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• 產(chǎn)品描述： ML402, a thiophene-carboxamide, is a selective K2P2.1(TREK-1) and K2P10.1(TREK-2) activator. ML402 is inactive against K2P4.1(TRAAK)

• 靶點(diǎn)： TREK-1/2;PotassiumChannel

• 體外研究：
  Xenopus oocyte two-electrode voltage-clamp measurements show that ML335 and ML402 activate K2P2.1 and K2P10.1 but not K2P4.1(14.3±2.7 μM, K2P2.1-ML335; 13.7±7.0 μM, K2P2.1-ML402; 5.2±0.5 μM, K2P10.1-ML335; and 5.9±1.6 μM, K2P10.1-ML402). The K2P?modulator pocket has a single difference among TREK subfamily members at the cation-π interaction position, K2P2.1 Lys271, which is also a lysine in K2P10.1 but a glutamine in K2P4.1. Swapping the Lys271 equivalent between K2P2.1 and K2P4.1 results in a clear phenotype reversal for ML335 and M402 activation. K2P2.1 (K271Q) is insensitive to ML335 and ML402, whereas K2P4.1 (Q258K) responds to both with a similar EC50?to K2P2.1 (14.3±2.7 μM, K2P2.1-ML335; 16.2±3.0 μM, K2P4.1(Q258K)-ML335; 13.7±7.0 μM, K2P2.1-ML402; 13.6±1.5 μM, K2P4.1 (Q258K)-ML402) but with a lower magnitude response than K2P2.1

• 參考文獻(xiàn)：
  1. Lolicato M, et al. K2P2.1 (TREK-1)-activator complexes reveal a cryptic selectivity filter binding site. Nature. 2017 Jul 20;547(7663):364-368.

• 溶解性： Soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	3.381 ml	16.904 ml	33.808 ml
  5 mM	0.676 ml	3.381 ml	6.762 ml
  10 mM	0.338 ml	1.69 ml	3.381 ml
  50 mM	0.068 ml	0.338 ml	0.676 ml

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *