N-ethyl-1-(1H-indazol-5-ylsulfonyl)-N-[[2-(trifluoromethyl)phenyl]methyl]piperidine-4-carboxamide

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CAS:1627138-52-6
Purity:99.69% Package:2mg;42USD|5mg;68USD|10mg;122USD Remarks:REAGENT;FOR LABORATORY USE ONLY
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CAS:1627138-52-6
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CAS:1627138-52-6
Purity:98% Package:100mg Remarks:S89286
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Products Intro: Product Name:ML380
CAS:1627138-52-6
Purity:98 Package:1G,5G,10G,50G,100G,500G

N-ethyl-1-(1H-indazol-5-ylsulfonyl)-N-[[2-(trifluoromethyl)phenyl]methyl]piperidine-4-carboxamide manufacturers

  • ML380
  • ML380 pictures
  • $42.00
  • 2026-04-20
  • CAS:1627138-52-6
  • Purity: 99.84%
  • Supply Ability: 10g
N-ethyl-1-(1H-indazol-5-ylsulfonyl)-N-[[2-(trifluoromethyl)phenyl]methyl]piperidine-4-carboxamide Basic information
Product Name:N-ethyl-1-(1H-indazol-5-ylsulfonyl)-N-[[2-(trifluoromethyl)phenyl]methyl]piperidine-4-carboxamide
Synonyms:N-ethyl-1-(1H-indazol-5-ylsulfonyl)-N-[[2-(trifluoromethyl)phenyl]methyl]piperidine-4-carboxamide;ML380;positive,ML380,Muscarinic acetylcholine receptor,allosteric,inhibit,ACh,modulator,Inhibitor,mAChR,PAM;4-Piperidinecarboxamide, N-ethyl-1-(1H-indazol-5-ylsulfonyl)-N-[[2-(trifluoromethyl)phenyl]methyl]-;1-((1H-Indazol-5-yl)sulfonyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide;ML380, 10 mM in DMSO;1-((1H-Indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide
CAS:1627138-52-6
MF:C23H25F3N4O3S
MW:494.53
EINECS:
Product Categories:
Mol File:1627138-52-6.mol
N-ethyl-1-(1H-indazol-5-ylsulfonyl)-N-[[2-(trifluoromethyl)phenyl]methyl]piperidine-4-carboxamide Structure
N-ethyl-1-(1H-indazol-5-ylsulfonyl)-N-[[2-(trifluoromethyl)phenyl]methyl]piperidine-4-carboxamide Chemical Properties
Boiling point 661.2±65.0 °C(Predicted)
density 1.388±0.06 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMSO: 100 mg/mL (202.21 mM)
form Solid
pka12.84±0.40(Predicted)
color White to off-white
Safety Information
MSDS Information
N-ethyl-1-(1H-indazol-5-ylsulfonyl)-N-[[2-(trifluoromethyl)phenyl]methyl]piperidine-4-carboxamide Usage And Synthesis
UsesML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR[1][2][3].
Biological ActivityML380 is a potent, isotype-selective and blood-brain barrier-permeable positive allosteric modulator (PAM) of M5 mAChR with EC50 values of 190 and 610 nM for human and rat M5, respectively.
in vivo

ML380 (1 mg/kg; iv) displays high clearance (66 mL/min/kg), a moderate volume of distribution (1.6 L/kg), and a short half-life (t 1/2 , 22 min) in rats.

target

IC50: 190 nM (hM5), 610 nM (rM5)

References[1] Gentry PR, et, al. Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380). J Med Chem. 2014 Sep 25;57(18 DOI:10.1021/jm500995y
[2] Berizzi AE, et, al. Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators. Mol Pharmacol. 2016 Oct;90(4):427-36. DOI:10.1124/mol.116.104182
[3] Berizzi AE, et, al. Structure-Activity Relationships of Pan-Gα q/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators. ACS Chem Neurosci. 2018 Jul 18;9(7):1818-1828. DOI:10.1021/acschemneuro.8b00136
N-ethyl-1-(1H-indazol-5-ylsulfonyl)-N-[[2-(trifluoromethyl)phenyl]methyl]piperidine-4-carboxamide Preparation Products And Raw materials
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