BL 1249 |
| Catalog No.GC10094 |
K2P2.1 (TREK-1) channel opener
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 18200-13-0
Sample solution is provided at 25 µL, 10mM.
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[(5, 6, 7, 8-tetrahydro-naphthalen-1-yl)-[2-(1H-tetrazol-5-yl)-phenyl]-amine], named BL 1249, is a putative potassium channel opener with bladder-relaxant properties. In cultured bladder smooth muscle cells, BL 1249 decreased DiBAC4 (3) fluorescence in a concentration-dependent manner with an EC50 of 1.26 ± 0.6 µM. In human bladder cells, BL 1249 resulted in hyperpolarization in a concentration-dependent manner and yielded an EC50 of 1.49±0.08 µM. BL 1249 relaxed 30 mM KCl precontracted bladder strips in a concentration-dependent manner and yielded an EC50 of 1.1 ± 0.37 µM [1].
There are several types of potassium channels in urinary bladder myocytes and they are important in determining contractility and excitability of bladder smooth muscle. These channels include maxi-K+, KATP, members of the voltage-gated Kv family, SK family and, possibly, members of the KCNQ family. Open potassium channels can increase potassium efflux from the cell and produce membrane potential hyperpolarization, thereby decrease the activation of voltage-dependent calcium channels [1].
In human bladder myocytes, BL 1249 produced large instantaneously non-inactivating, activating outward currents that were readily reversible following drug washout. The BL 1249-induced current was hence of a reversal potential of near -80 mV under the physiological K+ gradient, this indicated that the current is carried by K+ ions [1].
In anesthetized rats, BL 1249 at a concentration of 1 mg/kg significantly decreased (p< 0.01) micturition contractions during the 15-min period immediately following dosing; for the 15- to 30-min period, the decrease was significant but less (p< 0.05). Administration of BL 1249 at a concentration of 1 mg/kg had no effect on mean arterial blood pressure (MABP) during the 0- to 15-min period immediately following administration. During the 15- to 30-min period, BL 1249 administration increased MABP by less than 10% [1].
Reference:
[1]. Svetlana Tertyshnikova, Ronald J. Knox, Mary Jane Plym, et al. BL-1249 [(5, 6, 7, 8-Tetrahydro-naphthalen-1-yl)-[2-(1H-tetrazol-5-yl)-phenyl]-amine]: A Putative Potassium Channel Opener with Bladder-Relaxant Properties. The Journal of Pharmacology and Experimental Therapeutics, 2015, 313(1):250-259.
| Cas No. | 18200-13-0 | SDF | |
| Chemical Name | N-(2-(2H-tetrazol-5-yl)phenyl)-5,6,7,8-tetrahydronaphthalen-1-amine | ||
| Canonical SMILES | C1(CCCCC1=CC=C2)=C2NC3=CC=CC=C3C4=NNN=N4 | ||
| Formula | C17H17N5 | M.Wt | 291.35 |
| Solubility | <29.14mg/ml in 1eq. NaOH; <29.14mg/ml in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.4323 mL | 17.1615 mL | 34.323 mL |
| 5 mM | 0.6865 mL | 3.4323 mL | 6.8646 mL |
| 10 mM | 0.3432 mL | 1.7161 mL | 3.4323 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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