| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Catestatin TFA targets the nicotinic acetylcholine receptors (nAChRs) as a non-competitive antagonist. It inhibits catecholamine secretion from chromaffin cells and noradrenergic neurons. The peptide acts as a key pleiotropic regulator of the cardiovascular system, inflammatory processes, autoimmune reactions, and metabolic homeostasis. By blocking nAChRs, it decreases blood pressure through stimulating histamine release, inhibiting catecholamine secretion, and causing vasodilation.
|
|---|---|
| ln Vitro |
In vitro, Catestatin TFA functions as a non-competitive nicotinic antagonist to inhibit catecholamine release from chromaffin cells via nAChRs. It is also recognized to possess antimicrobial effects against various bacterial strains. The peptide exhibits cardioprotective properties and has been shown to influence the reperfusion injury salvage kinase (RISK) signalling pathway and activate mitoKATP channels in cellular models.
|
| ln Vivo |
In vivo, Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure. It decreases blood pressure by stimulating histamine release, inhibiting catecholamine secretion, and causing vasodilation in the peripheral system. It has also been shown to dilate human blood vessels in vivo, particularly in females. The peptide is involved in the pathogenesis of arterial hypertension, coronary artery disease, and heart failure.
|
| Enzyme Assay |
Binding of Catestatin TFA to nAChRs is typically assessed using radioligand binding assays on membrane preparations from cells expressing nAChR subtypes. Various concentrations of the peptide are incubated with a labeled nicotinic antagonist (e.g., [3H]-epibatidine) in a binding buffer. After incubation, bound and free radioligands are separated by filtration, and radioactivity is measured to calculate Ki or IC₅0 values. The non-competitive nature can be confirmed by Schild plot analysis.
|
| Cell Assay |
For cellular assays, cells expressing nAChRs, such as bovine adrenal chromaffin cells, are pre-treated with various concentrations of Catestatin TFA for a defined period. Cells are then stimulated (e.g., with nicotine or depolarizing agents) to trigger catecholamine release. The culture medium is collected, and catecholamine levels (epinephrine, norepinephrine) are quantified by HPLC-ECD or ELISA. The half-maximal inhibitory concentration (IC₅0) for inhibition of catecholamine release is then calculated.
|
| Animal Protocol |
In vivo animal studies for Catestatin TFA are performed using rodent models (rats or mice) to study its cardiovascular effects. A typical protocol involves administering Catestatin TFA via intravenous injection at doses ranging from 10 to 100 ug/kg. Blood pressure is continuously monitored via a catheter inserted into the carotid artery. Endpoints include changes in mean arterial pressure (MAP) and heart rate. Additionally, blood samples may be collected to measure plasma catecholamine levels.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for Catestatin TFA are not extensively detailed in standard product literature. As a 21-amino acid endogenous peptide, its PK profile is characteristic of native peptides. It has a relatively short half-life in the circulation due to rapid proteolytic degradation by peptidases and renal clearance. The peptide is not orally bioavailable and is typically administered via intravenous or intraperitoneal routes in research settings.
|
| Toxicity/Toxicokinetics |
Comprehensive toxicological data for Catestatin TFA are not provided in standard product literature. As an endogenous peptide, it is generally well-tolerated at physiological concentrations. At research-use doses, no specific toxicities have been extensively reported. For laboratory use, standard chemical safety precautions for handling peptides should be followed, including the use of appropriate personal protective equipment.
|
| References |
|
| Additional Infomation |
Catestatin TFA has the molecular formula C10₉H1₇4F3N3₇O2₈S and a molecular weight of 2539.84. The peptide sequence is Arg-Ser-Met-Arg-Leu-Ser-Phe-Arg-Ala-Arg-Gly-Tyr-Gly-Phe-Arg-Gly-Pro-Gly-Leu-Gln-Leu. It appears as a white to off-white solid powder. The compound is stored at -20degC or -80degC, sealed, and away from moisture. It is soluble in water at 20 mg/mL with ultrasonic and heating to 60degC.
|
| Molecular Formula |
C109H174F3N37O28S
|
|---|---|
| Molecular Weight |
2539.84
|
| Related CAS # |
Catestatin;142211-96-9
|
| Sequence |
Arg-Ser-Met-Arg-Leu-Ser-Phe-Arg-Ala-Arg-Gly-Tyr-Gly-Phe-Arg-Gly-Pro-Gly-Leu-Gln-Leu
|
| SequenceShortening |
RSMRLSFRARGYGFRGPGLQL
|
| Appearance |
White to off-white solid powder
|
| Synonyms |
Catestatin TFA; DTXSID90173378; RefChem:123990; DTXCID2095869;
|
| 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, 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)
|
| Solubility (In Vitro) |
H2O :~20 mg/mL (~7.87 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 7.14 mg/mL (2.81 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3937 mL | 1.9686 mL | 3.9373 mL | |
| 5 mM | 0.0787 mL | 0.3937 mL | 0.7875 mL | |
| 10 mM | 0.0394 mL | 0.1969 mL | 0.3937 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
