| 名称 | GW3965 hydrochloride |
| 描述 | GW3965 hydrochloride (GW3965 HCl) belongs to synthetic small molecules and is a liver X receptor (LXR) agonist (hLXRα EC50 = 190 nM; hLXRβ EC50 = 30 nM) with subtype selectivity, cell permeability, and oral activity. This compound is used in research related to metabolism, inflammation, and neuropathic pain. |
| 细胞实验 | Cells are seeded in 96 wells and are treated after 24 hours with different drugs indicated in each experiment in medium containing 1% FBS or lipoprotein deficient serum. Relative proliferation is determined using Cell Proliferation Assay Kit. Cells are incubated 1.5 hrs after adding tetrazolium salt WST-1 [2-(4-iodophenyl)-3- (4-nitrophenyl)-5-(2, 4-disulfo-phenyl)-2H-tetrazolium, monosodium salt] at 5% CO2, 37oC and the absorbance of the treated and untreated cells are measured using a microplate reader at 420 to 480 nm. Cells seeded in 12 well plates are counted using a hemocytometer, and dead cells are assessed using trypan blue exclusion assays. |
| 激酶实验 | Steady-state drug accumulation assay: AuxB1 and CHrB30 cells are grown to confluency in 12-well (24 mm) tissue culture dishes and the steady-state accumulation of [3H]-vinblastine is measured. Accumulation is initiated by the addition of 0.1 μ Ci [3H]-vinblastine and unlabelled vinblastine to a final concentration of 100 nM . The accumulation of [3H]-paclitaxel is measured using 0.1 μ Ci [3H]-paclitaxel and unlabelled drug to a final concentration of 1 μM . Cells are incubated in a reaction volume of 1 mL for 60 min at 37 ℃ under 5% CO2 in order to reach steady-state. The effect of the modulators XR9576 on [3H]-ligand accumulation is investigated in the concentration range 10-9 - 10-6 M. Modulators are added from a DMSO stock giving a final solvent concentration of 0.2 % (v/v). Following cell harvesting, accumulated drug is measured by liquid scintillation counting and normalized for cell protein content. Plots of amount accumulated as a function of modulator concentration are fitted with the general dose-response equation: Y={(a-b)/(1+(X/c)d)}+b Where: Y=response; a=initial response; b=final response; c=EC50 concentration; d=slope value; X=drug concentration. |
| 体外活性 | 方法：将脓毒症小鼠分离的脾脏髓源性抑制细胞（MDSCs）与1 μM GW3965 hydrochloride共孵育1小时，采用流式细胞术检测细胞凋亡。
结果：GW3965 hydrochloride可诱导脾脏MDSCs凋亡。[1]
方法：采用吉非替尼耐药的非小细胞肺癌PC9细胞，以5 μM GW3965 hydrochloride单独或联合吉非替尼处理48小时，通过MTT法检测细胞活力，Western blot检测自噬相关蛋白LC3 II/I及Beclin 1表达，AO染色观察自噬体形成，流式细胞术评估细胞凋亡。
结果：GW3965 hydrochloride联合吉非替尼较单药组协同抑制细胞活力，上调LC3 II/I比值及Beclin 1表达，增加自噬体积累及凋亡率。[2] |
| 体内活性 | 方法：采用胶原酶诱导脑出血小鼠模型，GW3965 hydrochloride以10 mg/kg剂量腹腔注射，溶于50% DMSO，术后1小时开始给药，每日一次，连续7天。
结果：GW3965 hydrochloride治疗组病灶体积减小、血肿清除加快、白质损伤减轻，并促进神经功能恢复。[3]
方法：采用盲肠结扎穿孔（CLP）诱导的脓毒症小鼠模型，GW3965 hydrochloride以3 mg/kg剂量皮下注射，溶于5% DMSO/30% PEG300/5% Tween 80/60% ddH₂O，于术后1、6、12、24、48、72小时共给药6次。
结果：GW3965 hydrochloride提高小鼠存活率，减轻多器官损伤，降低血清炎症因子水平。[4] |
| 存储条件 | Store at low temperature,Keep away from moisture
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 71.2 mg/mL (115.12 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.23 mM), Sonication is recommended.
Ethanol : 12.4 mg/mL (20.05 mM), Sonication is recommended.
|
| 关键字 | LXRα/SRC1 LiSA | LXR | LiverXReceptor | Liver X receptor | Inhibitor | inhibit | hLXRβ | hLXRα | GW-3965 hydrochloride | GW3965 Hydrochloride | GW-3965 | GW3965 | GW 3965 Hydrochloride | GW 3965 |
| 相关产品 | BMS-779788 | T0901317 | GW6340 | Rovazolac | SR 1903 | SR9238 | IMB-808 | Taraxasterol | BE1218 | SBI-477 | Saikosaponin A | DMHCA |
| 相关库 | 经典已知活性库 | 已知活性化合物库 | 转录因子库 | 代谢化合物库 | 抗菌活性库 | 抗感染化合物库 | 含氟化合物库 | 抗心血管疾病化合物库 | NO PAINS 化合物库 | 临床前化合物库 | 核受体化合物库 | 抗代谢疾病化合物库 |
