Dapagliflozin
别名: BMS-512148 中文名称：达格列净
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Dapagliflozin是一种有效的，选择性的hSGLT2抑制剂，EC50为1.1 nM，比作用于hSGLT1选择性高1200倍。Phase 4。
Dapagliflozin Chemical Structure
CAS: 461432-26-8
客户使用Selleck的Dapagliflozin发表文献36篇
产品质控
相关信号通路图
SGLT抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HEK293.ETN cells | Function assay | 1.5 h | Inhibition of human SGLT2 transfected in HEK293.ETN cells assessed as AMG uptake after 1.5 hrs by scintillation counting, IC50=0.0067 μM | 19896374 | |
| CHOK1 cells | Function assay | 3 h | Inhibition of human SGLT2 expressed in CHOK1 cells assessed as inhibition of [14C]-AMG uptake after 3 hrs by microbeta scintillation counting analysis, IC50=0.001 μM | 24842618 | |
| CHO cells | Function assay | 2 h | Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50=0.00049 μM | 20434909 | |
| COS-7 cells | Function assay | 2 h | Inhibition of human SGLT1 transfected in COS-7 cells assessed as AMG uptake after 2 hrs by scintillation counting, IC50=0.89 μM | 19896374 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent methyl-alpha-D-[U-14C]glucopyranoside uptake after 2 hrs, IC50 = 0.0014 μM. | 20149653 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent methyl-alpha-D-[U-14C]glucopyranoside uptake after 2 hrs, IC50 = 1.2 μM. | 20149653 | |
| HEK293 | Function assay | 1.5 hrs | Inhibition of human SGLT2 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 1.5 hrs by liquid scintillation counting, IC50 = 0.0067 μM. | 20576578 | |
| COS7 | Function assay | 2 hrs | Inhibition of human SGLT1 expressed in african green monkey COS7 cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50 = 0.89 μM. | 20576578 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, EC50 = 0.003 μM. | 21128592 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT1 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, EC50 = 0.4285 μM. | 21128592 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50 = 0.00049 μM. | 21193308 | |
| CHO | Function assay | 60 mins | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting, IC50 = 0.004 μM. | 21398124 | |
| CHO | Function assay | 60 mins | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting in presence of 100% plasma, IC50 = 0.022 μM. | 21398124 | |
| CHO | Function assay | 60 mins | Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting, IC50 = 0.37 μM. | 21398124 | |
| CHO | Function assay | 60 mins | Inhibition of SGLT6 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting, IC50 = 0.38 μM. | 21398124 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counter, IC50 = 0.00049 μM. | 21514014 | |
| CHO | Function assay | 60 mins | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-Glucose uptake using [14C]-methyl glucopyranoside after 60 mins by microbeta plate counting, IC50 = 0.003 μM. | 21565497 | |
| COS7 | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in african green monkey COS7 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 2 hrs by scintillation counting in presence of 25 % human plasma, IC50 = 0.0032 μM. | 21737266 | |
| 293 | Function assay | 1.5 hrs | Inhibition of human SGLT1 expressed in human 293 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 1.5 hrs by scintillation counting in presence of 25 % human plasma, IC50 = 3.1 μM. | 21737266 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in CHO cells assessed as reduction of [14C]-labeled AMG after 2 hrs by liquid scintillation counting, IC50 = 0.00135 μM. | 21868239 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50 = 0.00049 μM. | 21906953 | |
| CHO-K1 | Function assay | 120 mins | Inhibition of human SGLT2 expressed in CHO-K1 cells incubated for 120 mins at 37 degC by [14C]-AMG uptake assay, EC50 = 0.0024 μM. | 22818040 | |
| CHO-K1 | Function assay | 120 mins | Inhibition of human SGLT1 expressed in CHO-K1 cells incubated for 120 mins at 37 degC by [14C]-AMG uptake assay, EC50 = 0.593 μM. | 22818040 | |
| CHO | Function assay | 45 mins | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins, IC50 = 0.0013 μM. | 22889351 | |
| CHO | Function assay | 45 mins | Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins, IC50 = 0.8 μM. | 22889351 | |
| CHOK1 | Function assay | 3 hrs | Inhibition of human SGLT1 expressed in CHOK1 cells assessed as inhibition of [14C]-AMG uptake after 3 hrs by microbeta scintillation counting analysis, IC50 = 0.891 μM. | 24842618 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50 = 0.00049 μM. | 24900297 | |
| CHO | Function assay | 2 hrs | Competitive inhibition of full-length human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by scintillation counting, IC50 = 0.005 μM. | 25650254 | |
| CHO | Function assay | 120 mins | Inhibition of human SGLT2 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method, IC50 = 0.0015 μM. | 28447791 | |
| CHO | Function assay | 120 mins | Inhibition of human SGLT1 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method, IC50 = 0.629 μM. | 28447791 | |
| CHO | Function assay | 1 hr | Inhibition of human SGLT2 expressed in CHO cells assessed as reduction in [14C]AMG uptake after 1 hr by microbeta counting method, EC50 = 0.002 μM. | 29216560 | |
| CHO | Function assay | 1 hr | Inhibition of human SGLT1 expressed in CHO cells assessed as reduction in [14C]AMG uptake after 1 hr by microbeta counting method, EC50 = 0.86 μM. | 29216560 | |
| CHO | Function assay | 1 hr | Inhibition of full-length human SGLT2 expressed in CHO cells assessed as decrease in [14C]-methyl alpha-D-glucopyranoside uptake after 1 hr by liquid scintillation counting method, IC50 = 0.00105 μM. | 29764742 | |
| HEK293 | Function assay | 10 mins | Inhibition of human SGLT2 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake preincubated for 10 mins followed by [14C]-AMG addition and measured after 2 hrs by liquid scintillation counting method, IC50 = 0.0014 μM. | 29954682 | |
| HEK293 | Function assay | 10 mins | Inhibition of human SGLT1 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake preincubated for 10 mins followed by [14C]-AMG addition and measured after 2 hrs by liquid scintillation counting method, IC50 = 1.83 μM. | 29954682 | |
| CHO | Function assay | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation, EC50 = 0.0011 μM. | 18260618 | ||
| CHO | Function assay | Inhibition of rat SGLT2 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation, EC50 = 0.003 μM. | 18260618 | ||
| CHO | Function assay | Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation, EC50 = 1.39 μM. | 18260618 | ||
| HEK293.ETN | Function assay | Inhibition of human SGLT2 expressed in HEK293.ETN cells assessed as methyl-alpha-D-[U-14C]glucopyranoside uptake by scintillation counting, IC50 = 0.0067 μM. | 19700318 | ||
| COS7 | Function assay | Inhibition of human SGLT1 expressed in african green monkey COS7 cells assessed as methyl-alpha-D-[U-14C]glucopyranoside uptake by scintillation counting, IC50 = 0.885 μM. | 19700318 | ||
| HEK293 | Function assay | Inhibition of human SGLT1 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methylglucopyranoside uptake, IC50 = 0.81 μM. | 19785435 | ||
| CHO | Function assay | Inhibition of human recombinant SGLT2 expressed in CHO cells by liquid scintillation counting, IC50 = 0.00049 μM. | 20181486 | ||
| CHO | Function assay | Inhibition of human SGLT2 expressed in CHO cells using methyl-alpha-D-glucopyranoside by liquid scintillation counting, IC50 = 0.00135 μM. | 21592794 | ||
| CHO-K1 | Function assay | Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay, IC50 = 0.0013 μM. | 22652255 | ||
| CHO-K1 | Function assay | Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay, IC50 = 0.8 μM. | 22652255 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Dapagliflozin是一种有效的，选择性的hSGLT2抑制剂，EC50为1.1 nM，比作用于hSGLT1选择性高1200倍。Phase 4。 | ||
|---|---|---|---|
| 特性 | Dapagliflozin是第一类刺激血糖的药物，作用于正常大鼠比其他SGLT2抑制剂更有效。 | ||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Dapagliflozin对hSGLT1不敏感，IC50是hSGLT2的1200倍。[1] Dapagliflozin作用于hSGLT2比Phlorizin效果高32倍。作用于hSGLT1比Phlorizin效果低4倍。Dapagliflozin高度选择性抗GLUT转运蛋白，20 μM Dapagliflozin在无蛋白buffer中抑制达8-9%，在4%牛血清蛋白存在时没有抑制效果。[2] Dapagliflozin可渗透Caco-2 细胞膜，可作为P-糖蛋白（P-gp）底物，但不是P-gp抑制剂。10 μM Dapagliflozin稳定作用于大鼠，犬，猴，人类血清。Dapagliflozin作用于人类P450酶，没有抑制反应，也没有诱导。Dapagliflozin在体外代谢通路中可参与糖脂化，羟乙基化，脱乙基作用。[3] |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | HIF-1α / p-AMPK / AMPK / p-ERK / ERK / β-actin DDR1 HIF-1α / PHD2 / tubulin p-elf2α / t-elf2α / tubulin-α Bax / Bcl2 / PARP / β-actin |
|
27391020 | |
| Growth inhibition assay | Tumor volume |
|
28763435 | |
| IHC | TUNEL-positive cells HIF1 TUNEL-positive cells mice kidney sections HE staining / SGLT2 |
|
27391020 | |
| Immunofluorescence | Metabolic switch in diabetic kidneys F-actin EdU PECAM-1 / α-SMA podocytes |
|
32444604 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 |
Dapagliflozin按 0.1 mg/kg剂量口服给药高血糖 链脲佐菌素(STZ)大鼠，降低血糖水平，降低达55%，归因于与糖链相关的代谢稳定。 Dapagliflozin具有很好的吸收，分布，代谢，排泄 (ADME) 谱，且具有口服生物有效性。[1] Dapagliflozin 按1 mg/kg 剂量作用于正常大鼠，处理24小时，造成明显糖尿，这种作用存在剂量依赖性，且提高尿量。Dapagliflozin 作用于Zucker 糖尿病肥胖(ZDF)大鼠，处理6小时后，诱导 尿糖和尿量分泌升高。Dapagliflozin 处理ZDF大鼠，2周后，快速降低葡萄糖水平, 且不会对肾脏和肝脏造成毒性。[2] Dapagliflozin 明显缓解多糖症病情发展, 使血糖水平降低。Dapagliflozin 可提高胰岛素敏感性,降低β细胞质量和修复的胰腺功能。[4] |
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|---|---|---|
| 动物实验 | Animal Models | 正常Sprague Dawley大鼠或链脲佐菌素诱导的雄性Sprague Dawley大鼠 |
| Dosages | 0.01-10 mg/kg (1 mL/kg) | |
| Administration | 口服处理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06012266 | Not yet recruiting | Heart Failure |
Centre Hospitalier Universitaire Vaudois|Great Ormond Street Hospital for Children NHS Foundation Trust|University College London |
January 2024 | Phase 2 |
| NCT06000462 | Not yet recruiting | Obesity|Dapagliflozin Adverse Reaction|Weight Loss|Effect of Drug |
Oman Ministry of Health |
December 2023 | Phase 2|Phase 3 |
| NCT04887935 | Not yet recruiting | Prostate Cancer|Cancer of Prostate |
Washington University School of Medicine |
December 31 2023 | Phase 1 |
| NCT06165601 | Not yet recruiting | Chronic Kidney Diseases |
University Hospital Montpellier |
December 1 2023 | Not Applicable |
化学信息&溶解度
| 分子量 | 408.87 | 分子式 | C21H25ClO6 |
| CAS号 | 461432-26-8 | SDF | Download Dapagliflozin SDF |
| Smiles | CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)C3C(C(C(C(O3)CO)O)O)O)Cl | ||
| 储存条件(自收到货起) | 3年 -20°C 粉末（密封） | ||
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体外溶解度 |
DMSO : 100 mg/mL ( (244.57 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 100 mg/mL Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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