| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Obestatin (rat) TFA has been reported as an endogenous ligand for the orphan G protein-coupled receptor 39 (GPR39). Early studies demonstrated that obestatin binding to GPR39 stimulates cAMP production and regulates downstream signaling pathways. However, it should be noted that the ligand-receptor relationship between obestatin and GPR39 remains highly controversial in the scientific community, as multiple subsequent independent studies have failed to replicate this finding, failing to detect specific binding or functional activation of GPR39 by obestatin. Therefore, the true physiological target remains to be identified.
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| ln Vitro |
In vitro studies have demonstrated various biological activities of Obestatin (rat) TFA. At the biochemical level, the peptide binds to membranes from GPR39-overexpressing cells with a Kd value of approximately 1 nM and stimulates cAMP production. At the tissue level, obestatin inhibits ghrelin-induced contractions of isolated mouse jejunum muscle strips. At the cellular level, obestatin has also been reported to promote cell survival, inhibit apoptosis, and exhibit antioxidant properties.
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| ln Vivo |
The classic in vivo effects of Obestatin (rat) TFA include suppression of food intake and reduction of body weight. Early studies showed that in fasted mice, obestatin suppresses food intake in a time-dependent and dose-dependent manner and reduces gastric emptying. In normal rats, obestatin inhibits jejunal contractions and reduces body weight gain. Additionally, obestatin has demonstrated anti-myocardial infarction and anti-inflammatory effects. It should be noted that these early findings have been challenged by subsequent independent studies, with many failing to replicate the appetite-suppressing effects of obestatin.
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| Enzyme Assay |
Receptor binding studies for obestatin are typically performed using radioligand binding assays. Briefly, membrane homogenates are prepared from GPR39-overexpressing cells (e.g., CHO or HEK293 cells) and incubated with ¹²⁵I-labeled obestatin (tracer) in binding buffer, along with various concentrations of unlabeled obestatin for competition binding. Following incubation at room temperature for 60-90 minutes, the reaction is terminated by rapid vacuum filtration, and filters are washed with ice-cold buffer. After drying, retained radioactivity on filters is measured using a gamma counter to calculate specific binding percentage, and competition binding curves are fitted to obtain Kd and IC₅₀ values. Membranes from non-transfected cells serve as negative controls.
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| Cell Assay |
GPR39-overexpressing CHO or HEK293 cells are seeded into 24-well or 96-well culture plates and cultured in medium containing 10% fetal bovine serum to 70-80% confluence. After serum starvation for synchronization (12-24 hours), various concentrations of Obestatin (rat) TFA (e.g., 0.1-1000 nM) are added. For cAMP detection, cells are stimulated in the presence of IBMX for 15-30 minutes, then lysed, and intracellular cAMP accumulation is measured by competitive ELISA or radioimmunoassay. For calcium mobilization assays, cells are loaded with calcium-sensitive dyes (e.g., Fluo-4 AM), and fluorescence changes upon obestatin addition are monitored using a fluorescence microplate reader.
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| Animal Protocol |
Six-to-eight-week-old male C57BL/6 mice or Sprague-Dawley rats are used. Animals are fasted overnight (16-18 hours) prior to experiments with free access to water. Obestatin (rat) TFA is dissolved in saline and administered intraperitoneally at doses ranging from 12.5-1000 nmol/kg, with injection volumes of 0.1-0.2 mL/10g body weight. Post-administration, cumulative food and water intake are measured at specific time points (e.g., 1, 2, 4, 6, 12 hours). For gastric emptying assays, a test meal containing phenol red is administered by gavage, animals are euthanized after 15-30 minutes, and gastric residual phenol red is measured. Each experimental group typically contains 8-12 animals.
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| ADME/Pharmacokinetics |
As a peptide molecule, obestatin exhibits pharmacokinetic characteristics typical of peptide drugs. Studies indicate that obestatin has a short biological half-life and is rapidly degraded in vivo. The peptide has extremely low oral bioavailability and is typically administered via injection routes (intraperitoneal, subcutaneous, or intravenous). The TFA salt form is intended to improve the stability of the lyophilized peptide for storage and experimental handling.
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| Toxicity/Toxicokinetics |
Toxicological data on Obestatin (rat) TFA are currently limited. In published in vivo studies, obestatin at experimental doses (e.g., 12.5-1000 nmol/kg intraperitoneal injection) has not been reported to cause significant acute toxicity reactions or behavioral abnormalities. Body weight and general condition of study animals remained normal during the experimental period. Since obestatin has not yet entered human clinical trials, safety data including long-term toxicity, genotoxicity, reproductive toxicity, and carcinogenicity are completely absent. Relevant products are explicitly stated for research use only and are not for human use.
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| References |
| Molecular Formula |
C116H175F3N34O33
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|---|---|
| Molecular Weight |
2630.83
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| CAS # |
1312186-27-8
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| Related CAS # |
Obestatin(rat);869705-22-6
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| Appearance |
Typically exists as solid at room temperature
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| Synonyms |
Obestatin (rat) trifluoroacetic 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 |
| 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 | 0.3801 mL | 1.9005 mL | 3.8011 mL | |
| 5 mM | 0.0760 mL | 0.3801 mL | 0.7602 mL | |
| 10 mM | 0.0380 mL | 0.1901 mL | 0.3801 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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