2. GPCR/G Protein
  3. Endothelin Receptor
  4. 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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CI-1020 Chemical Structure

CI-1020 Chemical Structure

CAS No. : 162256-50-0

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CI-1020 Related Antibodies

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Description

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].

IC50 & Target[1]

ETA

0.3 nM (IC50)

In Vitro

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 Related Antibodies
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].

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

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.
Molecular Weight

506.50

Formula

C28H26O9
CAS No.
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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Purity & Documentation
References
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CI-1020 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CI-1020162256-50-0PD156707CI1020CI 1020PD 156707PD-156707Endothelin Receptororally activeselectivehypoxic pulmonary hypertensionInhibitorinhibitorinhibit

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