| 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).
|
|---|---|
| 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.
|
| 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.
|
| Molecular Formula |
C24H19N2NAO5S
|
|---|---|
| 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 |
Blue to dark blue solid
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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
|
| Heavy Atom Count |
33
|
| Complexity |
861
|
| Defined Atom Stereocenter Count |
0
|
| 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+]
|
| 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
|
| 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 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: ~50 mg/mL (~106.3 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.31 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (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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