CI 1020

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Cat.No. 2942 - CI 1020 | C28H26O9 | CAS No. 162256-50-0
Description: Highly selective, orally active ETA antagonist
Alternative Names: PD 156707
Chemical Name: 3-(1,3-Benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(3,4,5-trimethoxyphenyl)methyl]-2(5H)-furanone
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Highly selective, orally active, non-peptide endothelin-A receptor (ETA) antagonist (IC50 values are 0.3 and 480 nM for ETA and ETB receptors respectively). Antihypertensive; blocks ET-1-induced pressor responses following oral administration.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 506.5
Formula C28H26O9
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 162256-50-0
PubChem ID 9870830
InChI Key PWIPORDFWDZCJG-UHFFFAOYSA-N
Smiles O=C1C(C2=CC=C(OCO4)C4=C2)=C(CC3=CC(OC)=C(OC)C(OC)=C3)C(O)(C5=CC=C(OC)C=C5)O1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 25.32 50

Preparing Stock Solutions

The following data is based on the product molecular weight 506.5. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.97 mL 9.87 mL 19.74 mL
5 mM 0.39 mL 1.97 mL 3.95 mL
10 mM 0.2 mL 0.99 mL 1.97 mL
50 mM 0.04 mL 0.2 mL 0.39 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Doherty et al (1995) Discovery of a novel series of orally active non-peptide endothelin-A (ETA) receptor-selective antagonists. J.Med.Chem. 38 1259 PMID: 7731010

Jones et al (1999) The effect of the endothelin ETA receptor antagonist CI-1020 on hypoxic pulmonary vasoconstriction. Eur.J.Pharmacol. 374 367 PMID: 10422781

Coe et al (2002) The endothelin A receptor antagonists PD 156707 (CI-1020) and PD 180988 (CI-1034) reverse the hypoxic pulmonary vasoconstriction in ther perinatal lamb. J.Pharmacol.Exp.Ther. 302 672 PMID: 12130731


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Citations for CI 1020

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