| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Large-conductance calcium-activated potassium channel (BK channel) (EC50 = 251 nM).
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|---|---|
| ln Vitro |
A concentration-dependent, negative shift in the V1/2 is caused by GoSlo-SR-5-69[1].
GoSlo-SR-5-69 causes a concentration-dependent, negative shift in the V1/2, meaning it makes BK channels easier to open, even in the absence of high intracellular calcium. The EC50 for this effect is 251 nM. |
| ln Vivo |
No specific in vivo data is available. However, BK channel activators are known to have vasorelaxant effects, lowering blood pressure, and can modulate neuronal excitability. GoSlo-SR-5-69 would likely have similar in vivo effects, but further studies are required.
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| Enzyme Assay |
Recombinant human BK channels (encoded by KCNMA1) are expressed in HEK293 cells. Inside-out or whole-cell patch-clamp recordings are performed. The compound is applied to the intracellular (or extracellular) side, and the shift in the voltage dependence of activation (V1/2) is measured. EC50 is calculated.
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| Cell Assay |
HEK293 cells stably expressing BK channels are cultured in DMEM with 10% FBS. Whole-cell patch-clamp electrophysiology is performed using an internal solution with low Ca2+ buffering. The test compound is applied at varying concentrations, and the activation of BK current is measured. EC50 is determined.
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| Animal Protocol |
In vivo studies can be performed using BK channel activators like GoSlo-SR-5-69. Typically, the compound is formulated in a suitable vehicle (e.g., 10% DMSO, 40% PEG300, 5% Tween-80, 45% saline) and administered intravenously or intraperitoneally to rats or mice. Blood pressure is measured via a catheter.
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| ADME/Pharmacokinetics |
No specific PK data is available. The compound has a molecular weight of 470.47 and is soluble in DMSO. Its high molecular weight and polar groups may limit oral bioavailability, but it can be formulated for intravenous or intraperitoneal administration.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available. As a BK channel activator, it could cause hypotension at high doses. Care should be taken when handling as it may be harmful if absorbed through the skin. For research use only.
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| References |
[1]. Subhrangsu Roy, et al. Development of GoSlo-SR-5-69, a potent activator of large conductance Ca2+-activated K+ (BK) channels. Eur J Med Chem. 2014 Mar 21;75:426-37.
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| Additional Infomation |
GoSlo-SR-5-69 is a potent and specific BK channel activator used as a research tool to study the role of BK channels in various physiological processes, including smooth muscle tone, neuronal firing, and hearing.
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| Molecular Formula |
C24H19N2NAO5S
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|---|---|
| Molecular Weight |
470.47
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| Exact Mass |
470.091
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| CAS # |
1363419-31-1
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| PubChem CID |
56944133
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
33
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| Complexity |
861
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C([H])=C(C2C(C3=C([H])C([H])=C([H])C([H])=C3C(C=2C=1N([H])[H])=O)=O)N([H])C1C([H])=C([H])C2=C(C=1[H])C([H])([H])C([H])([H])C([H])([H])C2([H])[H])(=O)(=O)[O-].[Na+]
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| InChi Key |
JOJJZTFRBZWSBX-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C24H20N2O5S.Na/c25-22-19(32(29,30)31)12-18(26-15-10-9-13-5-1-2-6-14(13)11-15)20-21(22)24(28)17-8-4-3-7-16(17)23(20)27;/h3-4,7-12,26H,1-2,5-6,25H2,(H,29,30,31);/q;+1/p-1
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| Chemical Name |
sodium;1-amino-9,10-dioxo-4-(5,6,7,8-tetrahydronaphthalen-2-ylamino)anthracene-2-sulfonate
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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 | 2.1255 mL | 10.6277 mL | 21.2553 mL | |
| 5 mM | 0.4251 mL | 2.1255 mL | 4.2511 mL | |
| 10 mM | 0.2126 mL | 1.0628 mL | 2.1255 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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