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PZ0416

Sigma-Aldrich

PF-05480090

≥98% (HPLC)

Synonym(e):

(2R,3S)-2-(4-(But-2-ynyloxy)phenylsulfonamido)-N,3-dihydroxybutanamide, (2R,3S)-2-({[4-(2-Butynyloxy)phenyl]sulfonyl}amino)-N,3-dihydroxybutanamide, (2R,3S)-2-[[[4-(2-Butyn-1-yloxy)phenyl]sulfonyl]amino]-N,3-dihydroxybutanamide, PF 05480090, PF 548, PF 5480090, PF-548, PF-5480090, PF05480090, PF548, PF5480090, TMI 002, TMI 2, TMI-002, TMI-2, TMI002, TMI2, WAY 180022, WAY 18022, WAY-180022, WAY-18022, WAY180022, WAY18022

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About This Item

Empirische Formel (Hill-System):
C14H18N2O6S
CAS-Nummer:
287406-12-6
Molekulargewicht:
342.37
UNSPSC-Code:
12352200
NACRES:
NA.77

Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 2 mg/mL, clear

Lagertemp.

2-8°C

SMILES String

C[C@@H]([C@H](C(NO)=O)NS(=O)(C1=CC=C(C=C1)OCC#CC)=O)O

Biochem./physiol. Wirkung

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.).

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

Suchen Sie nach Analysenzertifikate (COA), indem Sie die Lot-/Chargennummer des Produkts eingeben. Lot- und Chargennummern sind auf dem Produktetikett hinter den Wörtern ‘Lot’ oder ‘Batch’ (Lot oder Charge) zu finden.

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Die Dokumentenbibliothek aufrufen

Mengcheng Shen et al.
Circulation research, 123(3), 372-388 (2018-06-23)
ADAM17 (a disintegrin and metalloproteinase-17) is a membrane-bound enzyme that regulates bioavailability of multiple transmembrane proteins by proteolytic processing. ADAM17 has been linked to several pathologies, but its role in thoracic aortic aneurysm (TAA) has not been determined. The objective
Marta Stolarczyk et al.
American journal of physiology. Lung cellular and molecular physiology, 314(4), L555-L568 (2018-01-20)
The EGF receptor (EGFR)/a disintegrin and metalloproteinase 17 (ADAM17) signaling pathway mediates the shedding of growth factors and secretion of cytokines and is involved in chronic inflammation and tissue remodeling. Since these are hallmarks of cystic fibrosis (CF) lung disease
Amy W Ku et al.
eLife, 5 (2016-12-09)
Myeloid-derived suppressor cells (MDSC) contribute to an immunosuppressive network that drives cancer escape by disabling T cell adaptive immunity. The prevailing view is that MDSC-mediated immunosuppression is restricted to tissues where MDSC co-mingle with T cells. Here we show that

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