推薦產品
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
InChI
1S/C22H20N2O3/c1-15-7-5-8-16(13-15)21(25)23-17-9-6-10-18(14-17)24-22(26)19-11-3-4-12-20(19)27-2/h3-14H,1-2H3,(H,23,25)(H,24,26)
InChI 密鑰
UTAJHKSGYJSZBR-UHFFFAOYSA-N
生化／生理作用
Orignially characterized as an mGluR5 negative allosteric modulator (IC50 = 1.35 μM, Emax = 3.82% of Glu Emax; rat mGluR5 HEK293A cells), ML365 is now better known as selective two-pore potassium (K2P) channel TASK1 (K2P3.1; KCNK3) inhibitor with 100- and 62-fold selectivity over TASK3 (K2p9.1; KCNK9), respectively, by thellium flux (rat TASK1/TASK3 CHO cell IC50 = 4/390 nM) and QPatch assay (rat TASK1/TASK3 CHO cell IC50 = 16/990 nM). ML365 is employed in the range from 40 nM to 20 μM. Selective TASK1 blockage is achieved at the lower end of the concentration range, while TASK3 activity can also be inhibited at the high end of the range.
儲存類別代碼
13 - Non Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
分析證明 (COA)
輸入產品批次/批號來搜索 分析證明 (COA)。在產品’s標籤上找到批次和批號，寫有 ‘Lot’或‘Batch’.。
Peadar B O'Donohoe et al.
Physiological reports, 6(19), e13876-e13876 (2018-10-05)
Sensing of hypoxia and acidosis in arterial chemoreceptors is thought to be mediated through the inhibition of TASK and possibly other (e.g., BKCa ) potassium channels which leads to membrane depolarization, voltage-gated Ca-entry, and neurosecretion. Here, we investigate the effects
Takuma Sonoda et al.
Neuron, 99(4), 754-767 (2018-07-19)
Melanopsin is expressed in distinct types of intrinsically photosensitive retinal ganglion cells (ipRGCs), which drive behaviors from circadian photoentrainment to contrast detection. A major unanswered question is how the same photopigment, melanopsin, influences such vastly different functions. Here we show
M A Skarsfeldt et al.
Acta physiologica (Oxford, England), 223(3), e13049-e13049 (2018-02-08)
The zebrafish has emerged as a novel model for investigating cardiac physiology and pathology. The aim of this study was to investigate the atrium-specific ion channels responsible for shaping the atrial cardiac action potential in zebrafish. Using quantitative polymerase chain
Ya Zhou et al.
Bioorganic & medicinal chemistry letters, 19(23), 6502-6506 (2009-10-31)
This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype identified by a functional HTS approach. This work demonstrates fundamentally new mGluR5 NAM chemotypes
Nicholas C Vierra et al.
Science signaling, 10(497) (2017-09-21)
Ca2+ handling by the endoplasmic reticulum (ER) serves critical roles in controlling pancreatic β cell function and becomes perturbed during the pathogenesis of diabetes. ER Ca2+ homeostasis is determined by ion movements across the ER membrane, including K+ flux through
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