| Chemical Properties | Back Directory | [density ]
1.515±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear (Warmed) | [form ]
Solid | [pka]
8.643±0.40(predicted) | [color ]
White to off-white | [SMILES]
CC1=NC2=NC(SCC(N(C(C(N3)=O)=C(N)N(CC4=CC=CC=C4)C3=O)C)=O)=NN2C(C)=C1 |
| Hazard Information | Back Directory | [Uses]
nti-inflammatory agent 49 (compound SC9) is a quite potent and selective inhibitor of Drp1-Fis1 interaction and can reduce FIS1-mediated mitochondrial dysfunction. The IC50 of SC9 inhibiting GTPase in vitro is 270 nM[1]. | [Biological Activity]
Cell penetrantpotent and selective inhibitor of GTPase activity of dynamin-related protein 1 (Drp1).
Drp1 inhibitor SC9 is a cell penetrantpotent and selective inhibitor of GTPase activity of dynamin-related protein 1 (Drp1) th at binds to a switch I-adjacent grove (SWAG) on Drp1. SC9 inhibits Drp1-Fis1 interaction in cells and eases the burden of Drp1-mediated pathologies such as LPS-induced mitochondrial dysfunction. It rescues mice from LPS-induced endotoxemia. | [in vivo]
Anti-inflammatory agent 49 (10 mg/kg, every 8 h for 72 h) rescues mice from LPS-induced endotoxemia[1]. | Animal Model: | Female BALB/c AnNCrl micee (Strain Code 028)[1] | | Dosage: | LPS doses 10–16.67 mg/kg, SC9 doses 10 mg/kg(after 4 h) | | Administration: | Intraperitoneal injection: 0.2 mL of LPS,0.1 mL of CS9; scored every 8 h for 72 h. | | Result: | Improved mouse survival at all LPS doses tested at the different LPS doses (10 to 16.6 mg/kg) .
Dramatically reduced the occurrence of critical symptoms such as respiratory distress. |
| [References]
[1] Luis Rios, et al. Targeting an allosteric site in dynaminrelated protein 1 to inhibit Fis1-mediated mitochondrial dysfunction. Nat Commun. 2023 Jul 19;14(1):4356 DOI:10.1038/s41467-023-40043-0 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|