AS-605240

供应商：上海经科化学科技有限公司

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本试剂(AS-605240)
仅供科研实验使用,不得用于其他用途！

简介：
货 号：A-2109
名 称：AS-605240
别 名：AS-605240 Free Base
C A S ：648450-29-7
分子量：257.27
分子式：C12H7N3O2S
纯 度：HPLC/TLC:>99%
说 明：
文 献：AS-605240 is a selective and ATP-competitive p110[gamma] inhibitor (Ki = 7.8 nM, IC50 = 8 nM at an ATP concentration corresponding to the experimental Km value), with over 30-fold selectivity for PI3K[delta] and PI3K[beta], and 7.5-fold selectivity over PI3K[alpha]. AS-605240 inhibited leukocyte migration in vivo and ameliorated [alpha]CII-induced arthritis and collagen-induced arthritis. Camps M., et al. "Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis." Nat. Med. 11: 936-943 (2005). This research compound is the free base form of AS-605240. We also offer the potassium salt form; please see AS-605240, Potassium Salt, Cat. No. [A-2188] The PI3K[gamma] pathway is highly activated in type 1 diabetes. AS-605240 inhibited T-cell activation and the production of inflammatory cytokines by autoreactive T cells in vitro and in vivo. It blocked and reversed autoimmune diabetes in NOD mice. Azzi J., et al. "The novel therapeutic effect of phosphoinositide 3-kinase-γ inhibitor AS605240 in autoimmune diabetes." Diabetes 61: 1509-1518 (2012). AS-605240 significantly enhanced resistance against L. mexicana by inhibition of parasite entry into phagocytes and reduction in recruitment of host phagocytes and regulatory T cells to the site of infection. AS-605240 was shown to be as effective as the standard antileishmanial drug sodium stibogluconate in treatment of cutaneous leishmaniasis caused by L. mexicana. Cummings H.E., et al. "Critical role for phosphoinositide 3-kinase gamma in parasite invasion and disease progression of cutaneous leishmaniasis." Proc. Natl. Acad. Sci. USA 109: 1251-1256 (2012). Accumulation of cholesterol by macrophage uptake of low-density lipoprotein (LDL) plays a key role in the formation of atherosclerotic plaques. AS-605240 was shown to inhibit murine bone marrow-derived macrophages differentiated with GM-CSF from becoming foam cells. Anzinger J.J., et al. "Murine bone marrow-derived macrophages differentiated with GM-CSF become foam cells by PI3Kγ-dependent fluid-phase pinocytosis of native LDL." J. Lipid Res. 53: 34-42 (2012). AS-605240 enhanced vasodilatation and reduced blood pressure in normotensive mice in a concentration-dependent manner. Carnevale D., et al. "PI3Kγ inhibition reduces blood pressure by a vasorelaxant Akt/L-type calcium channel mechanism." Cardiovasc. Res. 93: 200-209 (2012). AS-605240 inhibited inflammatory cell recruitment and production of inflammatory cytokines, and prevented bleomycin-induced pulmonary fibrosis in rats. Wei X., et al. "A phosphoinositide 3-kinase-gamma inhibitor, AS605240 prevents bleomycin-induced pulmonary fibrosis in rats." Biochem. Biophys. Res. Commun. 397: 311-317 (2010). AS-605240 inhibited trypsin-induced pruriceptive, inflammatory, and nociceptive responses in mice. Pereira P.J., et al. "Inhibition of phosphatidylinositol-3 kinase γ reduces pruriceptive, inflammatory, and nociceptive responses induced by trypsin in mice." Pain 152: 2861-2869 (2011).