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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
55 Results for "
ET receptor antagonist
" in MedChemExpress (MCE) Product Catalog:
Products (55)
55 Results for "ET receptor antagonist" in MCE Product Catalog:
32
32 Publications Verification
Cat. No.: HY-A0013
CAS No.: 147536-97-8
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Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
32
32 Publications Verification
Cat. No.: HY-A0013A
CAS No.: 157212-55-0
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Bosentan hydrate is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
15
15 Cited Publications
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BQ-788 is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM .
15
15 Cited Publications
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BQ-788 sodium salt is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells .
2
2 Cited Publications
Synonyms: BSF 208075; LU 208075
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Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
2
2 Cited Publications
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A-192621, a chemical probe, is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level .
1
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Relugolix (TAK-385)?is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .
1
1 Cited Publications
Cat. No.: HY-17352
CAS No.: 180384-56-9
Synonyms: Ro 61-1790; VML 588; AXV-034343
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Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction .
1
1 Cited Publications
Cat. No.: HY-17352A
CAS No.: 503271-02-1
Synonyms: Ro 61-1790 disodium; VML 588 disodium; AXV-034343 disodium
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Clazosentan disodium (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan disodium inhibits ET-1-mediated vasoconstriction. Clazosentan disodium prevents cerebral vasospasm, vasospasm-related cerebral infarction .
Cat. No.: HY-17351
CAS No.: 180384-57-0
Synonyms: RO 610612
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Cardiovascular Disease Neurological Disease Endocrinology Cancer
Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.
Synonyms: Ro 67-0565; SPP-301
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Avosentan (Ro 67-0565; SPP-301) is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks ETB receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure .
Synonyms: Lu-135252
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Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors . Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM .
Cat. No.: HY-19529
CAS No.: 150725-87-4
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Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.
Cat. No.: HY-119667
CAS No.: 167256-08-8
Synonyms: SB 217242
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Enrasentan (SB 217242) is an endothelin (ET) receptor antagonist. Enrasentan has antihypertensive effects .
Synonyms: FI3542
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Ebrotidine (FI3542) is a competitive histamine H2 receptor (histamine H2 receptor) antagonist with gastric acid secretion inhibitory and gastric mucosal protective effects. Ebrotidine alleviates gastric mucosal injury and epithelial cell apoptosis induced by Indomethacin (HY-14397) and Helicobacter pylori LPS (HY-D1056), and accelerates chronic gastric ulcer healing by promoting rapid recovery of IL-4 and inhibiting TNF-α, endothelin-1 (ET-1) and NOS-2. Ebrotidine can be used in studies on gastric ulcer healing, NSAID-induced gastric mucosal injury, Helicobacter pylori-associated gastritis, and H2 receptor-mediated gastric mucosal protection mechanisms .
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PD-156707 is an orally active, nonpeptide and selective Endothelin-A receptor antagonist. PD-156707 binds to human ET-A and ET-B receptors with Ki values of 0.17 nM and 133.8 nM, respectively. PD-156707 shows reversal of established chronic hypoxic pulmonary hypertension in rats. PD-156707 can be used for the study of diseases associated with abnormal ET-A receptor activation, particularly pulmonary hypertension, stroke, and heart failure .
Cat. No.: HY-16474R
CAS No.: 737789-87-6
Synonyms: TAK-385 (Standard)
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Relugolix (Standard) is the analytical standard of Relugolix. This product is intended for research and analytical applications. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .
Cat. No.: HY-155737
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ET receptor antagonist 1 (compound 16h) is an orally active ET receptor antagonist (IC50=0.18 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 1 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
Cat. No.: HY-155739
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ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist (IC50=0.26 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 3 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
Cat. No.: HY-124234
CAS No.: 169679-53-2
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TA-0201 is a novel orally active, competitive, non-peptide endothelin receptor antagonist. TA-0201 antagonizes the specific binding of [ 125I]ET-1 to cloned human receptors of ETA and ETB with Ki values of 15 pM and 41 nM, respectively. TA-0201 inhibits the pressor response to the exogenous big ET-1 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
