추천 제품
분석
≥98% (HPLC)
양식
powder
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
2-8°C
SMILES string
N(c2cc(ccc2)NC(=O)c3cc(ccc3)C)C(=O)c1c(cccc1)OC
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 key
UTAJHKSGYJSZBR-UHFFFAOYSA-N
생화학적/생리학적 작용
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.
Selective two-pore potassium (K2P) channel TASK1 (K2P3.1; KCNK3) inhibitor with 62- to 100-fold selectivity over TASK3 (K2p9.1; KCNK9).
Storage Class Code
13 - Non Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
가장 최신 버전 중 하나를 선택하세요:
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
자사의 과학자팀은 생명 과학, 재료 과학, 화학 합성, 크로마토그래피, 분석 및 기타 많은 영역을 포함한 모든 과학 분야에 경험이 있습니다..
고객지원팀으로 연락바랍니다.