SLx-2119 Struktur

SLx-2119

Bezeichnung:SLx-2119

CAS-Nr911417-87-3

Englisch Name:SLx-2119

CBNumberCB82624291

SummenformelC26H24N6O2

Molgewicht452.51

MOL-Datei911417-87-3.mol

SLx-2119 physikalisch-chemischer Eigenschaften

Schmelzpunkt	>228oC (dec.)
Siedepunkt	682.6±55.0 °C(Predicted)
Dichte	1.318±0.06 g/cm3(Predicted)
storage temp.	2-8°C(protect from light)
Löslichkeit	Soluble in DMSO (25 mg/ml)
pka	13?+-.0.40(Predicted)
Aggregatzustand	solid
Farbe	White
Stabilität	Stable for 1 year as supplied from date of purchase. Solutions in DMSO may be stored at -20°C for up to 1 month.

Gefahreninformationscode (GHS)

SLx-2119 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
KD 025 is an inhibitor of Rho-associated kinase 2 (ROCK2; IC₅₀ = 0.105 μM). It is selective for ROCK2 over ROCK1 (IC₅₀ = 24 μM). KD 025 (10 μM) decreases the expression of connective tissue growth factor (CTGF) and induces remodeling of the actin cytoskeleton in isolated human ileal fibrotic smooth muscle cells. It inhibits heat-killed C. albicans- or S. epidermidis-induced production of IL-17 in isolated human peripheral blood mononuclear cells (PBMCs) when used at concentrations ranging from 1.25 to 10 μM. KD 025 (100 and 200 mg/kg) reduces infarct volume in a mouse model of cerebral ischemia induced by transient middle cerebral artery occlusion (MCAO). It decreases disease severity in a mouse model of sclerodermatous chronic graft versus host disease (GVHD) when administered at a dose of 150 mg/kg. Formulations containing KD 025 have been used in the treatment of chronic GVHD.
Verwenden
KD 025 is an inhibitor of Rho-associated protein kinase II (ROCK-II), a serine/threonine kinase that regulates the formation of actin stress fibers and focal adhesions, smooth muscle contraction, and gene expression (1, 2). KD025 has been shown to reduce infarct volume after transient middle cerebral artery occlusion (2).
Trademarks
Rezurock
Allgemeine Beschreibung
Class: serine-threonine kinase; Treatment: chronic GVHD; Other name: SLx-2119, KD025; Oral bioavailability = 64%; Elimination half-life = 19 h; Protein binding = 99.9%
target
Primary target: ROCK2
Einzelnachweise
Boerma et al. (2008) Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin; Blood Coagul. Fibrinolysis.?19 709 Zanin-Zhorov et al. (2014) Selective oral ROCK2 inhibitor down-regulates IL-21 and IL-17 secretion in human T cells via STAT3-dependent mechanism; Natl. Acad. Sci. USA?111 16814 Flynn et al. (2016) Targeted Rho-associated kinase 2 inhibition suppresses murine and human chronic GVHD through a Stat3-dependent mechanism; 127 2144 Jagasia et al. (2021) ROCK2 Inhibition with Belumosudil (KD025) for the Treatment of Chronic Graft-Versus-Host Disease; Clin. Invest.?39 1888 Diep et al. (2018) Anti-adipogenic effects of KD025 (SLx-2119), a ROCK2-specific inhibitor, in 3T3-L1 cells; Rep.?8 2477 Diep et al. (2019) KD025 (SLx-2119) suppresses adipogenesis at intermediate stage in human adipose-derived stem cells; Adipocyte?9 114 Wei et al. (2020) ROCK2 inhibition enhances the thermogenic program in white and brown fat tissue in mice; FASEB J.?34 474 Tran and Chun (2021) ROCK2-Specific Inhibitor KD025 Suppresses Adipocyte Differentiation by Inhibiting Casein Kinase 2; Molecules?26 4747

SLx-2119 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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