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A-192621

CAT: 0804-HY-120295-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-120295-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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][2][3].
CAS Number
195529-54-5
UNSPSC
12352005
Target
Apoptosis; Endothelin Receptor
Type
Reference compound
Related Pathways
Apoptosis; GPCR/G Protein
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Endocrinology; Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/a-192621.html
Purity
99.85
Solubility
DMSO : ≥ 100 mg/mL
Smiles
O=C([C@H]1[C@H](C2=CC=C(OCCC)C=C2)N(CC(NC3=C(CC)C=CC=C3CC)=O)C[C@@H]1C4=CC=C(OCO5)C5=C4)O
Molecular Formula
C33H38N2O6
Molecular Weight
558.66
References & Citations
[1]Wu-Wong JR, et al. Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies. Clin Sci (Lond) . 2002 Aug;103 Suppl 48:107S-111S.|[2]Sakai S, et al. Antagonists to endothelin receptor type B promote apoptosis in human pulmonary arterial smooth muscle cells. Life Sci. 2016 Aug 15;159:116-120.|[3]Wessale JL, et al. Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies. Clin Sci (Lond) . 2002 Aug;103 Suppl 48:112S-117S.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
ETA; ETB

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