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- IG10501
- 2025年07月23日
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- 详细信息
- 技术资料
- 保存条件：
Stroe at -20℃，6 months.
- 保质期：
Stroe at -20℃，6 months.
- 英文名：
GW3965 Hydrochloride(10mM in DMSO,Sterile）
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
405911-17-3
- 规格：
1ml
| 基本信息 | |
| CAS | No.405911-17-3 |
| 英文名称 | GW3965 Hydrochloride(10mM in DMSO,Sterile） |
| 分子式 | C33H31ClF3NO3·HCl |
| 分子量 | 618.51 |
| 溶解性 | 请根据自己的实验要求使用。 |
| 外观(性状) | 无菌溶液 |
| 储存条件 | Stroe at -20℃，6 months. |
| 靶点 | Liver X Receptor（LXR） |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | GW3965 HCl是一种有效的，选择性LXR激动剂。 |
| 生物活性 | GW3965 hydrochloride is a potent and selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ， respectively.[1-4] |
| IC50 | EC50: 190 nM (hLXRα)， 30 nM (hLXRβ)[4] |
| In Vitro | GW3965 hydrochloride promotes GBM cell death?in vitro?with enhanced efficacy in EGFRvIII-expressing tumor cells. GW3965 hydrochloride up-regulates expression of the cholesterol transporter gene ABCA1 and the E3 ubiquitin ligase IDOL and reduces LDLR levels[2]. LXR ligands inhibits platelet aggregation and calcium mobilization stimulated by collagen or CRP. GW3965 hydrochloride (1 or 5 μM) displays a minor inhibitory effect on fibrinogen binding and P-selectin exposure， when platelets are stimulated with 1 μg/mL CRP. But using higher concentrations of GW3965 hydrochloride (10 μM) or T0901317 (40 μM)， the levels of fibrinogen and P-selectin on the platelet surface are reduced[3]. |
| 细胞实验 | GW3965 hydrochloride induces an increase of neuroactive steroids in the spinal cord， the cerebellum and the cerebral cortex of STZ-rats， but not in the CNS of non-pathological animals. GW3965 hydrochloride treatment induces an increase of dihydroprogesterone in the spinal cord of diabetic animals in association with an increase of myelin basic protein expression[1]. GW3965 hydrochloride (40 mg/kg， p.o.) strongly induces ABCA1 expression and reduces LDLR expression， and this is accompanied by 59% inhibition of tumor growth， and a 25-fold increase in GBM cell apoptosis in vivo[2]. GW3965 hydrochloride (2 mg/kg， i.v.) increases bleeding time and modulated platelet thrombus formation in vivo[3]. |
| 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.[1-4] |
| 动物实验 | Diabetes is induced in two-month-old male rats by a single i.p. injection of freshly prepared STZ (65?mg/kg) in 0.09?M citrate buffer， pH 4.8. Control animals are injected with 0.09 mol/L citrate buffer at pH 4.8. Hyperglycemia is confirmed 48 h after streptozotocin injection by measuring tail vein blood glucose levels using a glucometer OneTouch Ultra2. Only animals with mean plasma glucose levels over 300 mg/mL are classified as diabetic. Glycemia is also assessed before treatment with Ro5-4864 or GW3965 hydrochloride and before death. Two months after STZ injection， diabetic animals are treated once a week with Ro5-4864 (3 mg/kg) or GW3965 hydrochloride (50 mg/kg). Thus， they receive four subcutaneous injections in a month. Control diabetic rats receive 200 μL of vehicle (sesame oil). Four-month-old non-diabetic male rats are injected， following the same experimental schedule， with Ro5-4864， GW3965 hydrochloride or vehicle. Rats are killed 24?h after the last treatment.[1-4] |
| 数据来源文献 | [1]. Mitro， Nico.， et al. LXR and TSPO as new therapeutic targets to increase the levels of neuroactive steroids in the central nervous system of diabetic animals. Neurochemistry International (2012)， 60(6)， 616-621. [2]. Guo， Deliang.， et al. An LXR Agonist Promotes Glioblastoma Cell Death through Inhibition of an EGFR/AKT/SREBP-1/LDLR-Dependent Pathway. Cancer Discovery (2011)， 1(5)， 442-456. [3]. Spyridon， Michael.， et al. LXR as a novel antithrombotic target. Blood (2011)， 117(21)， 5751-5761. [4]. Collins JL， et al. Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. J Med Chem. 2002 May 9;45(10):1963-6. |
| 单位 | 瓶 |
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IG10501 GW3965 Hydrochloride(10mM in DMSO,Sterile） 代谢酶/蛋白酶 索莱宝
￥1300
