N-[2-Methoxy-4-(4-morpholinyl)phenyl]-2-(3-pyridinyl)-4-thiazolecarboxamide Struktur

N-[2-Methoxy-4-(4-morpholinyl)phenyl]-2-(3-pyridinyl)-4-thiazolecarboxamide

Bezeichnung:N-[2-Methoxy-4-(4-morpholinyl)phenyl]-2-(3-pyridinyl)-4-thiazolecarboxamide

CAS-Nr1042672-97-8

Englisch Name:N-[2-Methoxy-4-(4-morpholinyl)phenyl]-2-(3-pyridinyl)-4-thiazolecarboxamide

CBNumberCB32604265

SummenformelC20H20N4O3S

Molgewicht396.46

MOL-Datei1042672-97-8.mol

N-[2-Methoxy-4-(4-morpholinyl)phenyl]-2-(3-pyridinyl)-4-thiazolecarboxamide physikalisch-chemischer Eigenschaften

Dichte	1.335
storage temp.	Sealed in dry,Store in freezer, under -20°C
Löslichkeit	insoluble in EtOH; insoluble in H2O; ≥9.9 mg/mL in DMSO
Aggregatzustand	solid
pka	10.19±0.70(Predicted)

Gefahreninformationscode (GHS)

N-[2-Methoxy-4-(4-morpholinyl)phenyl]-2-(3-pyridinyl)-4-thiazolecarboxamide Chemische Eigenschaften,Einsatz,Produktion Methoden

Biologische Aktivität
irak inhibitor 6 is an interleukin-1 receptor associated kinase 4 (irak-4) inhibitor.the interleukin-1 receptor associated kinases (iraks) are a family of serine/threonine kinases related with regulating cellular signalling downstream of the il-18, il-1 and various toll-like receptors. irak-4 is reported to be essential for the activation of the intracellular signalling cascades including nfкb and mapk pathways, which are critical for the production of inflammatory cytokines.
in vitro
a quantitative structure–activity relationship (qsar) study of irak inhibitor 6 and its analogs were conducted by using the genetic algorithm and multiple linear regression (ga-mlr) method [1]. in vitro study showed that compared with its unsubstituted phenyl amide analog, the ortho-substitution with chloro, methoxy and difluoromethoxy analogs of irak inhibitor 6 improved potency against irak-4 significantly. these potency effects were additive, with the most active example in the set being irak inhibitor 6, in which the presence of nitrogen-linked substituents at the para position had a beneficial effect on the rate of turnover by human microsomes (20 μl/min/mg protein) [2].
IC 50
0.16 μm for irak-4
Einzelnachweise
[1] pourbasheer e, riahi s, ganjali mr, norouzi p. quantitative structure-activity relationship (qsar) study of interleukin-1 receptor associated kinase 4 (irak-4) inhibitor activity by the genetic algorithm and multiple linear regression (ga-mlr) method. j enzyme inhib med chem. 2010 dec;25(6):844-53.
[2] buckley gm, gowers l, higueruelo ap, jenkins k, mack sr, morgan t, parry dm, pitt wr, rausch o, richard md, sabin v, fraser jl. irak-4 inhibitors. part 1: a series of amides. bioorg med chem lett. 2008 jun 1;18(11):3211-4.

N-[2-Methoxy-4-(4-morpholinyl)phenyl]-2-(3-pyridinyl)-4-thiazolecarboxamide Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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