Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
C[C@@H]([C@H](C(NO)=O)NS(=O)(C1=CC=C(C=C1)OCC#CC)=O)O
InChI
1S/C14H18N2O6S/c1-3-4-9-22-11-5-7-12(8-6-11)23(20,21)16-13(10(2)17)14(18)15-19/h5-8,10,13,16-17,19H,9H2,1-2H3,(H,15,18)/t10-,13+/m0/s1
InChI key
VMOSDDURWLNMNG-GXFFZTMASA-N
Biochem/physiol Actions
PF-05480090 (PF-5480090; TMI-2) is an orally active, potent TACE (ADAM17) inhibitor (IC50 = 2 nM) with good selectivity over ADAM10 (IC50 = 1.09 μM), MMP-1/7 (IC50 = 2.47/0.96 μM) and MMP-8/9/13/14 (IC50 =35/ 777/96/582 nM). TMI-2 inhibits LPS-induced TNF production in cultrues (RAW/THP-1 IC50 = 200/430 nM), ex vivo (human whole blood IC50 = 1 μM) and in vivo (ED50 = 3 mg/kg; TMI-2 p.o. 1 hr prior to 40 ng LPS/mouse i.v.). TMI-2 is efficacious in a rat model of adjuvant-induced arthritis (AIA; 30 and 100 mg/kg p.o. b.i.d.) and a murine model of collagen-induced arthritis (CIA; 100 mg/kg p.o. b.i.d.).
存储类别
11 - Combustible Solids
怎么回事?
WGK 3
闪点 (F)
Not applicable
闪点 (°C)
Not applicable