BL-1249
| Code | Size | Price |
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| TAR-T14666-100mg | 100mg | Enquire | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| TAR-T14666-50mg | 50mg | Enquire | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃
Documents
Further Information
Bioactivity:
BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM). BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively[1][2].
CAS:
18200-13-0
Formula:
C17H17N5
Molecular Weight:
291.358
Pathway:
Membrane transporter/Ion channel
Purity:
0.98
SMILES:
C1CCc2c(C1)cccc2Nc1ccccc1-c1nnn[nH]1
Target:
Potassium Channel
References
1. Tertyshnikova S, 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. J Pharmacol Exp Ther. 2005 Apr;313(1):250-9.
2. Pope L, et al. Protein and Chemical Determinants of BL-1249 Action and Selectivity for K2P Channels. ACS Chem Neurosci. 2018 Dec 19;9(12):3153-3165.
3. Iwaki Y, et al. Towards a TREK-1/2 (TWIK-Related K+ Channel 1 and 2) dual activator tool compound: Multi-dimensional optimization of BL-1249. Bioorg Med Chem Lett. 2019 Jul 1;29(13):1601-1604.