1. GPCR/G Protein
    Apoptosis
  2. Endothelin Receptor
    Apoptosis
  3. A-192621

A-192621 

Cat. No.: HY-120295
Handling Instructions

A-192621 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.

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A-192621 Chemical Structure

A-192621 Chemical Structure

CAS No. : 195529-54-5

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Description

A-192621 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][2][3].

IC50 & Target[1]

ETB

4.5 nM (IC50)

ETB

8.8 nM (Ki)

ETA

4280 nM (IC50)

ETA

5600 nM (Ki)

In Vitro

A-192621 (1-100 μM; 48 hours; PASMCs) treatment markedly reduces the cell viability of PASMCs in a dose-dependent manner[2].
A-192621 (1-100 μM; 48 hours; PASMCs) treatment significantly increases the caspase-3/7 activity and cleaved caspase-3 expression in PASMCs. A-192621 induces apoptosis in a dose-dependent manner and increases the cells' susceptibility to apoptosis by Doxorubicin treatment[2].

Cell Viability Assay[2]

Cell Line: Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin
Concentration: 1 μM, 10 μM, 50 μM, 100 μM
Incubation Time: 72 hours
Result: The viability of PASMCs was significantly decreased in a dose-dependent manner.

Western Blot Analysis[2]

Cell Line: Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin
Concentration: 1 μM, 10 μM, 100 μM
Incubation Time: 72 hours
Result: The caspase-3/7 activity in PASMCs was significantly increased in a dose-dependent manner.
In Vivo

A-192621 (30-100 mg/kg; oral administration; daily; for 3 days; male Sprague-Dawley rats) treatment inhibits both dilatory and pressor responses induced by S6c mediated by ETB with an ED50 value of 30 mg/kg, and failed to inhibit the ET-1-induced pressor response mediated by ETA. A-192621 alone causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level in the conscious normotensive rat[3].

Animal Model: Male Sprague-Dawley rats (250-350 g)[3]
Dosage: 30 mg/kg 100 mg/kg
Administration: Oral administration; daily; for 3 days
Result: Inhibited both dilatory and pressor responses induced by S6c mediated by ETB with an ED50value of 30 mg/kg.
Molecular Weight

558.66

Formula

C₃₃H₃₈N₂O₆

CAS No.

195529-54-5

SMILES

O=C([[email protected]]1[[email protected]](C2=CC=C(OCCC)C=C2)N(CC(NC3=C(CC)C=CC=C3CC)=O)C[[email protected]@H]1C4=CC=C(OCO5)C5=C4)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

A-192621A192621A 192621Endothelin ReceptorApoptosisETBcaspase-3apoptosisDoxorubicinvascularremodelingbloodpressureET-1Inhibitorinhibitorinhibit

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