Basic information Safety Supplier Related

CI 1020

Basic information Safety Supplier Related

CI 1020 Basic information

Product Name:
CI 1020
Synonyms:
  • 3-(1,3-Benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(3,4,5-trimethoxyphenyl)methyl]-2(5H)-furanone
  • CI 1020
  • PD 156707
  • 2(5H)-Furanone, 3-(1,3-benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(3,4,5-trimethoxyphenyl)methyl]-
CAS:
162256-50-0
MF:
C28H26O9
MW:
506.5
Product Categories:
  • Aromatics
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
Mol File:
162256-50-0.mol
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CI 1020 Chemical Properties

storage temp. 
Store at +4°C
solubility 
Soluble to 50 mM in DMSO
form 
Powder
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CI 1020 Usage And Synthesis

Uses

A novel endothelin-A receptor antagonist, in hypoxic pulmonary hypertension.

Biological Activity

Highly selective, orally active, non-peptide endothelin-A receptor (ET A ) antagonist (IC 50 values are 0.3 and 480 nM for ET A and ET B receptors respectively). Antihypertensive; blocks ET-1-induced pressor responses following oral administration.

in vivo

CI-1020 (30 mg/kg, p.o.) represents full inhibition of the ET-A and has no significant effect on basal blood pressure in normotensive rats[2].
CI-1020 (40 mg/kg, p.o.) attenuates established pulmonary hypertension in rats previously exposed to chronic hypoxia[4].

Animal Model:normal rats [2]
Dosage:30 mg/kg
Administration:oral administration (p.o.)
Result:Inhibited the ET-A and has no significant effect on basal blood pressure in normotensive rats.
Animal Model:basal blood pressure in normotensive rats[4]
Dosage:40 mg/kg/day
Administration:oral administration (p.o.)
Result:Reduced the increase in RV/LV+S and the percentage DEL induced by chronic hypoxia.
Lowered the increase in pulmonary resistance in isolated perfused lungs significantly.

IC 50

ETA: 0.3 nM (IC50)

CI 1020Supplier

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