品牌	貨號	產(chǎn)品規(guī)格	價格(RMB)	庫存（上海）	北京	武漢	南京
源葉(MedMol)	S84819-1mg	99%	￥170.00元	10	-	-	-
源葉(MedMol)	S84819-5mg	99%	￥430.00元	10	-	-	-
源葉(MedMol)	S84819-10mg	99%	￥790.00元	9	-	-	-
源葉(MedMol)	S84819-50mg	99%	￥3700.00元	7	-	-	-
源葉(MedMol)	S84819-100mg	99%	￥5500.00元	預計交期：2-3天	-	-	-

產(chǎn)品介紹

ML402, a thiophene-carboxamide, is a selective K2P2.1(TREK-1) and K2P10.1(TREK-2) activator. ML402 is inactive against K2P4.1(TRAAK)

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：

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：

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威性，僅供客戶參考交流研究之用。

參考文獻

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