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J-104132

Catalog No. T27647 CAS 198279-45-7

Synonyms: L753037, L 753037, J104132, J 104132, L-753037

J-104132 is a potetn and selective endothelin A/B receptor antagonist (Ki: cloned human ETA = 0.034 nM; cloned human ETB = 0.104 nM) . In vitro, J-104132 is a potent antagonist of ET-1-induced accumulation of [3H]inositol phosphates in Chinese hamster ovary cells stably expressing cloned human ETA receptors (IC50 = 0.059 nM). Pretreatment with J-104132 prevents the lethal response to ET-1 when administered i.v. (ED50 = 0.045 mg/kg) or p.o. in fed animals (ED50 = 0.35 mg/kg).

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J-104132, CAS 198279-45-7

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 4,370.00
50 mg	10-14 weeks	$ 5,780.00
100 mg	10-14 weeks	$ 8,200.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

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Description

Synonyms	L753037, L 753037, J104132, J 104132, L-753037
Molecular Weight	531.6
Formula	C31H33NO7
CAS No.	198279-45-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Kitada K, Yui N, Mori T, Ohkita M, Matsumura Y. Vasoprotective effects of an endothelin receptor antagonist in ovariectomized female rats. Life Sci. 2014 Nov 24;118(2):379-85. doi: 10.1016/j.lfs.2014.01.009. PubMed PMID: 24468711. 2. Kitada K, Yui N, Koyama M, Kimura K, Suzuki R, Tanaka R, Mori T, Ohkita M, Matsumura Y. Endothelin ETB receptor is involved in sex differences in the development of balloon injury-induced neointimal formation. J Pharmacol Exp Ther. 2011 Feb;336(2):533-9. doi: 10.1124/jpet.109.165308. PubMed PMID: 21075838. 3. Kitada K, Yui N, Matsumoto C, Mori T, Ohkita M, Matsumura Y. Inhibition of endothelin ETB receptor system aggravates neointimal hyperplasia after balloon injury of rat carotid artery. J Pharmacol Exp Ther. 2009 Dec;331(3):998-1004. doi: 10.1124/jpet.109.157065. PubMed PMID: 19737855. 4. Homma N, Nagaoka T, Morio Y, Ota H, Gebb SA, Karoor V, McMurtry IF, Oka M. Endothelin-1 and serotonin are involved in activation of RhoA/Rho kinase signaling in the chronically hypoxic hypertensive rat pulmonary circulation. J Cardiovasc Pharmacol. 2007 Dec;50(6):697-702. PubMed PMID: 18091588.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

J-104132 198279-45-7 L753037 L 753037 J104132 J 104132 L-753037 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.