GSK269962A HCl

製品コードS7687 バッチS768702

印刷

化学情報

Chemical Structure Synonyms GSK269962B, GSK269962 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C29H30N8O5.HCl
分子量 607.06 CAS No. 2095432-71-4
Solubility (25°C)* 体外 DMSO 100 mg/mL (164.72 mM)
Ethanol 28 mg/mL (46.12 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 GSK269962A HClは一種の選択性的なROCK阻害剤で、ROCK1とROCK2に作用する時のIC50値が1.6nMと4nMに分かれることです。
in vitro GSK269962A completely abolished the actin stress fiber formation induced by angiotensin II in human smooth muscles. Such suppressive effect on actin fiber formation was observed beginning at around 1 μM GSK269962A. GSK269962A induced vasorelaxation in preconstricted rat aorta(tissue baths) with an IC50 of 35 nM. the relaxation induced by GSK269962A is reversible. GSK269962A suppressed IL-6 mRNA transcription and reduced LPS-induced IL-6 and TNF-α protein production in macrophages[1].
in vivo Oral administration of GSK269962A produced a profound dose-dependent reduction of systemic blood pressure in spontaneously hypertensive rats. The reduction of blood pressure was acute and substantial. The maximal effect on blood pressure was observed approximately 2 h after oral gavages. The reduction of blood pressure was accompanied by an acute, dose-dependent increase in heart rate, presumably due to the activation of baroreflex mechanism[1]. ROCK inhibition with the use of GSK 269962 in the 10 mg/kg dose, in turn, triggered an increase in VV(voided volume), PVR(post-void residual), VT(volume threshold), VE(voiding efficiency), ICI(intercontraction interval), BC(bladder compliance), and VTNVC(volume threshold to elicit NVC). The inhibition of the ROCK pathway through GSK 269962 appeared to have no effect on either HR(heart rate), SBP(systolic blood pressure), MBP(systolic blood pressure), or DBP(diastolic blood pressure)[2]. NVC:nonvoiding contractions.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human primary smooth muscle cells
濃度 3 μM
反応時間 150 min
実験の流れ Human primary smooth muscle cells were serum-starved(cells were grown on coverslips, and at approximately 50% confluence, they were serum-starved overnight) and stimulated with AngII (100 nM) for 2 h. ROCK inhibitors (3 μM for SB-772077-B or GSK269962A) were added 30 min before AngII stimulation, and cells were fixed and stained with rhodamine phalloidin. Confocal images of actin stain were obtained.
動物実験 動物モデル female Wistar rats
投薬量 5 or 10 mg/kg
投与方法 intra-arterially

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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Periodic propagating waves coordinate RhoGTPase network dynamics at the leading and trailing edges during cell migration [ Elife, 2020, 9:e58165] PubMed: 32705984
Dissecting heterogeneity in malignant pleural mesothelioma through histo-molecular gradients for clinical applications. [ Nat Commun, 2019, 10(1):1333] PubMed: 30902996
B. anthracis Lethal Toxin but not Edema Toxin, Increases Pulmonary Artery Pressure and Permeability in Isolated Perfused Rat Lungs [Cui X Am J Physiol Heart Circ Physiol, 2019, 10.1152/ajpheart.00685.2018] PubMed: 30767685
CTGF/VEGFA-activated Fibroblasts Promote Tumor Migration Through Micro-environmental Modulation [ Mol Cell Proteomics, 2018, 17(8):1502-1514] PubMed: 29669735

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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