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

N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide Struktur
893990-34-6
CAS-Nr.
893990-34-6
Englisch Name:
N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
Synonyma:
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
Summenformel:
C16H14N4OS2
Molgewicht:
342.44
MOL-Datei:
893990-34-6.mol

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

Schmelzpunkt:
127 - 132°C
Dichte
1.39±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
L?slichkeit
DMSO: >20mg/mL
Aggregatzustand
powder
pka
7.59±0.50(Predicted)
Farbe
Pale Beige to Beige

Sicherheit

WGK Germany  3

N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

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 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 58)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795
ivan@atkchemical.com China 32957 60
TargetMol Chemicals Inc.
support@targetmol.com United States 38631 58
Amadis Chemical Company Limited 		571-89925085
sales@amadischem.com China 131957 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 15839 69
Haoyuan Chemexpress Co., Ltd. 021-58950125
info@chemexpress.com China 7552 61
MedChemexpress LLC 021-58955995
sales@medchemexpress.cn United States 4861 58
LETOPHARM LIMITED +86-21-5821 5861
sales@letopharm.com China 2384 58
Sigma-Aldrich 021-61415566 800-8193336
 orderCN@merckgroup.com China 51456 80
SPIRO PHARMA
eric_feng1954@126.com China 9248 55
  • N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
  • VU 0240551
  • N-(4-Methylthiazol-2-yl)-2-(6-phenylpyridazin-3-ylthio)acetaMide
  • CID 7211972
  • SID 56405457
  • VU0240551-1
  • VU0240551-2-D4
  • N-(4-Methyl-thiazol-2-yl)-2-(6-phenyl-pyridazin-3-ylsulfanyl)-acetamide
  • CS-1198
  • Acetamide, N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]-
  • 893990-34-6
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