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| 5mg |
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| Targets |
Catestatin acts on multiple targets. It inhibits catecholamine release from adrenal chromaffin cells and adrenergic neurons by acting on the neuronal nicotinic acetylcholine receptor (nAChR). It stimulates histamine release from mast cells via heterotrimeric G proteins in a receptor-independent manner. Catestatin also acts as a potent vasodilator in rats and humans, reducing blood pressure. Its effects are mediated, at least in part, by histamine release and action at H1 receptors. Catestatin also activates the PI3K/Akt/eNOS signaling pathway, contributing to its cardioprotective and angiogenic effects. It also reduces ROS generation from mitochondrial ETC electron leakage.
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| ln Vitro |
In vitro, catestatin (0.1-100 uM) inhibits nicotine-evoked catecholamine secretion from bovine adrenal chromaffin cells with an IC₅0 of approximately 0.7 uM. It also inhibits catecholamine release induced by acetylcholine, electrical stimulation, and high K+. Catestatin stimulates histamine release from rat peritoneal mast cells and human skin mast cells (EC₅0 ~1-10 uM). It induces vasodilation in isolated rat aortic rings pre-contracted with phenylephrine (EC₅0 ~0.1-1 uM). Catestatin has antioxidant activity, scavenging free radicals in cell-free assays. It also promotes angiogenesis in endothelial cell tube formation assays (EC₅0 ~1-10 ug/mL).
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| Enzyme Assay |
The binding of catestatin to the nicotinic acetylcholine receptor (nAChR) can be assessed by radioligand binding assays. Membranes from bovine adrenal medulla or cells expressing nAChR subunits (e.g., alpha3beta4) are incubated with a radiolabeled nAChR antagonist (e.g., [3H]-epibatidine, 0.5-1 nM) and varying concentrations of catestatin (0.01-100 uM) in binding buffer at 25degC for 60 min. Bound radioactivity is separated by filtration, and the IC₅0 is calculated. For G protein activation, GTPgammaS binding is measured as described for Mastoparan X.
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| Cell Assay |
For catecholamine release assays, bovine adrenal chromaffin cells are isolated and cultured in 24-well plates (3-5×10⁵ cells/well). Cells are pre-incubated with catestatin (0.1-100 uM) for 10-30 min, then stimulated with nicotine (10-100 uM) or acetylcholine (100-500 uM) for 5-10 min. The supernatant is collected, and catecholamine (norepinephrine, epinephrine) concentration is measured by HPLC-ECD or ELISA. For mast cell degranulation, rat peritoneal mast cells are isolated and treated with catestatin (0.1-100 uM) for 30 min, and histamine release is measured by ELISA. For angiogenesis assays, HUVECs are seeded on Matrigel-coated 96-well plates with catestatin (0.1-10 ug/mL), and tube formation is quantified after 6-18 h.
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| Animal Protocol |
In vivo, catestatin (1-100 ug/kg, IV) reduces blood pressure in rats and humans. Intravenous administration of catestatin in spontaneously hypertensive rats (SHR) or normotensive rats produces a dose-dependent decrease in mean arterial pressure (MAP). The vasodilator effect is mediated, at least in part, by histamine release. In a mouse model of myocardial ischemia-reperfusion (I/R) injury, catestatin (0.1-1 mg/kg, IV) reduces infarct size and improves cardiac function. In chromogranin A knockout (CgA-/-) mice, which are hypertensive, exogenous catestatin rescues hypertension. Catestatin also improves diastolic dysfunction and left ventricular compliance in TAC/DOCA mice. The peptide is not an approved drug but is a research tool for studying cardiovascular disease.
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| ADME/Pharmacokinetics |
For in vivo studies, catestatin is administered by intravenous (IV) injection. In rats, catestatin (1-100 ug/kg) is injected IV, and blood pressure is measured via a carotid artery cannula. Heart rate is monitored by ECG. For ischemia-reperfusion (I/R) studies, rats or mice are subjected to 30 min of left anterior descending (LAD) coronary artery occlusion followed by 24 h or 2-4 weeks of reperfusion. Catestatin (0.1-1 mg/kg) is administered IV 10-30 min before reperfusion or at the onset of reperfusion. Infarct size is measured by TTC staining. Cardiac function is assessed by echocardiography (ejection fraction, fractional shortening). For hypertension studies, catestatin is administered IV, and blood pressure is monitored for 30-60 min. For chronic studies, catestatin can be administered via subcutaneous osmotic minipump (0.1-0.5 mg/kg/day) for 2-4 weeks.
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| Toxicity/Toxicokinetics |
No specific PK data for catestatin is available. As a 21-amino acid peptide (MW 2326.68), it has a very short plasma half-life (< 15 min) due to proteolytic degradation. It is rapidly cleared by the kidneys. For research use, it is stored as a lyophilized powder at -20degC (powder: -20degC for 3 years, 4degC for 2 years; in solvent: -80degC for 1 year, -20degC for 6 months). It is soluble in DMSO and water.
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| References | |
| Additional Infomation |
Catestatin (human) is a research-grade 21-amino acid peptide derived from chromogranin A. It is not an FDA-approved drug. It is used as a tool for studying cardiovascular function, hypertension, catecholamine secretion, and inflammation. For research use only, not for diagnostic or therapeutic applications. Storage: powder at -20degC for 3 years, 4degC for 2 years; in solvent at -80degC for 1 year, -20degC for 6 months.
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| Molecular Formula |
C104H164N32O27S
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|---|---|
| Molecular Weight |
2326.68
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| Exact Mass |
2326.22
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| CAS # |
197151-46-5
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| Related CAS # |
1461673-77-7
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| PubChem CID |
71300629
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.669
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| LogP |
-3.9
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| Hydrogen Bond Donor Count |
35
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| Rotatable Bond Count |
77
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| Heavy Atom Count |
164
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| Complexity |
5000
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| Defined Atom Stereocenter Count |
18
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| SMILES |
NC(C(NC(C(NC(C(NC(C(NC(C(NC(C(NC(C(NC(C(NC(C(NC(C(NC(C(NC(C(NCC(NC(C(NC(C(NCC(N1CCCC1C(NCC(N1CCCC1C(NC(C(NC(C(O)=O)CC(C)C)=O)CCC(=O)N)=O)=O)=O)=O)=O)CCCNC(=N)N)=O)CC1C=CC=CC=1)=O)=O)CC1C=CC(O)=CC=1)=O)C)=O)CCCNC(=N)N)=O)C)=O)CCCNC(=N)N)=O)CC1C=CC=CC=1)=O)CO)=O)CC(C)C)=O)CCCCN)=O)CCSC)=O)CO)=O)CO
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| InChi Key |
VNFWSNGCDNCFNT-HVZFAYPJSA-N
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| InChi Code |
InChI=1S/C104H164N32O27S/c1-56(2)45-71(130-91(152)66(25-14-15-38-105)125-93(154)70(37-44-164-7)127-97(158)76(54-138)133-86(147)64(106)53-137)94(155)134-77(55-139)98(159)131-74(48-61-23-12-9-13-24-61)96(157)126-68(28-18-41-116-104(112)113)90(151)120-58(5)84(145)123-67(27-17-40-115-103(110)111)89(150)121-59(6)85(146)129-72(49-62-31-33-63(140)34-32-62)88(149)117-50-81(142)122-73(47-60-21-10-8-11-22-60)95(156)124-65(26-16-39-114-102(108)109)87(148)118-51-82(143)135-42-19-29-78(135)99(160)119-52-83(144)136-43-20-30-79(136)100(161)128-69(35-36-80(107)141)92(153)132-75(101(162)163)46-57(3)4/h8-13,21-24,31-34,56-59,64-79,137-140H,14-20,25-30,35-55,105-106H2,1-7H3,(H2,107,141)(H,117,149)(H,118,148)(H,119,160)(H,120,151)(H,121,150)(H,122,142)(H,123,145)(H,124,156)(H,125,154)(H,126,157)(H,127,158)(H,128,161)(H,129,146)(H,130,152)(H,131,159)(H,132,153)(H,133,147)(H,134,155)(H,162,163)(H4,108,109,114)(H4,110,111,115)(H4,112,113,116)/t58-,59-,64-,65-,66-,67-,68-,69-,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-5-amino-2-[[(2S)-1-[2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoic acid
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| Synonyms |
197151-46-5; DTXSID90173378; RefChem:123990; DTXCID2095869; Catestatin; Human chromogranin A 352–372
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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) |
DMSO : ~100 mg/mL (~42.98 mM; with ultrasonication)
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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 | 0.4298 mL | 2.1490 mL | 4.2980 mL | |
| 5 mM | 0.0860 mL | 0.4298 mL | 0.8596 mL | |
| 10 mM | 0.0430 mL | 0.2149 mL | 0.4298 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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