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Merck
CN

SML3838

TP003

≥98% (HPLC)

Synonym(s):

2′,4-Difluoro-5′-[8-fluoro-7-(1-hydroxy-1-methylethyl)imidazo[1,2-a]pyridin-3-yl]-[1,1′-biphenyl]-2-carbonitrile, 4,2’-Difluoro-5’-[8-fluoro-7-(1-hydroxy-1-methylethyl)imidazo[1,2-a]pyridine-3-yl]biphenyl-2-carbonitrile, TP-003

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About This Item

Empirical Formula (Hill Notation):
C23H16F3N3O
CAS Number:
Molecular Weight:
407.39
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Quality Level

Biochem/physiol Actions

Potent and subtype selective agonist at α3GABAA receptors
TP003 is a potent and subtype selective agonist at α3 GABAA receptors that exhibits an anxiolytic-like effect in both rodent and non-human primate behavioral models of anxiety. Also it appears that TP003 have anxiolytic properties but lacks ataxic, hyperphagic, and pronounced sedative effects characteristic of classical benzodiazepines in monkeys. TP003 is consider as α3-over-α1 selective positive allosteric modulator (PAM) at GABBAAR.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Contribution of GABA(A) receptors containing ?3 subunits to the therapeutic-related and side effects of benzodiazepine-type drugs in monkeys
Psychopharmacology, 215(2), 311-319 (2011)
Evidence for a significant role of alpha 3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepines.
The Journal of Neuroscience, 25(46), 10682-10688 (2005)
Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors
Biochemical Pharmacology, 158, 339-358 (2018)

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