| Identification | Back Directory | [Name]
Unii-0789652qul | [CAS]
130112-42-4 | [Synonyms]
Ccris 8109
Mivotilate
Unii-0789652qul
Mivotilate [inn]
YH439 >=98% (HPLC)
Isopropyl-2-(1,3-dithietane-2-ylidene)-2[N-(4-methyl2-thiazol-2-yl)carbamoyl] acetate
Isopropyl 2-(1,3-dithietane-2-ylidine)-2-(N-(4-methyl-2-thiazol-2-yl)carbamoyl)acetate
2-(1,3-Dithietan-2-ylidene)-3-[(4-methyl-2-thiazolyl)amino]-3-oxo-propanoic acid 1-methylethyl ester
Propanoic acid, 2-(1,3-dithietan-2-ylidene)-3-[(4-methyl-2-thiazolyl)amino]-3-oxo-, 1-methylethyl ester | [Molecular Formula]
C12H14N2O3S3 | [MDL Number]
MFCD02752797 | [MOL File]
130112-42-4.mol | [Molecular Weight]
330.45 |
| Chemical Properties | Back Directory | [density ]
1.467±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥5mg/mL | [form ]
solid | [pka]
4.89±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
Mivotilate is an orally-active hepatoprotective agent introduced for the treatment of liver cirrhosis and hepatitis-B infection. It is a
dithietanylidene malonate analogue of malotilate and is without the
haemotological adverse effects associated with the latter. Mivotilate can be
obtained by partial saponification of the corresponding diisopropylmalonate,
conversion of the acid function into mixed anhydride then to the amide with an
aminothiazole. It displays potent hepatoprotective activity in rat and mice liver
injury models by a mechanism involving the inactivation of Kupffer cells.
Mivotilate was shown to exert multiple effects on the hepatic cytochrome P450
system, particularly to inhibit CYP2E1 expression and to up-regulate the
CYP1A1 expression. The low oral bioavailability of Mivotilate in rats (F<0.22%)
could be primarilly attributed to poor absorption and considerable hepatic and
gastrointestinal first-pass effects. Mivotilate prevents mutagenesis caused by
agents such as benzo[a]pyrene and reduces skin tumors induced by these
agents. | [Originator]
Yuhan Corp (South Korea) | [Uses]
Vasodilator (coronary). | [Definition]
ChEBI: Mivotilate is an aromatic amide, an isopropyl ester and a secondary carboxamide. | [in vivo]
Mivotilate (YH439, 150 mg/kg, p.o.) reduces CYP2E1-mediated NDMA demethylase activity in rats, but shows no obvious effect on NADPH-dependent P450 oxidoreductase activity. Mivotilate (75-300 mg/kg) rapidly decreases immunoreactive CYP2E1 protein. Mivotilate (150 mg/kg, p.o.) inhibits the transcription of CYP2E1 in rats[2]. |
|
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
ChemeGen 中国
|
| Tel: |
18818260767 |
| Website: |
https://www.chemegen.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
| Company Name: |
MedChemExpress
|
| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
|