B-90063

Name: B-90063
Brand: BOC Sciences
Rating: 5 (1 reviews)

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Category	Enzyme inhibitors
Catalog number	BBF-03222
CAS
Molecular Weight	582.69
Molecular Formula	C28H30N4O6S2

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Product Description

B-90063 is an endothelin transferase (ECE) inhibitor produced by Blastobacter sp. SANK 71894. It has a strong inhibitory effect on human and rat ECE, with IC50 of 1.0 and 3.2 µmol/L, respectively.

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IUPAC Name	5-[[6-formyl-4-oxo-2-(2-pentyl-1,3-oxazol-4-yl)-1H-pyridin-3-yl]disulfanyl]-4-oxo-6-(2-pentyl-1,3-oxazol-4-yl)-1H-pyridine-2-carbaldehyde
Canonical SMILES	CCCCCC1=NC(=CO1)C2=C(C(=O)C=C(N2)C=O)SSC3=C(NC(=CC3=O)C=O)C4=COC(=N4)CCCCC
InChI	InChI=1S/C28H30N4O6S2/c1-3-5-7-9-23-31-19(15-37-23)25-27(21(35)11-17(13-33)29-25)39-40-28-22(36)12-18(14-34)30-26(28)20-16-38-24(32-20)10-8-6-4-2/h11-16H,3-10H2,1-2H3,(H,29,35)(H,30,36)
InChI Key	XGYVRFWCPUXVES-UHFFFAOYSA-N

Appearance	Yellow Crystal Powder
Boiling Point	760.0±60.0°C at 760 mmHg
Melting Point	73-74°C
Density	1.4±0.1 g/cm3

1. B-90063, a novel endothelin converting enzyme inhibitor isolated from a new marine bacterium, Blastobacter sp. SANK 71894

S Takaishi, N Tuchiya, A Sato, T Negishi, Y Takamatsu, Y Matsushita, T Watanabe, Y Iijima, H Haruyama, T Kinoshita, M Tanaka, K Kodama J Antibiot (Tokyo). 1998 Sep;51(9):805-15. doi: 10.7164/antibiotics.51.805.

A novel endothelin-converting enzyme (ECE) inhibitor, B-90063, was isolated from the culture supernatant of the newly discovered marine bacterium Blastobacter sp. SANK 71894. Based on spectral analyses and chemical reactions, the structure of B-90063 was determined to be bis[6-formyl-4-hydroxy-2-(2'-n-pentyloxazol-4'-yl)-4-pyridon -3-yl]-disulfide (1a). Human and rat ECEs were inhibited more potently by B-90063, with respective IC50 values of 1.0 and 3.2 microM, than were other neutral endopeptidases such as NEP and type-I and -IV collagenases. B-90063 also inhibited the binding of ET-1 to rat ET(A) and bovine ET(B) receptors, though its antagonistic activities were weak. B-90063, thus, may abolish the physiological actions of endothelins through the ECE inhibitory and receptor antagonistic mechanisms.

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