CI-1020  (Synonyms: PD156707)

CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ET_A) 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].

CI-1020 (1 μM, 28 days) blocks intimal hyperplasia in human saphenous veins completely in organ culture ^[1].
CI-1020 (1 μM, 14 days) is not toxic to the tissue^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

506.50

C₂₈H₂₆O₉

162256-50-0

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

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [2]. Doherty AM, et al. Discovery and development of an endothelin A receptor-selective antagonist PD 156707. Pharm Biotechnol. 1998;11:81-112.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]