Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BL-1249 is a selective and potent non-steroidal potassium channel activator with anti-inflammatory activity that activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 34,000 | |||
10 mg | 在庫あり | ¥ 52,500 | |||
25 mg | 在庫あり | ¥ 105,500 | |||
50 mg | 在庫あり | ¥ 186,500 | |||
100 mg | 在庫あり | ¥ 294,000 | |||
500 mg | 在庫あり | ¥ 594,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 37,500 |
説明 | BL-1249 is a selective and potent non-steroidal potassium channel activator with anti-inflammatory activity that activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2). |
ターゲット&IC50 | TREK2:8.0 μM (EC50), Smooth muscle cells (SMCs):21.0 μM (Human, EC50), TREK1:5.5 μM (EC50) |
In vitro | Evaluated by a decrease in fluorescence of the voltage-sensitive dye bis(1,2-dibutylbarbituric acid)trimethine oxonol (EC50 = 1.26 +/- 0.6 μM) or direct electrophysiological measurements (EC50 = 1.49 +/- 0.08 μM), BL-1249 demonstrates concentration-dependent membrane depolarization in cultured human bladder smooth muscle cells[2]. Patch clamp experiments indicate that, akin to a diverse range of other TREK subfamily gating signals, BL-1249 stimulates a selective screening 'C-type' gate that controls K2P functionality. BL-1249 exhibits selectivity within the TREK subfamily, activating K2P2.1 (TREK-1) and K2P10.1 (TREK-2) approximately 10 times more actively than K2P4.1 (TRAAK). Studies on mutants and K2P2.1 (TREK-1)/K2P4.1 (TRAAK) chimeras highlight the critical role of the C-terminal tail in the action of BL-1249, and identify the M2/M3 transmembrane helix interface as a key site of BL-1249 selectivity[1]. |
In vivo | In an anesthetized rat model, BL-1249 (1 mg/kg i.v.) decreased the number of isovolumic contractions, without significantly affecting blood pressure. Thus, BL-1249 behaves as a potassium channel activator that exhibits bladder versus vascular selectivity both in vitro and in vivo[2]. |
分子量 | 291.35 |
分子式 | C17H17N5 |
CAS No. | 18200-13-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (102.97 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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BL-1249 18200-13-0 Membrane transporter/Ion channel Potassium Channel BL1249 BL 1249 Inhibitor inhibitor inhibit