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Merck
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Documenti

PZ0416

Sigma-Aldrich

PF-05480090

≥98% (HPLC)

Sinonimo/i:

(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

Formula empirica (notazione di Hill):
C14H18N2O6S
Numero CAS:
287406-12-6
Peso molecolare:
342.37
Codice UNSPSC:
12352200
NACRES:
NA.77

Livello qualitativo

100

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear

Temperatura di conservazione

2-8°C

Stringa SMILE

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

Azioni biochim/fisiol

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.).

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

Cerca il Certificati d'analisi (COA) digitando il numero di lotto/batch corrispondente. I numeri di lotto o di batch sono stampati sull'etichetta dei prodotti dopo la parola ‘Lotto’ o ‘Batch’.

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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
Yuhua Zhang et al.
International immunopharmacology, 4(14), 1845-1857 (2004-11-09)
TNF-alpha converting enzyme (TACE) is a validated therapeutic target for the development of oral tumor necrosis factor-alpha (TNF-alpha) inhibitors. Here we report the pre-clinical results and characterization of a selective and potent TACE inhibitor, (2R, 3S)-2-([[4-(2-butynyloxy)phenyl]sulfonyl]amino)-N,3-dihydroxybutanamide (TMI-2), in various in
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
Joseph C Lownik et al.
Biochemical and biophysical research communications, 512(4), 723-728 (2019-03-31)
Group 2 innate lymphoid cells (ILC2s) play an important role in the initiation of type-2 immune responses. Numerous targets have been identified that may activate or repress ILC2 function, though few negative regulatory feedback pathways induced upon activation have been
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