Size | Price | |
---|---|---|
100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
IC50: 1-3 nM (KV2 channels); 24-54 nM (KV4.3 channels)[2]
|
---|---|
ln Vitro |
Guangxitoxin 1E has an IC50 of 1-3 nM for KV2 inhibition, however it has no discernible effect on the potassium channels KV1.2, KV1.3, KV1.5, KV3.2, and BK, nor on the calcium and sodium channels CaV1.2,caV2. When it comes to KV4.3 channels, the IC50 is 24-54 nM[2], while it is 2, NaV1.5, NaV1.7, and NaV1.8. 90% of IDR and KV2 are inhibited by Guangxitoxin 1E in mouse β-cells. 1. As gating-modifier peptides are known to do, this causes the voltage dependency of channel activation to shift to greater depolarized potentials. Guangxitoxin 1E increases insulin production from mice pancreatic islets in a glucose-dependent manner, augments intracellular calcium oscillations induced by glucose, and broadens the β-cell action potential[2].
|
References |
[1]. Hönigsperger C, et al. Physiological roles of Kv2 channels in entorhinal cortex layer II stellate cells revealed by Guangxitoxin-1E. J Physiol. 2017 Feb 1;595(3):739-757.
[2]. Herrington J, et al. Blockers of the delayed-rectifier potassium current in pancreatic beta-cells enhance glucose-dependent insulin secretion. Diabetes. 2006 Apr;55(4):1034-42. |
Molecular Formula |
C178H248N44O45S7
|
---|---|
Molecular Weight |
3948.61
|
CAS # |
1233152-82-3
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
S(C)CCC(C(N1CCCC1C(=O)O)=O)NC(C1CCCN1C(C(CC1C=CC=CC=1)NC(C(CC(N)=O)NC(C1CSSCC2C(NC3CSSCC(C(NCC(NCC(NC(CC4C=CC=CC=4)C(NC(CC4=CNC5C=CC=CC4=5)C(NC(CC4=CNC5C=CC=CC4=5)C(NC(CCCCN)C(NC(C(NCC(NC(CO)C(NCC(NC(CCCCN)C(N4CCCC4C(NC(C)C(N2)=O)=O)=O)=O)=O)=O)=O)CSSCC(C(NC(CO)C(N2CCCC2C(NC(C(NC(C(NCC(NC(CC(C)C)C(N1)=O)=O)=O)CC1=CNC2C=CC=CC1=2)=O)CCCCN)=O)=O)=O)NC(C(C(C)C)NC(C(CC1C=CC(=CC=1)O)NC(C(CCCCN)NC(C1CCCN1C3=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)NC(C(CCC(=O)O)NC(CNC(C(CCC(=O)O)N)=O)=O)=O)=O)=O)=O)=O)=O
|
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: ≥ 1 mg/mL (0.25 mM)
|
---|---|
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 | 0.2533 mL | 1.2663 mL | 2.5325 mL | |
5 mM | 0.0507 mL | 0.2533 mL | 0.5065 mL | |
10 mM | 0.0253 mL | 0.1266 mL | 0.2533 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.