ChemicalBook > CAS DataBase List > 1H-Indole-4-carboxamide, 1-[6-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-4-pyrimidinyl]-2,3-dihydro-N-(2-hydroxyethyl)-

1H-Indole-4-carboxamide, 1-[6-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-4-pyrimidinyl]-2,3-dihydro-N-(2-hydroxyethyl)-

Product Name
1H-Indole-4-carboxamide, 1-[6-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-4-pyrimidinyl]-2,3-dihydro-N-(2-hydroxyethyl)-
CAS No.
2624131-45-7
Chemical Name
1H-Indole-4-carboxamide, 1-[6-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-4-pyrimidinyl]-2,3-dihydro-N-(2-hydroxyethyl)-
Synonyms
PW0787;PW0787, 10 mM in DMSO;GPR52,PW-0787,oral,PW0787,Inhibitor,PW 0787,brain-penetrant,selective,inhibit,psychostimulant,behavior;1H-Indole-4-carboxamide, 1-[6-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-4-pyrimidinyl]-2,3-dihydro-N-(2-hydroxyethyl)-
CBNumber
CB78896424
Molecular Formula
C23H20F4N4O2
Formula Weight
460.42
MOL File
2624131-45-7.mol
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1H-Indole-4-carboxamide, 1-[6-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-4-pyrimidinyl]-2,3-dihydro-N-(2-hydroxyethyl)- Property

Boiling point:
605.1±55.0 °C(Predicted)
Density 
1.388±0.06 g/cm3(Predicted)
storage temp. 
4°C, protect from light
solubility 
DMSO : 50 mg/mL (108.60 mM; Need ultrasonic)
form 
Solid
pka
14.18±0.20(Predicted)
color 
Off-white to yellow
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Hazard and Precautionary Statements (GHS)

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1H-Indole-4-carboxamide, 1-[6-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-4-pyrimidinyl]-2,3-dihydro-N-(2-hydroxyethyl)- Chemical Properties,Usage,Production

Uses

PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). PW0787 suppresses psychostimulant behavior[1].

Biological Activity

PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). PW0787 suppresses psychostimulant behavior[1]. PW0787 (0.3, 1, 3, or 10 mg/kg; IP) displays antipsychotic-like activity by significantly inhibiting amphetamine-induced hyperlocomotor behavior in mice[1].PW0787 is evaluated in rats after a single dose of 20 mg/kg by oral (PO) or 10 mg/kg by intravenous (IV) administration. PW0787 has excellent plasma exposure after PO (AUC0-inf = 13,749 ng?h/mL) and IV dosing (AUC0-inf=9030 ng?h/mL), as well as high maximum serum concentration following PO (Cmax=3407 ng/mL) and IV administration (Cmax=6726 ng/mL). Additionally, PW0787 displays good volume of plasma distribution (Vss=1.5 L/kg) and acceptable plasma clearance (CL=1.1 L/h/kg) after 10 mg/kg IV. Excellent oral bioavailability (F) with the value of 76% is observed[1].

in vivo

PW0787 (0.3, 1, 3, or 10 mg/kg; IP) displays antipsychotic-like activity by significantly inhibiting amphetamine-induced hyperlocomotor behavior in mice[1].
PW0787 is evaluated in rats after a single dose of 20 mg/kg by oral (PO) or 10 mg/kg by intravenous (IV) administration. PW0787 has excellent plasma exposure after PO (AUC0-inf = 13,749 ng?h/mL) and IV dosing (AUC0-inf=9030 ng?h/mL), as well as high maximum serum concentration following PO (Cmax=3407 ng/mL) and IV administration (Cmax=6726 ng/mL). Additionally, PW0787 displays good volume of plasma distribution (Vss=1.5 L/kg) and acceptable plasma clearance (CL=1.1 L/h/kg) after 10 mg/kg IV. Excellent oral bioavailability (F) with the value of 76% is observed[1].

Animal Model:Na?ve male C57/BL6 mice weighing between 24 and 31 g
Dosage:0.3, 1, 3, or 10 mg/kg (dissolved in 0.9% saline containing 20% HP-β-CD with a final pH of the solution adjusted to 7.4)
Administration:IP
Result:Suppressed amphetamine (AMPH)-induced horizontal activity at both 3 mg/kg and 10 mg/kg doses.

References

[1]. Wang P, et al. Discovery of Potent and Brain-Penetrant GPR52 Agonist that Suppresses Psychostimulant Behavior. J Med Chem. 2020;63(22):13951-13972.

1H-Indole-4-carboxamide, 1-[6-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-4-pyrimidinyl]-2,3-dihydro-N-(2-hydroxyethyl)- Preparation Products And Raw materials

Raw materials

Preparation Products

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1H-Indole-4-carboxamide, 1-[6-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-4-pyrimidinyl]-2,3-dihydro-N-(2-hydroxyethyl)- Suppliers

China 18 United States 2 Global 20
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2624131-45-7, 1H-Indole-4-carboxamide, 1-[6-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-4-pyrimidinyl]-2,3-dihydro-N-(2-hydroxyethyl)-Related Search:


  • PW0787
  • GPR52,PW-0787,oral,PW0787,Inhibitor,PW 0787,brain-penetrant,selective,inhibit,psychostimulant,behavior
  • PW0787, 10 mM in DMSO
  • 1H-Indole-4-carboxamide, 1-[6-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-4-pyrimidinyl]-2,3-dihydro-N-(2-hydroxyethyl)-
  • 2624131-45-7