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品質等級
化驗
≥98% (HPLC)
形狀
solid
儲存條件
protect from light
顏色
pink to brown
溶解度
DMSO: ~17.5 mg/mL
H2O: insoluble
儲存溫度
−20°C
SMILES 字串
C1CCc2c(C1)cccc2Nc3ccccc3-c4nnn[nH]4
InChI
1S/C17H17N5/c1-2-8-13-12(6-1)7-5-11-15(13)18-16-10-4-3-9-14(16)17-19-21-22-20-17/h3-5,7,9-11,18H,1-2,6,8H2,(H,19,20,21,22)
InChI 密鑰
YYNRZIFBTOUICE-UHFFFAOYSA-N
一般說明
BL-1249 is a non-steroid anti-inflammatory drug and an inhibitor of the cyclooxygenase (COX) enzyme.
應用
BL-1249 has been used:
- as an activator of mechano-gated K2P channel in contracted mouse ileum and colon tissues
- as a TWIK related potassium channel (TREK2) modulator and in U-2 OS osteosarcoma cell line
- as a TREK1 and TREK2 activator in mice.
生化／生理作用
BL-1249 also activates TWIK related potassium channel 2 (TREK2). It interacts with K2P channel at the negatively charged activator site and modulates channel opening.
BL-1249 is a putative activator of potassium TREK-1 channel.
特點和優勢
This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
訊號詞
Warning
危險分類
Aquatic Chronic 4 - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
標靶器官
Respiratory system
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
個人防護裝備
dust mask type N95 (US), Eyeshields, Gloves
Svetlana Tertyshnikova et al.
The Journal of pharmacology and experimental therapeutics, 313(1), 250-259 (2004-12-21)
BL-1249 [(5,6,7,8-tetrahydro-naphthalen-1-yl)-[2-(1H-tetrazol-5-yl)-phenyl]-amine] produced a concentration-dependent membrane hyperpolarization of cultured human bladder myocytes, assessed as either a reduction in fluorescence of the voltage-sensitive dye bis-(1,2-dibutylbarbituric acid)trimethine oxonol (EC50 = 1.26 +/- 0.6 microM) or by direct electrophysiological measurement (EC50 = 1.49
Paul D Wright et al.
Biochemical and biophysical research communications, 520(1), 35-40 (2019-10-01)
TREK2 (KCNK10, K2P10.1) is a two-pore domain potassium (K2P) channel and a potential target for the treatment of pain. Like the majority of the K2P superfamily, there is currently a lack of useful pharmacological tools to study TREK2. Here we
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