabolism, and bone remodeling. Its in vivo antagonism of amylin receptors helps delineate the physiological functions of endogenous amylin, particularly in metabolic regulation and pancreatic endocrine function.
|
| Enzyme Assay |
In vitro enzyme/receptor binding (cell-free) assays for Calcitonin (8-32), salmon typically involve radioligand binding competition studies using membrane preparations from cells expressing recombinant amylin or calcitonin receptors. The compound is incubated with varying concentrations of radiolabeled amylin or calcitonin in binding buffer containing appropriate protease inhibitors. Non-specific binding is determined in the presence of excess unlabeled ligand. After incubation at room temperature for 1-2 hours, bound and free radioligands are separated by rapid filtration through glass fiber filters, followed by washing and scintillation counting. IC50 or Ki values are calculated from competition curves using nonlinear regression analysis.
|
| Cell Assay |
In vitro cell-based assays for Calcitonin (8-32), salmon typically use cell lines stably expressing recombinant amylin receptors (e.g., AMY1, AMY2, AMY3) or calcitonin receptors. Cells are seeded in 96-well plates and pre-incubated with varying concentrations of the peptide antagonist for 30-60 minutes, followed by stimulation with a fixed concentration of amylin or calcitonin agonist. Functional readouts include cAMP accumulation measured by ELISA or HTRF, or intracellular calcium mobilization detected by fluorescent calcium indicators. Antagonist potency is expressed as IC50 or pKB values. The reversible nature of the antagonist allows for washout experiments to confirm competitive binding kinetics.
|
| Animal Protocol |
In vivo animal studies with Calcitonin (8-32), salmon are commonly conducted in rat models. A typical protocol involves intravenous or intraperitoneal administration of the peptide at doses ranging from 10-100 microg/kg, followed by assessment of metabolic or endocrine parameters. In the perfused rat pancreas model, the compound is infused through the pancreatic artery, and insulin, glucagon, and somatostatin release are measured in the perfusate. Blood glucose, calcium, and hormone levels are monitored at various time points post-administration. Studies may also involve co-administration with amylin to evaluate antagonist effects on amylin-induced physiological responses.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Calcitonin (8-32), salmon are characteristic of peptide therapeutics. As a 24-amino acid peptide with a molecular weight of 2725.06 Da, it is susceptible to proteolytic degradation in the gastrointestinal tract and has poor oral bioavailability. When administered parenterally (intravenous or subcutaneous), the peptide has a relatively short plasma half-life due to rapid clearance via renal filtration and enzymatic degradation. It is typically formulated in aqueous solution and stored at -20degC or -80degC for long-term stability. The compound is soluble in water at concentrations up to 100 mg/mL. In vivo pharmacokinetic studies require appropriate formulation and route of administration for optimal exposure.
|
| Toxicity/Toxicokinetics |
Toxicological data for Calcitonin (8-32), salmon are primarily derived from preclinical studies in animal models. As a research-use peptide antagonist, comprehensive toxicity profiles are not as extensively documented as for therapeutic agents. The compound is generally well-tolerated at pharmacological doses in rodent studies, with no significant acute toxicity reported. Standard safety precautions for peptide handling apply, including avoidance of repeated freeze-thaw cycles and protection from light and moisture. It is intended for research use only and not for human therapeutic applications. Long-term toxicity and carcinogenicity studies have not been systematically conducted for this research compound.
|
| References | |
| Additional Infomation |
Calcitonin (8-32), salmon is a research-grade peptide antagonist supplied for laboratory use only. It is classified as a GPCR/G Protein pathway modulator targeting the amylin receptor. The compound is frequently used as a universal calcitonin-family blocking reagent or as an intermediate-selectivity control alongside AC187 and CGRP(8-37) in receptor pharmacology studies. Its sequence is VLGKLSQELHKLQTYPRTNTSGTP-NH2 (single-letter code). Storage recommendations: powder at -80degC for up to 2 years or -20degC for 1 year; in solution at -80degC for 6 months or -20degC for 1 month, sealed under nitrogen and protected from moisture and light. Not approved for clinical use.
|
| Molecular Formula |
C119H198N36O37
|
|---|---|
| Molecular Weight |
2725.06000
|
| Exact Mass |
2723.47
|
| CAS # |
155069-90-2
|
| PubChem CID |
102601690
|
| Appearance |
White to off-white solid powder
|
| LogP |
-13.3
|
| Hydrogen Bond Donor Count |
41
|
| Hydrogen Bond Acceptor Count |
42
|
| Rotatable Bond Count |
90
|
| Heavy Atom Count |
192
|
| Complexity |
6110
|
| Defined Atom Stereocenter Count |
26
|
| SMILES |
C[C@H]([C@@H](C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N3CCC[C@H]3C(=O)N)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC4=CNC=N4)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](C(C)C)N)O
|
| InChi Key |
CUQBOYYGZCRRKW-LPJWDPCBSA-N
|
| InChi Code |
InChI=1S/C119H198N36O37/c1-56(2)42-74(146-113(187)92(125)60(9)10)98(172)131-50-88(166)135-68(22-15-17-37-120)100(174)142-77(45-59(7)8)108(182)149-82(54-157)111(185)140-71(31-34-85(122)163)102(176)138-73(33-36-91(169)170)103(177)144-76(44-58(5)6)107(181)145-78(47-66-49-129-55-134-66)109(183)137-69(23-16-18-38-121)101(175)143-75(43-57(3)4)106(180)139-72(32-35-86(123)164)105(179)153-95(63(13)160)116(190)148-80(46-65-27-29-67(162)30-28-65)117(191)155-41-21-26-84(155)112(186)141-70(24-19-39-130-119(127)128)104(178)152-94(62(12)159)115(189)147-79(48-87(124)165)110(184)151-93(61(11)158)114(188)133-51-89(167)136-81(53-156)99(173)132-52-90(168)150-96(64(14)161)118(192)154-40-20-25-83(154)97(126)171/h27-30,49,55-64,68-84,92-96,156-162H,15-26,31-48,50-54,120-121,125H2,1-14H3,(H2,122,163)(H2,123,164)(H2,124,165)(H2,126,171)(H,129,134)(H,131,172)(H,132,173)(H,133,188)(H,135,166)(H,136,167)(H,137,183)(H,138,176)(H,139,180)(H,140,185)(H,141,186)(H,142,174)(H,143,175)(H,144,177)(H,145,181)(H,146,187)(H,147,189)(H,148,190)(H,149,182)(H,150,168)(H,151,184)(H,152,178)(H,153,179)(H,169,170)(H4,127,128,130)/t61-,62-,63-,64-,68+,69+,70+,71+,72+,73+,74+,75+,76+,77+,78+,79+,80+,81+,82+,83+,84+,92+,93+,94+,95+,96+/m1/s1
|
| Chemical Name |
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S,3R)-1-[[(2S)-4-amino-1-[[(2S,3R)-1-[[2-[[(2S)-1-[[2-[[(2S,3R)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-2-amino-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : ~100 mg/mL (~36.70 mM)
|
|---|---|
| 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 | 0.3670 mL | 1.8348 mL | 3.6696 mL | |
| 5 mM | 0.0734 mL | 0.3670 mL | 0.7339 mL | |
| 10 mM | 0.0367 mL | 0.1835 mL | 0.3670 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
