(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
- Product Name
- (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
- CAS No.
- 847928-32-9
- Chemical Name
- (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
- Synonyms
- 1G244;1G-244,1G244;(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione;2-Amino-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-1-(1,3-dihydro-2H-isoindol-2-yl)-1,4-butaned;(2S)-2-amino-4-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-1-(1,3-dihydroisoindol-2-yl)butane-1,4-dione;1,4-Butanedione, 2-amino-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-1-(1,3-dihydro-2H-isoindol-2-yl)-, (2S)-
- CBNumber
- CB23367548
- Molecular Formula
- C29H30F2N4O2
- Formula Weight
- 504.57
- MOL File
- 847928-32-9.mol
(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione Property
- Boiling point:
- 674.3±55.0 °C(Predicted)
- Density
- 1.304±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C(protect from light)
- solubility
- Soluble in DMSO (>20 mg/ml)
- pka
- 7.25±0.33(Predicted)
- form
- solid
- color
- Off-white
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
N-Bromosuccinimide Price
- Product number
- CS-0064911
- Product name
- 1G244
- Purity
- 98.55%
- Packaging
- 5mg
- Price
- $85
- Updated
- 2021/12/16
- Product number
- CS-0064911
- Product name
- 1G244
- Purity
- 98.55%
- Packaging
- 10mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- CS-0064911
- Product name
- 1G244
- Purity
- 98.55%
- Packaging
- 25mg
- Price
- $320
- Updated
- 2021/12/16
- Product number
- Y0432
- Product name
- 1G244
- Packaging
- 10mg
- Price
- $389
- Updated
- 2021/12/16
- Product number
- 847928329
- Product name
- (S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione
- Packaging
- 100mg
- Price
- $1163.25
- Updated
- 2021/12/16
(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione Chemical Properties,Usage,Production
Description
1G244 (847928-32-9) is a potent and selective inhibitor of the prolyl dipeptidases DPP8 (IC50 = 14 nM) and DPP9 (IC50 = 53 nM).1,2? It does not inhibit DPP2, DPP4 or fibroblast activation protein (FAP) at 100 μM.1,2 1G244 is a slow binding competitive inhibitor of DPP8 but a competitive and reversible inhibitor of DPP9.2? Inhibition of DPP8/9 by 1G244 has been shown to cause pro-caspase-1-dependent pyroptosis in macrophages and monocytes.3 1G244 also induced cell death in DPP8/9 knockout cells at higher concentration indicating there may be some off-target effects.3 1G244 blocks adipogenesis in preadipocyte 3T3-L1 and 3T3-F422A cells.4? DPP8/9 inhibition attenuates PPARg2 induction during preadipocyte differentiation.4 Because of its inhibitory effects on pro-inflammatory macrophages, 1G244 inhibition of DPP8/9 has been examined as a potential therapy for reducing atherosclerosis and/or in the prevention of plaque rupture.5,6 Cell permeable.
References
Jiaang et al. (2005), Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8; Bioorg.Med.Chem.Lett.15 687 Wu et al. (2009), Biochemistry, pharmacokinetics, and toxicology of a potent and selective DPP8/9 inhibitor; Biochem.Pharmacol. 78 203 Okondo et al. (2017), DPP8/9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis; Nat.Chem.Biol. 13 46 Han et al. (2015), Inhibition of dipeptidyl peptidase 8/9 impairs preadipocyte differentiation; Sci.Rep. 5 12348 Matheeussen et al. (2013), Dipeptidyl peptidases in atherosclerosis: expression and role in macrophage differentiation, activation and apoptosis; Basic Res.Cardiol. 108 350 Waumans et al. (2016), The Dipeptidyl Peptidases 4,8, and 9 in Mouse Monocytes and Macrophages: DPP8/9 Inhibition Attenuates M1 Macrophage Activation in Mice; Inflammation 39 413
(S)-2-Amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione Preparation Products And Raw materials
Raw materials
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