212481-66-8
Chemical Structure
ABT-546
Synonym(s): A-216546
- CAS No.: 212481-66-8
- Formula:C30H48N2O6
- Molecular Weight:532.71
IUPAC Name: (2S,3R,4S)-1-(2-(dibutylamino)-2-oxoethyl)-2-(2,2-dimethylpentyl)-4-(7-methoxybenzo[d][1,3]dioxol-5-yl)pyrrolidine-3-carboxylic acid
InChIKey: OAEWNSKRLBVVBV-QSEAXJEQSA-N
SMILES: O=C([C@H]1[C@H](CC(C)(C)CCC)N(CC(N(CCCC)CCCC)=O)C[C@@H]1C2=CC(OC)=C(OCO3)C3=C2)O
Biological Activity: ABT-546 (A-216546) is an orally active ETA receptor antagonist, with Ki values of 0.46 nM and 13000 nM for human ETA and ETB receptors, respectively, and exhibits >25000-fold selectivity over the ETB receptor. ABT-546 effectively inhibits ET-1 (HY-P0202)-induced phosphoinositide hydrolysis (IC50 = 0.59 nM) and arachidonic acid release (IC50 = 3.03 nM), and antagonizes ET-1-induced contraction in isolated vascular rings. ABT-546 crosses the placental barrier but shows extremely low fetal exposure, with a favorable safety profile. ABT-546 inhibits ET-1-induced pressor response and downregulates the NLRP3/ROS/GSDMD-mediated pyroptosis pathway. ABT-546 can be used for research on abdominal aortic aneurysm[1][2][3][4][5][6].
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ABT-546 | ABT-546 (A-216546) is an orally active ETA receptor antagonist, with Ki values of 0.46 nM and 13000 nM for human ETA and ETB receptors, respectively, and exhibits >25000-fold selectivity over the ETB receptor. ABT-546 effectively inhibits ET-1 (HY-P0202)-induced phosphoinositide hydrolysis (IC50 = 0.59 nM) and arachidonic acid release (IC50 = 3.03 nM), and antagonizes ET-1-induced contraction in isolated vascular rings. ABT-546 crosses the placental barrier but shows extremely low fetal exposure, with a favorable safety profile. ABT-546 inhibits ET-1-induced pressor response and downregulates the NLRP3/ROS/GSDMD-mediated pyroptosis pathway. ABT-546 can be used for research on abdominal aortic aneurysm. | |||||||||||||||||||||
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References
- [1]. Liu G, et al. Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (ABT-546). J Med Chem. 1998 Aug 13;41(17):3261-75. [Content Brief]
- [2]. Wu-Wong JR, et al. Pharmacology of ABT-546: a highly selective antagonist for endothelin ET(A) receptor. Eur J Pharmacol. 1999 Feb 5;366(2-3):189-201. [Content Brief]
- [3]. Thaete LG, et al. Endothelin receptor antagonist has limited access to the fetal compartment during chronic maternal administration late in pregnancy. Life Sci. 2012 Oct 15;91(13-14):583-6. [Content Brief]
- [4]. 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. [Content Brief]
- [5]. Wu-Wong JR, et al. Endothelin stimulates glucose uptake and GLUT4 translocation via activation of endothelin ETA receptor in 3T3-L1 adipocytes. J Biol Chem. 1999 Mar 19;274(12):8103-10. [Content Brief]
- [6]. Liu S, et al. 3, 4-Benzopyrene (Bap) aggravated abdominal aortic aneurysm formation by targeting pyroptosis in smooth muscle cells through ET-1 mediated NLRP3-inflammasome activation. Int Immunopharmacol. 2023 Nov;124(Pt A):110851. [Content Brief]
