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N-[3-FLUORO-5-(3-PYRINDYL)PHENYL]-2,3-DIHYDRO-5-METHOXY-6-(TRIFLUOROMETHYL)-1H-INDOLE-1-CARBOXAMIDE

Basic information Safety Supplier Related

N-[3-FLUORO-5-(3-PYRINDYL)PHENYL]-2,3-DIHYDRO-5-METHOXY-6-(TRIFLUOROMETHYL)-1H-INDOLE-1-CARBOXAMIDE Basic information

Product Name:
N-[3-FLUORO-5-(3-PYRINDYL)PHENYL]-2,3-DIHYDRO-5-METHOXY-6-(TRIFLUOROMETHYL)-1H-INDOLE-1-CARBOXAMIDE
Synonyms:
  • N-[3-FLUORO-5-(3-PYRINDYL)PHENYL]-2,3-DIHYDRO-5-METHOXY-6-(TRIFLUOROMETHYL)-1H-INDOLE-1-CARBOXAMIDE
  • SB 228357
  • N-[3-Fluoro-5-(3-pyridinyl)phenyl]-2,3-dihydro-5-methoxy-6-(trifluoromethyl)-1H-indole-1-carboxamide
  • N-[3-fluoro-5-(3-pyridinyl)phenyl]-5-methoxy-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide
  • 1H-Indole-1-carboxamide, N-[3-fluoro-5-(3-pyridinyl)phenyl]-2,3-dihydro-5-methoxy-6-(trifluoromethyl)-
  • SB-228357,SB228357
  • SB228357, 10 mM in DMSO
  • N-(3-Fluoro-5-(pyridin-3-yl)phenyl)-5-methoxy-6-(trifluoromethyl)indoline-1-carboxamide
CAS:
181629-93-6
MF:
C22H17F4N3O2
MW:
431.38
Mol File:
181629-93-6.mol
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N-[3-FLUORO-5-(3-PYRINDYL)PHENYL]-2,3-DIHYDRO-5-METHOXY-6-(TRIFLUOROMETHYL)-1H-INDOLE-1-CARBOXAMIDE Chemical Properties

Boiling point:
625.4±55.0 °C(Predicted)
Density 
1.398±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO: ~8 mg/mL, soluble
form 
solid
pka
9.72±0.70(Predicted)
color 
white
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Safety Information

Safety Statements 
22-24/25
WGK Germany 
3

MSDS

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N-[3-FLUORO-5-(3-PYRINDYL)PHENYL]-2,3-DIHYDRO-5-METHOXY-6-(TRIFLUOROMETHYL)-1H-INDOLE-1-CARBOXAMIDE Usage And Synthesis

Uses

SB 228357 is a SR-2C/SR-2B receptor antagonist. It is used in the treatment of irritable bowel syndrome (IBS).

Definition

ChEBI: SB 228357 is an indolyl carboxylic acid.

Biological Activity

5-HT 2C/2B receptor antagonist (pK i values are 7.0, 8.1 and 9.1 at 5-HT 2A , 2B and 2C receptors respectively). Displays inverse agonism in a 5-HT-stimulated PI hydrolysis model of 5-HT 2C receptor function. Orally active in vivo .

in vivo

SB228357 (0-10 mg/kg; oral administration; for 90 minutes; male Sprague Dawley rats) treatment significantly reverses Haloperidol-induced catalepsy[2].

Animal Model:Male Sprague Dawley rats (200-250?g) injected with Haloperidol[2]
Dosage:0 mg/kg, 0.32 mg/kg, 1 mg/kg, 3.2 mg/kg, 10 mg/kg
Administration: Oral administration; for 90 minutes
Result:Significantly reversed Haloperidol-induced catalepsy.

IC 50

5-HT2A Receptor: 6.9 (pKi); 5-HT2C Receptor: 9 (pKi); 5-HT2B Receptor: 8 (pKi)

storage

Store at RT

N-[3-FLUORO-5-(3-PYRINDYL)PHENYL]-2,3-DIHYDRO-5-METHOXY-6-(TRIFLUOROMETHYL)-1H-INDOLE-1-CARBOXAMIDESupplier

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