Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
Kd: 1 nM (Ca2+-activated K+ channel)[1][3]
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ln Vitro |
Reversibly, iberiotoxin obstructs the Ca2+-activated K+ channel in the smooth muscle excised from the aortic valve of cows. Iberiotoxin has an IC50 value of roughly 250 pM and only acts at the channel's outer face. Iberiotoxin (Ki of 250 pM) partially inhibits the binding of 125I-charybdotoxin in the membrane vesicles of the bovine aortic sarcolemmal. Charybdotoxin binding is noncompetitively inhibited by iberiotoxin[1]. Treatment with iberiotoxin reduces the migration of rat mesenchymal stem cells (rMSCs) in the absence of platelet lysate (PL), indicating that BK channels control rMSC migration under normal circumstances. Iberiotoxin at 10 nM eliminates the migratory impact that PL causes in MSCs[2].
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ln Vivo |
Iberiotoxin (0.125 nmol/nl, 1.25 nmol/nl, and 12.5 nmol/nl) is pumped into the paraventricular hypothalamic nucleus (PVN) of male Wistar rats (6-7 weeks old) suffering from chronic heart failure (CHF) using osmotic minipumps. The right ventricular weight/body weight, lung weight/body weight ratio, left ventricular end-diastolic diameter, and left ventricular ejection fraction all increase and decrease following the perfusion of Iberiotoxin by microinjection of rAAV2-KCNMB4 shRNA virus[4].
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References |
[1]. A Galvez, et al. Purification and Characterization of a Unique, Potent, Peptidyl Probe for the High Conductance Calcium-Activated Potassium Channel From Venom of the Scorpion Buthus Tamulus. J Biol Chem. 1990 Jul 5;265(19):11083-90.
[2]. Santiago Echeverry, et al. Activation of BK Channel Contributes to PL-Induced Mesenchymal Stem Cell Migration. Front Physiol. 2020 Mar 24;11:210. [3]. S Candia, et al. Mode of Action of Iberiotoxin, a Potent Blocker of the Large Conductance Ca(2+)-activated K+ Channel. Biophys J. 1992 Aug;63(2):583-90. [4]. R J Wang, et al. Downregulation of Large Conductance Calcium-Activated Potassium Channels in Paraventricular Nucleus Contributes to Sympathoexcitation in Rats With Chronic Heart Failure. Zhonghua Xin Xue Guan Bing Za Zhi. 2018 Mar 24;46(3):178-186. |
Molecular Formula |
C179H274N50O55S7
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Molecular Weight |
4230.85
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CAS # |
129203-60-7
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Related CAS # |
Iberiotoxin TFA
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC(C[C@H]1C(N[C@H](C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(N[C@H]2CSSC[C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@](C(C3CCC(N3)=O)=O)(N)CC4=CC=CC=C4)=O)[C@H](O)C)=O)CC(O)=O)=O)C(C)C)=O)CC(O)=O)=O)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H]5CSSC[C@H](NC([C@@H](NC([C@@H](NC(CNC([C@@H](NC2=O)CCSC)=O)=O)CCCCN)=O)CCCCN)=O)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(O)=O)CCC(N)=O)=O)CC6=CC=C(O)C=C6)=O)CSSC[C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC5=O)CC7=CNC8=CC=CC=C78)=O)CO)=O)C(C)C)=O)C(N[C@H](C(N[C@H](C(N1)=O)CC(O)=O)=O)CCCCN)=O)=O)CCCNC(N)=N)=O)=O)CCC(O)=O)=O)CCCCN)=O)CO)=O)C(C)C)=O)CO)=O)=O)CCCCN)=O)=O)CCCNC(N)=N)=O)CC(O)=O)=O)C(C)C)=O)=O)CC9=CC=CC=C9)=O)C
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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 | 0.2364 mL | 1.1818 mL | 2.3636 mL | |
5 mM | 0.0473 mL | 0.2364 mL | 0.4727 mL | |
10 mM | 0.0236 mL | 0.1182 mL | 0.2364 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.