| Identification | Back Directory | [Name]
DMP 777 | [CAS]
157341-41-8 | [Synonyms]
DMP 777
L 694458
L-694458; DMP-777; DMP777
(S)-N-((R)-1-(Benzo[d][1,3]dioxol-5-yl)butyl)-3,3-diethyl-2-(4-(4methyl-piperazine-1-carbonyl)
(S)-N-((R)-1-(Benzo[d][1,3]dioxol-5-yl)butyl)-3,3-diethyl-2-(4-(4methyl-piperazine-1-carbonyl)phe
(S)-N-((R)-1-(Benzo[d][1,3]dioxol-5-yl)butyl)-3,3-diethyl-2-(4-(4-Methylpiperazine-1-carbonyl)phenoxy)-4-oxoazetidine-1-carboxaMide
(2S)-N-[(1R)-1-(1,3-Benzodioxol-5-yl)butyl]-3,3-diethyl-2-[4-[(4-methyl-1-piperazinyl)carbonyl]phenoxy]-4-oxo-1-azetidinecarboxamide
1-AzetidinecarboxaMide,N-[(1R)-1-(1,3-benzodioxol-5-yl)butyl]-3,3-diethyl-2-[4-[(4-Methyl-1-piperazinyl)carbonyl]phenoxy]-4-oxo-,(2S)-
(S)-N-((R)-1-(Benzo[d][1,3]dioxol-5-yl)butyl)-3,3-diethyl-2-(4-(4methyl-piperazine-1-carbonyl)phenoxy)-4-oxoazetidine-1-carboxamide (3.5% w/w solution) | [Molecular Formula]
C31H40N4O6 | [MDL Number]
MFCD00871548 | [MOL File]
157341-41-8.mol | [Molecular Weight]
564.67 |
| Chemical Properties | Back Directory | [density ]
1.227 | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 38.33 mg/mL (67.88 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble) | [form ]
Powder | [pka]
pKa 7.04(H2O tunde?ned Iunde?ned) (Uncertain) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
DMP 777 is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor. | [Biological Activity]
DMP 777 is a potent, selective, orally available inhibitor of human leukocyte elastase (HLE). | [in vivo]
DMP-777-treated rats show a marked decrease in H/K-ATPase staining parietal cells. DMP-777-induced loss of parietal cells is significantly ameliorated with coadministration of omeprazole. DMP-777-treated animals demonstrates marked foveolar hyperplasia in the fundus with prominent expansion of diastase-resistant, PAS-positive surface mucous cells. When DMP-777 is coadministered with omprazole, there is a significant decrease in BrdUpositive S-phase cells compared with rats that receive DMP-777 alone. After oral dosing of monkeys at 40 mg/kg with DMP-777 the only stereoisomer detected in the post-dose plasma samples is the starting material DMP-777, and no inversion of the configuration at positions 'a' and 'b' of DMP- 777 has occurred in vivo. Mist1-/- mice treated with DMP-777 show fewer chief cell to SPEM transitions. Mist1-/- mice treated with L635 demonstrates significantly fewer proliferative SPEM cells compared to control mice. | [target]
Human leukocyte elastase (HLE) | [References]
[1] Ogawa M, et al. Omeprazole treatment ameliorates oxyntic atrophy induced by DMP-777. Dig Dis Sci. 2006 Mar;51(3):431-9. DOI:10.1007/s10620-006-3151-x
[2] Zagrobelny J, et al. Separation of the four stereoisomers of a potent inhibitor (L-694,458) of human leukocyte elastase and its determination in human plasma using achiral/chiral chromatography with column switching. J Pharm Biomed Anal. 1998 Sep 1;17(6-7 DOI:10.1016/s0731-7085(98)00071-5
[3] Weis VG, et al. Maturity and age influence chief cell ability to transdifferentiate into metaplasia. Am J Physiol Gastrointest Liver Physiol. 2016 Nov 23:ajpgi.00326.2016 DOI:10.1152/ajpgi.00326.2016 |
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| Company Name: |
SPIRO PHARMA
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| Telephone: |
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| Website: |
www.spiropharma.com.cn |
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