| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Cholecystokinin Octapeptide, desulfated targets CCK-B receptors with selectivity. The lack of sulfation on the tyrosine residue reduces activity at CCK-A receptors while preserving binding to CCK-B receptors. The peptide is used to study CCK-B receptor-mediated central and gastric effects. It is classified as a CCK receptor modulator.
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|---|---|
| ln Vitro |
In vitro, Cholecystokinin Octapeptide, desulfated is used in specificity testing against gastrin and pepsinogen I proteins. It selectively binds to CCK-B receptors and is used to study CCK-B receptor-mediated signaling. The peptide's reduced activity at CCK-A receptors allows researchers to dissect the specific roles of CCK-B receptors in various biological processes.
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| ln Vivo |
In vivo, Cholecystokinin Octapeptide, desulfated is used to study central and gastric effects mediated by CCK-B receptors. These effects are independent of digestive enzyme stimulation. The peptide's selective CCK-B receptor activity makes it a valuable tool for studying the physiological roles of CCK-B receptors in the brain and gastrointestinal tract.
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| Enzyme Assay |
For non-cellular assays, Cholecystokinin Octapeptide, desulfated is evaluated for its binding affinity to CCK-A and CCK-B receptors using radioligand binding assays. Receptor binding is assessed using membrane preparations from cells expressing CCK-A or CCK-B receptors. Selectivity for CCK-B over CCK-A receptors is confirmed by comparing binding affinities. The peptide's ability to activate CCK-B receptor signaling is assessed using biochemical assays.
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| Cell Assay |
In vitro cell culture experiments are performed using cells expressing CCK-A or CCK-B receptors. Cells are treated with Cholecystokinin Octapeptide, desulfated at various concentrations. Endpoints include receptor activation (calcium flux, IP3 production), downstream signaling (MAPK activation), and cellular responses. The peptide's selective activity at CCK-B receptors is confirmed by comparing responses in cells expressing CCK-A versus CCK-B receptors. Specificity testing against gastrin and pepsinogen I proteins is also performed.
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| Animal Protocol |
In vivo animal studies are conducted in rodent models to study CCK-B receptor-mediated effects. Cholecystokinin Octapeptide, desulfated is administered centrally (intracerebroventricular) or peripherally (intravenous, intraperitoneal). Endpoints include gastric motility, food intake, anxiety-like behavior, and other central and gastric parameters. The peptide's effects are compared to those of sulfated CCK-8 to confirm the role of sulfation in receptor selectivity.
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| ADME/Pharmacokinetics |
Cholecystokinin Octapeptide, desulfated has a molecular formula of C49H62N10O13S2 and a molecular weight of approximately 1039.2 g/mol. It is a synthetic peptide lacking the sulfate group on its tyrosine residue. 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.
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| Toxicity/Toxicokinetics |
Cholecystokinin Octapeptide, desulfated is considered safe for research use at standard laboratory concentrations. As a peptide, it is expected to have low toxicity. Standard laboratory safety precautions should be followed during handling. The compound is for research use only and is not intended for therapeutic applications.
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| Additional Infomation |
Asp-Tyr-Met-Gly-Trp-Met-Asp-Phe-NH2 is an octet oligopeptide composed of Asp, Tyr, Met, Gly, Trp, Met, As, and Phe-NH2 residues linked in sequence. It can be used as a metabolite in humans, rats, and mice. It is both an oligopeptide and a peptide amide.
Cholecystokinin Octapeptide, desulfated (CCK-8 desulfated) is a synthetic peptide lacking sulfation on its tyrosine residue. It has reduced activity at CCK-A receptors and selective binding to CCK-B receptors. The peptide is used to study CCK-B receptor-mediated central and gastric effects. It is for research use only and is not approved for clinical use. |
| Molecular Formula |
C49H62N10O13S2
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|---|---|
| Molecular Weight |
1063.20578
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| Exact Mass |
1062.39
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| CAS # |
25679-24-7
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| Related CAS # |
Cholecystokinin Octapeptide, desulfated TFA;171486-94-5
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| PubChem CID |
444998
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| Appearance |
White to off-white solid powder
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| Density |
1.387 g/cm3
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| Boiling Point |
1496.8ºC at 760 mmHg
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| Flash Point |
859ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.638
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| LogP |
3.331
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
31
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| Heavy Atom Count |
74
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| Complexity |
1920
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CSCCC(C(NC(C(C(C(CC(=O)O)N)=O)=O)CC1C=CC(O)=CC=1)=O)NC(CNC(C(CC1=CNC2=CC=CC=C12)NC(C(NC(C(NC(C(CC1C=CC=CC=1)NN)=O)CC(=O)O)=O)CCSC)=O)=O)=O
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| InChi Key |
OIXQINQYMGNCII-YRVFCXMDSA-N
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| InChi Code |
InChI=1S/C49H62N10O13S2/c1-73-18-16-34(55-47(70)37(21-28-12-14-30(60)15-13-28)58-44(67)32(50)23-41(62)63)45(68)53-26-40(61)54-38(22-29-25-52-33-11-7-6-10-31(29)33)48(71)56-35(17-19-74-2)46(69)59-39(24-42(64)65)49(72)57-36(43(51)66)20-27-8-4-3-5-9-27/h3-15,25,32,34-39,52,60H,16-24,26,50H2,1-2H3,(H2,51,66)(H,53,68)(H,54,61)(H,55,70)(H,56,71)(H,57,72)(H,58,67)(H,59,69)(H,62,63)(H,64,65)/t32-,34-,35-,36-,37-,38-,39-/m0/s1
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| Chemical Name |
(3S)-3-amino-4-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]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 (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)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~94.05 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (2.35 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9405 mL | 4.7027 mL | 9.4055 mL | |
| 5 mM | 0.1881 mL | 0.9405 mL | 1.8811 mL | |
| 10 mM | 0.0941 mL | 0.4703 mL | 0.9405 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.