N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide

 化学構造式
893990-34-6
CAS番号.
893990-34-6
化学名:
别名:
英語名:
N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
英語别名:
CS-1198;VU 0240551;CID 7211972;VU0240551-1;SID 56405457;VU0240551-2-D4;N-(4-Methylthiazol-2-yl)-2-(6-phenylpyridazin-3-ylthio)acetaMide;N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide;Acetamide, N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]-;N-(4-Methyl-thiazol-2-yl)-2-(6-phenyl-pyridazin-3-ylsulfanyl)-acetamide
CBNumber:
CB82518969
化学式:
C16H14N4OS2
分子量:
342.44
MOL File:
893990-34-6.mol
MSDS File:
SDS

N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide 物理性質

融点 :
127 - 132°C
比重(密度) :
1.39±0.1 g/cm3(Predicted)
貯蔵温度 :
2-8°C
溶解性:
DMSO:>20mg/mL
外見 :
酸解離定数(Pka):
7.59±0.50(Predicted)
色:
ペールベージュからベージュ

安全性情報

WGK Germany  3

N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide 価格 もっと(7)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01TOC3888
VU 0240551
893990-34-6 10mg ¥69000 2024-03-01 購入
富士フイルム和光純薬株式会社(wako) W01TOC3888
VU 0240551
893990-34-6 50mg ¥288000 2024-03-01 購入
富士フイルム和光純薬株式会社(wako) W01TRCM330240
N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]-acetamide
893990-34-6 100mg ¥281100 2023-06-01 購入
Sigma-Aldrich Japan V3890 ≥98% (HPLC)
VU0240551 ≥98% (HPLC)
893990-34-6 5mg ¥46800 2024-03-01 購入
富士フイルム和光純薬株式会社(wako) W01TRCM330240
N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]-acetamide
893990-34-6 10mg ¥48600 2024-03-01 購入

N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide 化学特性,用途語,生産方法

説明

VU0240551 is a K+/Cl- cotransporter 2 (KCC2) inhibitor (IC50 = 568 nM). It selectively inhibits KCC2 over Na+/K+/Cl- cotransporter 1 (NKCC1; IC50 = >50 μM) but does inhibit the activity of adenosine A1 and A3 receptors, as well as inhibits activity of L-type calcium channels at the benzothiazepine site and human ether-a-go-go-related gene (hERG) potassium channels by greater than 50% in a panel of 68 receptors, ion channels, and transporters at 10 μM. VU0240551 decreases potassium ion uptake by 70% in HEK293 cells expressing KCC2 when used at a concentration of 1 μM.

Biochem/physiol Actions

VU0240551 is a potent, selective KCC2 inhibitor. KCC2 is a potassium-chloride exchanger expressed specifically in neurons. KCC2 functions to lower intracellular chloride concentrations below the electrochemical potential of the cells, thereby increasing the hyperexcitability of the neurons. KCC2 activity enhances GABA and other inhibitory neurotransmission and is implicated in pain processing. VU0240551 was discovered in a high-throughput screen, followed by directed medicinal chemistry. VU0240551 is selective for KCC2 over NKCC1. VU0240551 binds competitively to the K+ site and binds noncompetitively to the Cl- site. VU0240551 is the only small molecule with specificity for a KCC family member.

N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide 上流と下流の製品情報

原材料

準備製品


N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide 生産企業

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