5-Amino-3,4-dimethyl-thieno[2,3-c]pyridazine-6-carboxylic acid 4-trifluoromethanesulfonyl-benzylamide

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5-Amino-3,4-dimethyl-thieno[2,3-c]pyridazine-6-carboxylic acid 4-trifluoromethanesulfonyl-benzylamide manufacturers

  • VU0467154
  • VU0467154 pictures
  • $98.00
  • 2026-05-11
  • CAS:1451993-15-9
  • Purity: 99.53%
  • Supply Ability: 10g
5-Amino-3,4-dimethyl-thieno[2,3-c]pyridazine-6-carboxylic acid 4-trifluoromethanesulfonyl-benzylamide Basic information
Product Name:5-Amino-3,4-dimethyl-thieno[2,3-c]pyridazine-6-carboxylic acid 4-trifluoromethanesulfonyl-benzylamide
Synonyms:5-Amino-3,4-dimethyl-thieno[2,3-c]pyridazine-6-carboxylic acid 4-trifluoromethanesulfonyl-benzylamide;VU0467154, VU-0467154, VU 0467154;Thieno[2,3-c]pyridazine-6-carboxamide, 5-amino-3,4-dimethyl-N-[[4-[(trifluoromethyl)sulfonyl]phenyl]methyl]-;VUO467154 - M4 Receptor Agonist;VU0467154,Muscarinic acetylcholine receptor,VU 0467154,VU-0467154,mAChR,inhibit,Inhibitor;5-Amino-3,4-dimethyl-N-(4-((trifluoromethyl)sulfonyl)benzyl)thieno[2,3-c]pyridazine-6-carboxamide;VU0467154, 10 mM in DMSO;VU0467154
CAS:1451993-15-9
MF:C17H15F3N4O3S2
MW:444.45
EINECS:
Product Categories:
Mol File:1451993-15-9.mol
5-Amino-3,4-dimethyl-thieno[2,3-c]pyridazine-6-carboxylic acid 4-trifluoromethanesulfonyl-benzylamide Structure
5-Amino-3,4-dimethyl-thieno[2,3-c]pyridazine-6-carboxylic acid 4-trifluoromethanesulfonyl-benzylamide Chemical Properties
density 1.514±0.06 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMSO: Soluble
form A solid
pka11.80±0.46(Predicted)
color Light yellow to yellow
Safety Information
MSDS Information
5-Amino-3,4-dimethyl-thieno[2,3-c]pyridazine-6-carboxylic acid 4-trifluoromethanesulfonyl-benzylamide Usage And Synthesis
DescriptionVU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor that potentiates acetylcholine responses in CHO cells expressing M4 receptors (EC50s = 17.7, 630, and 1,000 nM for rat, human, and cynomolgus monkey receptors, respectively). It is selective for M4 over M1-3 and M5 receptors and a panel of receptors, transporters, and cation channels when used at a concentration of 10 μM. In vivo, VU0467154 (3-56.6 mg/kg, p.o.) reverses amphetamine-induced hyperlocomotion in rats. It reverses MK-801-induced hyperlocomotion, deficits in a pairwise visual discrimination task, and impairments in the acquisition of contextual fear conditioning in wild-type, but not M4 knockout, mice. VU0467154 (3-30 mg/kg) also increases freezing behavior in contextual and tone fear conditioning tests in wild-type mice when administered prior to the conditioning session. Chronic administration of VU0467154 (10 mg/kg once daily) reduces motor incoordination and prevents decreases in locomotion in the YAC128 transgenic mouse model of Huntington''s disease.
UsesVU 0467154, is a positive allosteric modulators of the M4 muscarinic acetylcholine receptor (mAChR), robustly potentiates the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey (cyno) M4 receptor, respectively.
in vivo

VU0467154 (1-56.6 mg/kg, p.o. or i.p.) reverses amphetamine-induced hyperlocomotion in rats. VU0467154 (0.3-30 mg/kg, i.p.) reverses amphetamine- and MK-801-induced hyperlocomotion in wild-type but not M4 KO mice. VU0467154 alone also enhances the acquisition of both contextual and cue-mediated fear conditioning in wild-type mice[1].

IC 50mAChR4
References[1] MICHAEL BUBSER. Selective Activation of M4 Muscarinic Acetylcholine Receptors Reverses MK-801-Induced Behavioral Impairments and Enhances Associative Learning in Rodents[J]. ACS Chemical Neuroscience, 2014, 5 10: 920-942. DOI: 10.1021/cn500128b
[2] TRISTANO PANCANI. Allosteric activation of M4 muscarinic receptors improve behavioral and physiological alterations in early symptomatic YAC128 mice.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2015: 14078-14083. DOI: 10.1073/pnas.1512812112
5-Amino-3,4-dimethyl-thieno[2,3-c]pyridazine-6-carboxylic acid 4-trifluoromethanesulfonyl-benzylamide Preparation Products And Raw materials
Tag:5-Amino-3,4-dimethyl-thieno[2,3-c]pyridazine-6-carboxylic acid 4-trifluoromethanesulfonyl-benzylamide(1451993-15-9) Related Product Information
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