| Identification | Back Directory | [Name]
MF 438 | [CAS]
921605-87-0 | [Synonyms]
MF 438
2-methyl-5-[6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazin-3-yl]-1,3,4-thiadiazole
3-(5-Methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]-1-piperidinyl]pyridazine
Pyridazine, 3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]-1-piperidinyl]- | [Molecular Formula]
C19H18F3N5OS | [MDL Number]
MFCD28386313 | [MOL File]
921605-87-0.mol | [Molecular Weight]
421.44 |
| Chemical Properties | Back Directory | [Boiling point ]
614.5±65.0 °C(Predicted) | [density ]
1.365±0.06 g/cm3(Predicted) | [storage temp. ]
-20° | [solubility ]
Soluble in DMSO (up to 5 mg/ml) or in Ethanol (up to 2 mg/ml with warming). | [form ]
solid | [pka]
2.29±0.10(Predicted) | [color ]
Off-white | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month. |
| Hazard Information | Back Directory | [Description]
MF-438 (921605-87-0) is a potent inhibitor of stearoyl-CoA desaturase 1 (SCD1) – IC50?= 2.3 nM.1?MF-438 was potent in an?in vivo?mouse liver PD assay (ED50?between 1 and 3 mg/kg).1?Cancer initiating cells (CSC-like) were shown to be much more sensitive to MF-438 inhibition of SCD1 than progenitor and terminally differentiated cancer cells in a lung cancer model.2?MF-438 showed good oral bioavailability and metabolic stability making it an excellent tool for studying the effects of SCD1 in various disease models. | [Uses]
MF-438 is a potent and orally bioavailable stearoyl-CoA desaturase 1 (SCD1) inhibitor with an IC50 of 2.3 nM for rSCD1[1]. | [in vivo]
MF-438 exhibits an ED50 between 1 and 3 mg/kg in a mouse model[1]. | [References]
1) Leger?et al. (2010),?Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438); Bioorg. Med. Chem. Lett.,?20?499
2) Noto?et al. (2013),?Stearoyl-CoA desaturase-1 is a key factor for lung cancer-initiating cells; Cell Death and Differ.,?4?e947
3) Rodriguez-Perez?et al.?(2017),?Altered fatty acid metabolism and reduced stearoyl-coenzyme A desaturase activity in asthma; Allergy,?72?1744 [Citation] |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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