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1065110-43-1

1065110-43-1 structure
1065110-43-1 structure
  • Name: PF 04479745
  • Chemical Name: PF-4479745
  • CAS Number: 1065110-43-1
  • Molecular Formula: C17H22N4
  • Molecular Weight: 282.383
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2021-01-07 09:10:28
  • Modify Date: 2024-01-12 07:27:09
  • PF-4479745 is a potent and selective 5-HT2C receptor agonist (EC50: 10 nM, ki: 15 nM). PF-4479745 can be used in the research of cardiovascular disease like hypertension[1].

Name PF-4479745
Synonyms MFCD28137682
PF-04479745
5H-Pyrimido[4,5-d]azepin-4-amine, 6,7,8,9-tetrahydro-N,9-dimethyl-2-(phenylmethyl)-, (9S)-
(9S)-2-Benzyl-N,9-dimethyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepin-4-amine
(9S)-6,7,8,9-Tetrahydro-N,9-dimethyl-2-(phenylmethyl)-5H-pyrimido[4,5-d]azepin-4-amine
PF-4479745
Description PF-4479745 is a potent and selective 5-HT2C receptor agonist (EC50: 10 nM, ki: 15 nM). PF-4479745 can be used in the research of cardiovascular disease like hypertension[1].
Related Catalog
Target

5-HT2C Receptor:10 nM (EC50)

5-HT2C Receptor:15 nM (Ki)

5-HT2A Receptor:360 nM (IC50)

5-HT2B Receptor:67 nM (IC50)

5-HT1A Receptor:500 nM (IC50)

5-HT6 Receptor:280 nM (IC50)

In Vitro PF-4479745 (copmpound 17) exhibits metabolic stability in both human liver microsomes (HLM) and human hepatocytes[1].
In Vivo PF-4479745 (compound 17, intravenous injection) shows high clearance rate (104 mL/min/kg)[1]. PF-4479745 demonstrates a robust dose-dependent effect in canine PUP (peak urethral pressure) model of SUI (stress urinary incontinence)[1].
References

[1]. R Ian Storer, et al. Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors. J Med Chem. 2014 Jun 26;57(12):5258-69.

Density 1.1±0.1 g/cm3
Boiling Point 473.4±45.0 °C at 760 mmHg
Molecular Formula C17H22N4
Molecular Weight 282.383
Flash Point 240.1±28.7 °C
Exact Mass 282.184448
LogP 2.68
Vapour Pressure 0.0±1.2 mmHg at 25°C
Index of Refraction 1.590
RIDADR NONH for all modes of transport
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