| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
H-D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 targets the mu-opioid receptor (MOR) as a potent antagonist. The D-Phe1, D-Trp4, and Pen7 substitutions confer high MOR selectivity and metabolic stability. It blocks mu-opioid receptor-mediated signaling, including analgesia and respiratory depression.
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|---|---|
| ln Vitro |
In vitro, the peptide competitively inhibits mu-opioid receptor-mediated signaling in isolated tissue preparations and cell-based assays. It is used to characterize MOR pharmacology and to validate the involvement of MOR in specific signaling pathways.
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| ln Vivo |
In a dose-dependent manner, CTOP (0-0.5 nmol, ICV, once) counteracts the analgesic effects of morphine [1]. In morphine-dependent rats, withdrawal hypothermia and weight loss are brought on by CTOP (0–2 nmol, ICV, once) [1]. In the nucleus accumbens, CTOP (0–1.5 nmol per side, intra-VTA injection) increases extracellular dopamine levels and, in a dose-dependent manner, increases locomotor activity [2].
In vivo, the peptide blocks mu-opioid receptor-mediated effects, including analgesia, respiratory depression, and gastrointestinal transit inhibition. It is used to study the role of MOR in pain, addiction, and other physiological processes. |
| Enzyme Assay |
For receptor binding assays, membranes from MOR-expressing cells are incubated with [3H]-DAMGO (0.5-1 nM) and increasing concentrations of the peptide in binding buffer (50 mM Tris-HCl, pH 7.4, 5 mM MgCl2) for 60-90 min at 25°C. Nonspecific binding is defined with 10 μM naloxone.
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| Cell Assay |
For functional assays, guinea pig ileum preparations are electrically stimulated, and the peptide (0.001-1000 nM) is added cumulatively to measure inhibition of twitch contractions. For cAMP assays, MOR-expressing cells are treated with peptide, and intracellular cAMP is measured by ELISA.
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| Animal Protocol |
Animal/Disease Models: Male CFLP mice (25-30 g) [1]
Doses: 0, 0.001, 0.05, 0.075, 0.1 and 0.5 nmol (prepared with artificial cerebrospinal fluid (CSF) and stored in plastic tubes at -25°C Store until use) Route of Administration: Intracerebroventricular (icv) administration, once Experimental Results:Antagonizes the analgesic effects of morphine in a dose-dependent manner, antagonizes morphine-induced hyperkinesis in a dose-dependent manner. Animal/Disease Models: Male CFLP mice (25-30 g, acute dependence on morphine induced by a single dose (100 mg/kg) morphine-HCl) [1] Doses: 0, 0.001, 0.05, 0.2 and 2 nmol Route of Administration: Intracerebroventricular (icv) administration, single Experimental Results:lowers body temperature in a dose-dependent manner and causes withdrawal hypothermia and weight loss in morphine-dependent animals. Animal/Disease Models: Long-Evans hooded rats (12, male, 350-450 g) [2] Doses: 0, 0.015, 0.15 and 1.5 nmol per side Route of Administration: Intra-VTA (ventral tegmental area) injection Experimental Results: Extracellular dopamine enha For in vivo studies, rats or mice receive the peptide (0.1-10 mg/kg) intravenously or intracerebroventricularly prior to morphine or DAMGO challenge. Antinociception and respiratory parameters are measured. Vehicle-treated animals serve as controls. |
| References | |
| Additional Infomation |
CTOP is a cyclic peptide.
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| Molecular Weight |
1062.26000
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|---|---|
| Exact Mass |
1061.45
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| CAS # |
103429-31-8
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| Related CAS # |
CTOP TFA
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| PubChem CID |
2884
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| Sequence |
{D-Phe}-Cys-Tyr-{D-Trp}-{Orn}-Thr-{Pen}-Thr-NH2 (Disulfide bridge:Cys2-Pen7){D-Phe}-CY-{D-Trp}-{Orn}T{Pen}T-NH2 (Disulfide bridge:Cys2-Pen7)
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| SequenceShortening |
{D-Phe}-CY-{D-Trp}-{Orn}T{Pen}T-NH2 (Disulfide bridge:Cys2-Pen7)
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.42g/cm3
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| Boiling Point |
1491.2ºC at 760mmHg
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| Flash Point |
855.7ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.68
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| LogP |
3.308
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
74
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| Complexity |
1930
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NCCCC1NC(=O)C(CC2=CNC3=CC=CC=C23)NC(=O)C(CC2=CC=C(O)C=C2)NC(=O)C(NC(C(CC2=CC=CC=C2)N)=O)CSSC(C)(C)C(C(NC(C(=O)N)C(O)C)=O)NC(=O)C(C(O)C)NC1=O
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| InChi Key |
PZWWYAHWHHNCHO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C50H67N11O11S2/c1-26(62)39(42(53)65)59-49(72)41-50(3,4)74-73-25-38(58-43(66)33(52)21-28-11-6-5-7-12-28)47(70)56-36(22-29-16-18-31(64)19-17-29)45(68)57-37(23-30-24-54-34-14-9-8-13-32(30)34)46(69)55-35(15-10-20-51)44(67)60-40(27(2)63)48(71)61-41/h5-9,11-14,16-19,24,26-27,33,35-41,54,62-64H,10,15,20-23,25,51-52H2,1-4H3,(H2,53,65)(H,55,69)(H,56,70)(H,57,68)(H,58,66)(H,59,72)(H,60,67)(H,61,71)
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| Chemical Name |
N-(1-amino-3-hydroxy-1-oxobutan-2-yl)-19-[(2-amino-3-phenylpropanoyl)amino]-10-(3-aminopropyl)-7-(1-hydroxyethyl)-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-3,3-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.9414 mL | 4.7069 mL | 9.4139 mL | |
| 5 mM | 0.1883 mL | 0.9414 mL | 1.8828 mL | |
| 10 mM | 0.0941 mL | 0.4707 mL | 0.9414 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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