Endothelin Receptors

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  1. Aprocitentan

    Catalog No. A21999
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    dual ETA/ETB antagonist
    Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Learn More
  2. Macitentan (n-butyl analogue)

    Catalog No. A21845
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    endothelin ETA and ETB receptor antagonist
    Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). Learn More
  3. Darusentan

    Catalog No. A21280
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    endothelin A (ETA) receptor antagonist
    Darusentan is a selective endothelin A (ETA) receptor antagonist. Learn More
  4. Tezosentan

    Catalog No. A21118
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    endothelin (ET) receptor antagonist
    Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively. Learn More
  5. Sparsentan

    Catalog No. A20879
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    angiotensin II and endothelin A receptor antagonist
    Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively. Learn More
  6. Endothelin Mordulator 1

    Catalog No. A13040
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    endothelin receptor modulator
    Endothelin Mordulator 1 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders. Learn More
  7. PD-159020

    Catalog No. A13499
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    ETA/ETB antagonist
    PD-159020 is a non-selective ETA/ETB antagonist, with IC50s of 30 and 50 nM for hETA and hETB, respectively. Learn More
  8. RO462005

    Catalog No. A13216
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    endothelin receptor agonist
    RO462005 is an endothelin receptor selective agonist. Learn More
  9. Macitentan

    Catalog No. A11492
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    Endothelin receptor antagonist
    Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). Learn More
  10. IRL-2500

    Catalog No. A13638
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    ETBR antagonist
    IRL-2500 is a potent, selective ETBR antagonist. It shows some selectivity for ETB receptors (IC50 values are 1.3 and 94 nM for ETB and ETA receptors respectively). Learn More
  11. Atrasentan HCl

    Catalog No. A15007
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    Endothelin antagonist receptor
    Atrasentan hydrochloride is an endothelin antagonist receptor (IC50=0.0551 nM, ETA) being developed for the treatment of prostate cancer. Learn More
  12. Bosentan

    Catalog No. A11091
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    ETAR/ETBR inhibitor
    Bosentan is a competitive antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors. Learn More
  13. Ambrisentan (BSF 208075)

    Catalog No. A11291
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    EndothelinA receptor antagonist
    Ambrisentan functions as an endothelin receptor antagonist, and is selective for the type A endothelin receptor (ETA). Learn More
  14. Avosentan (SPP301)

    Catalog No. A11301
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    Endothelin antagonist
    Avosentan (SPP301) is a potent and highly selective ETA receptor blocker. Learn More
  15. Sitaxsentan sodium (TBC-11251)

    Catalog No. A11564
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    ETA receptor antagonist
    Sitaxentan sodium (TBC-11251) is a selective endothelin receptor-A antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively. Learn More
  16. BQ-788

    Catalog No. A14369
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    ETBR antagonist
    BQ-788 sodium salt is a selective ETBR (Endothelin receptor B ) antagonist. Learn More
  17. Atrasentan

    Catalog No. A13779
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    ETA antagonist
    Atrasentan is an experimental drug that is being studied for the treatment of various types of cancer, including non-small cell lung cancer. It is an endothelin receptor antagonist selective for subtype A (ETA). Learn More
  18. Bosentan Hydrate

    Catalog No. A14944
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    ET-A and ET-B antagonist
    Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. Learn More
  19. BQ-123

    Catalog No. A15912
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    ETA receptor antagonist
    BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2. Learn More
  20. Endothelin-2, human

    Catalog No. A14894
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    Endothelin-2, human, endogenous peptide found predominately in the kidney and intestine. Displays similar selectivity for ETA and ETB endothelin receptors. Learn More
  21. Zibotentan (ZD4054)

    Catalog No. A11006
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    ETA-receptor Antagonist
    Zibotentan (ZD4054)is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM). Learn More

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