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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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A607282-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,334.90 | |
A607282-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $229.90 | |
A607282-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,001.90 | |
A607282-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $739.90 |
Synonyms | MS-30166 | (2R,3R,4S)-4-Benzo[1,3]dioxol-5-yl-1-[(2,6-diethyl-phenylcarbamoyl)-methyl]-2-(4-propoxy-phenyl)-pyrrolidine-3-carboxylic acid | 3-PYRROLIDINECARBOXYLIC ACID, 4-(1,3-BENZODIOXOL-5-YL)-1-(2-((2,6-DIETHYLPHENYL)AMINO)-2-OXOETHYL)-2-(4-PROPOXYPHEN |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | A192621 is a selective; orally available ETB endothelin receptor antagonist. A192621 has been shown to cause an increase in arterial blood pressure and to promote apoptosis in human pulmonary arterial smooth muscle cells. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | ANTAGONIST |
Mechanism of action | Antagonist of ET B receptor |
Product 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. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | (2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(2,6-diethylanilino)-2-oxoethyl]-2-(4-propoxyphenyl)pyrrolidine-3-carboxylic acid |
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INCHI | InChI=1S/C33H38N2O6/c1-4-16-39-25-13-10-23(11-14-25)32-30(33(37)38)26(24-12-15-27-28(17-24)41-20-40-27)18-35(32)19-29(36)34-31-21(5-2)8-7-9-22(31)6-3/h7-15,17,26,30,32H,4-6,16,18-20H2,1-3H3,(H,34,36)(H,37,38)/t26-,30-,32+/m1/s1 |
InChi Key | LQEHCKYYIXQEBM-FUKIBTTHSA-N |
Canonical SMILES | CCCOC1=CC=C(C=C1)C2C(C(CN2CC(=O)NC3=C(C=CC=C3CC)CC)C4=CC5=C(C=C4)OCO5)C(=O)O |
Isomeric SMILES | CCCOC1=CC=C(C=C1)[C@H]2[C@@H]([C@H](CN2CC(=O)NC3=C(C=CC=C3CC)CC)C4=CC5=C(C=C4)OCO5)C(=O)O |
Alternate CAS | 195529-54-5 |
PubChem CID | 5310991 |
MeSH Entry Terms | (2R-(2alpha,3beta,4alpha)-4-(1,3-benzodioxol-5-yl)-1-(2-(2,6-diethylphenyl)amino)-2-oxoethyl)-2-(4-propoxyphenyl)-3-pyrrolidinecarboxylic acid;A 192621;A-192621;A192621 |
Molecular Weight | 558.66 |
PubChem CID | 5310991 |
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ChEMBL Ligand | CHEMBL332794 |
BindingDB Ligand | 50080601 |
CAS Registry No. | 195529-54-5 |
GPCRdb Ligand | A192621 |
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