CI-1020

CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration[1][2][3].

Product Specifications

CAS Number

[162256-50-0]

Product Name Alternative

PD156707

UNSPSC

12352005

Target

Endothelin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/ci-1020.html

Solubility

10 mM in DMSO

Smiles

O=C1OC(C2=CC=C(OC)C=C2)(O)C(CC3=CC(OC)=C(OC)C(OC)=C3)=C1C4=CC=C(OCO5)C5=C4

Molecular Formula

C28H26O9

Molecular Weight

506.50

References & Citations

[1]Maguire JJ, et al. ETA receptor antagonists inhibit intimal smooth muscle cell proliferation in human vessels. Clin Sci (Lond) . 2002 Aug;103 Suppl 48:184S-188S.|[2]Doherty AM, et al. Discovery and development of an endothelin A receptor-selective antagonist PD 156707. Pharm Biotechnol. 1998;11:81-112. |[3]Jones RD, et al. The effect of the endothelin ET (A) receptor antagonist CI-1020 on hypoxic pulmonary vasoconstriction. Eur J Pharmacol. 1999 Jun 25;374 (3) :367-75.|[4]Sheedy W, et al. The effect of the ETA receptor antagonist (CI-1020) in rats with established hypoxic pulmonary hypertension. Pulm Pharmacol Ther. 1998 Apr-Jun;11 (2-3) :173-6.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

ETA

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