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

N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide C화학적 특성, 용도, 생산

개요

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.

용도

This molecule acts as an inhibitor of the K-Cl cotransporter KCC2, which is primarily responsible for maintaining intracellular Cl- concentrations including regulating an excess or lack of ions follow ing periods of under or overstimulation, as well as general dendritic development.

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 준비 용품 및 원자재

원자재

준비 용품

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

공급자	전화	이메일	국가	제품 수	이점
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
Amadis Chemical Company Limited	571-89925085	sales@amadischem.com	China	131981	58
J & K SCIENTIFIC LTD.	010-82848833 400-666-7788	jkinfo@jkchemical.com	China	96815	76
3B Pharmachem (Wuhan) International Co.,Ltd.	821-50328103-801 18930552037	3bsc@sina.com	China	15848	69
Haoyuan Chemexpress Co., Ltd.	021-58950125	info@chemexpress.com	China	7553	61
MedChemexpress LLC	021-58955995	sales@medchemexpress.cn	United States	4863	58
LETOPHARM LIMITED	+86-21-5821 5861	sales@letopharm.com	China	2384	58
Sigma-Aldrich	021-61415566 800-8193336	orderCN@merckgroup.com	China	51471	80
SPIRO PHARMA		eric_feng1954@126.com	China	9254	55
EMMX Biotechnology LLC	888-539-0666	info@emmx.com	United States	8449	60

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