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.
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- CAS No.: 162256-50-0
- Formule: C28H26O9
- Masse moléculaire:506.50
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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ETA 0.3 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO-K1 | IC50 |
120 nM
Compound: 1, (PD-156707)
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Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors / CHO-K1 cells
Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors / CHO-K1 cells
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[PMID: 9089328] |
| CHO-K1 | IC50 |
480 nM
Compound: 1, (PD-156707)
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Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
Binding affinity for human endothelin B receptor expressed in CHO-K1 cells.
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10.1016/S0960-894X(97)00002-4 |
| CHO-K1 | IC50 |
780 nM
Compound: 1, (PD-156707)
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Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
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[PMID: 9089328] |
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.
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Animal Model:normal rats [2]
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Dosage:30 mg/kg
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Administration:oral administration (p.o.)
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Result:Inhibited the ET-A and has no significant effect on basal blood pressure in normotensive rats.
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Animal Model:basal blood pressure in normotensive rats[4]
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Dosage:40 mg/kg/day
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Administration:oral administration (p.o.)
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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.
Chemical Information
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CAS No. 162256-50-0
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Masse moléculaire 506.50
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Formule C28H26O9
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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
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Synonyms
PD156707
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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