受注:045-509-1970 |
技術サポート:[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
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. |
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. |
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 |
|
Keratin isoform shifts modulate motility signals during wound healing [ bioRxiv, 2023, 2023.05.04.538989] | PubMed: 37205459 |
The Meningioma Enhancer Landscape Delineates Novel Subgroups and Drives Druggable Dependencies [ Cancer Discov, 2020, CD-20-0160] | PubMed: 32703768 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。