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| Targets |
Xenopsin targets neurotensin receptors, as it is a neurotensin-like peptide that shares sequence homology with mammalian neurotensin. It inhibits neurotensin binding to rat brain synaptic membranes with a Ki = 1.5. The compound's biological properties are mediated through its interaction with neurotensin receptors, which are G protein-coupled receptors involved in the regulation of various physiological processes including pain, temperature regulation, and gastrointestinal function. Xenopsin is a photopigment that is expanding our understanding of the evolution and diversity of vision in invertebrates.
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| ln Vitro |
Xenopsin is a bioactive octapeptide found in Xenopus laevis skin extracts [1]. The secretion of stomach acid induced by tetragastrin can be markedly inhibited by xenopsin [2].
In vitro studies have demonstrated that xenopsin is a bioactive octapeptide found in Xenopus laevis skin extracts. It inhibits neurotensin binding to rat brain synaptic membranes with a Ki of 1.5. The compound shows sequence homology to mammalian neurotensin and shares a number of its biological properties. Xenopsin inhibits gastrin-stimulated gastric acid secretion. The compound's in vitro activity has been characterized in receptor binding assays and functional assays measuring neurotensin receptor-mediated signaling. Its activity as a neurotensin receptor ligand makes it a valuable tool for studying neurotensin receptor function. |
| ln Vivo |
In vivo studies have shown that xenopsin inhibits gastrin-stimulated gastric acid secretion. As a neurotensin-like peptide, xenopsin shares biological properties with mammalian neurotensin, which is involved in the regulation of gastrointestinal function, pain perception, and thermoregulation. The compound's effects on gastric acid secretion have been documented, and it may have additional in vivo effects consistent with neurotensin receptor activation. However, detailed in vivo data for xenopsin beyond its effects on gastric acid secretion are limited. The compound is a naturally occurring peptide from Xenopus skin.
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| Enzyme Assay |
The in vitro receptor binding assay for xenopsin typically involves competition binding studies using membrane preparations from rat brain synaptic membranes. Radiolabeled neurotensin (e.g., ¹2⁵I-neurotensin or 3H-neurotensin) is incubated with membrane preparations and varying concentrations of xenopsin (typically 0.001 nM to 10 uM) in binding buffer (e.g., 50 mM Tris-HCl, pH 7.4, containing 0.1% BSA and protease inhibitors) at 4degC for 1-2 hours. Bound and free ligand are separated by filtration through glass fiber filters, and radioactivity is measured by gamma counting or scintillation counting. The inhibition constant (Ki) is calculated from IC50 values. Non-specific binding is determined in the presence of excess unlabeled neurotensin.
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| Cell Assay |
In vitro cellular assays for xenopsin are conducted using cell lines expressing neurotensin receptors, such as HT-29 or N1E-115 cells. Cells are seeded in 96-well or 24-well plates and treated with varying concentrations of xenopsin (typically 0.001 nM to 10 uM) for 15-60 minutes. Neurotensin receptor activation is assessed by measuring intracellular calcium mobilization using fluorescent calcium indicators (e.g., Fluo-4) or by measuring inositol phosphate accumulation. The compound's ability to activate or inhibit neurotensin receptor-mediated signaling is determined by comparing its effects to those of neurotensin. Receptor internalization may also be assessed by immunofluorescence staining of the neurotensin receptor. Cell viability is monitored to ensure that observed effects are not due to cytotoxicity.
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| Animal Protocol |
In vivo animal studies for xenopsin typically involve administration to rodents to assess its effects on gastric acid secretion and other neurotensin-mediated functions. The compound can be administered by intravenous, intraperitoneal, or intracerebroventricular injection at doses ranging from 0.01-10 mg/kg. Gastric acid secretion is measured in pylorus-ligated rats or by using gastric fistula models. The compound's effects on pain perception, body temperature, and gastrointestinal motility may also be assessed. Detailed protocols for in vivo studies with xenopsin are not extensively documented in the available literature, though the compound has been shown to inhibit gastrin-stimulated gastric acid secretion.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of xenopsin are characteristic of a peptide. The compound has a molecular weight of 980.2 g/mol and a molecular formula of C47H73N13O10. As a peptide, it is expected to have limited oral bioavailability and a short half-life due to rapid proteolytic degradation. The compound is typically administered by injection in research studies. It should be stored at 2-8degC. The compound is available for research purposes only. Detailed ADME parameters such as half-life, clearance, and bioavailability are not extensively documented in the available literature.
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| Toxicity/Toxicokinetics |
The toxicological profile of xenopsin is characteristic of a neurotensin-like peptide. As a naturally occurring peptide found in Xenopus skin, it is generally considered to have low toxicity in the context of research applications. The compound is for research use only and is not intended for human therapeutic use. Standard safety precautions should be followed when handling peptides in a laboratory setting. No specific LD50 values or detailed toxicity profiles have been reported. The compound's effects on gastric acid secretion and other physiological processes are dose-dependent and related to its neurotensin receptor agonist activity.
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| References | |
| Additional Infomation |
There are reports and data regarding the presence of xenopsin in the African clawed frog (Xenopus laevis).
See also: xenopsin (note moved to). Xenopsin (CAS 51827-01-1) is a neurotensin-like octapeptide from Xenopus laevis skin at the carboxyl terminus of its precursor. It shows sequence homology to mammalian neurotensin and shares a number of its biological properties. Xenopsin inhibits gastrin-stimulated gastric acid secretion and inhibits neurotensin binding to rat brain synaptic membranes (Ki = 1.5). The compound is also known as a recently characterized photopigment that is expanding our understanding of the evolution and diversity of vision in invertebrates. It is available for research purposes only with purity >98%. |
| Molecular Formula |
C47H73N13O10
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| Molecular Weight |
980.16362
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| Exact Mass |
979.56
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| CAS # |
51827-01-1
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| Related CAS # |
Xenopsin TFA
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| PubChem CID |
11766461
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| Appearance |
White to off-white solid powder
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| Density |
1.43g/cm3
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| Index of Refraction |
1.664
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| LogP |
3.592
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
28
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| Heavy Atom Count |
70
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| Complexity |
1860
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)O)NC(=O)[C@H](CC1=CNC2=CC=CC=C21)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@@H]4CCC(=O)N4
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| InChi Key |
VVZLRNZUCNGJQY-KITDWFFGSA-N
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| InChi Code |
InChI=1S/C47H73N13O10/c1-5-27(4)39(44(67)58-35(46(69)70)22-26(2)3)59-42(65)34(23-28-24-52-30-13-7-6-12-29(28)30)57-43(66)36-16-11-21-60(36)45(68)33(15-10-20-51-47(49)50)56-41(64)31(14-8-9-19-48)55-38(62)25-53-40(63)32-17-18-37(61)54-32/h6-7,12-13,24,26-27,31-36,39,52H,5,8-11,14-23,25,48H2,1-4H3,(H,53,63)(H,54,61)(H,55,62)(H,56,64)(H,57,66)(H,58,67)(H,59,65)(H,69,70)(H4,49,50,51)/t27-,31-,32-,33-,34-,35-,36-,39-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]acetyl]amino]hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic 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) |
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 | 1.0202 mL | 5.1012 mL | 10.2024 mL | |
| 5 mM | 0.2040 mL | 1.0202 mL | 2.0405 mL | |
| 10 mM | 0.1020 mL | 0.5101 mL | 1.0202 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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