| CAS NO: | 461432-26-8 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 25mg | 电议 |
| 100mg | 电议 |
| Physical Appearance | A yellow oil |
| Storage | Store at -20°C |
| M.Wt | 408.87 |
| Cas No. | 461432-26-8 |
| Formula | C21H25ClO6 |
| Solubility | insoluble in H2O; ≥116.6 mg/mL in EtOH; ≥15.1 mg/mL in DMSO |
| Chemical Name | (2S,3R,4R,5S,6R)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol |
| Canonical SMILES | CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)C3C(C(C(C(O3)CO)O)O)O)Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
hSGLT2的EC50值：1.1±0.06 nM
SGLT2的选择性抑制作用能防止肾对糖再吸收的过程以及促进葡萄糖经尿液排出，已被提出用于帮助糖尿病患者恢复正常的血浆葡萄糖水平。Dapagliflozin是一种有效的和选择性的肾钠-葡萄糖协同转运蛋白2（SGLT2）抑制剂。
体外：Dapagliflozin对hSGLT2和hSGLT1的EC50值分别为1.1 nM和1.4 μM，对SGLT2比对SGLT1的选择性高1200倍，而Phlorizin对两者的选择性只有10倍。Dapagliflozin对大鼠SGLT（rSGLT）2和hSGLT2的抑制能力相当，但Dapagliflozin对rSGLT2的选择性比对rSGLT1的降低至200倍[1]。
体内：对于体内实验，给予大鼠0.1 ~ 1.0 mg/kg的单次口服剂量后，Dapagliflozin显著引起糖尿病和正常大鼠的肾葡萄糖排泄，改善正常大鼠的葡萄糖耐受性以及缓解Zucker糖尿病肥胖大鼠的高血糖[2]。
临床试验：Dapagliflozin以1、2.5和5 mg/天的剂量可有效地减少未经治疗II型糖尿病患者的血糖水平和体重。Dapagliflozin的耐受性良好[3]。
参考文献：
[1] Meng W, Ellsworth BA, Nirschl AA, McCann PJ, Patel M, Girotra RN, Wu G, Sher PM, Morrison EP, Biller SA, Zahler R, Deshpande PP, Pullockaran A, Hagan DL, Morgan N, Taylor JR, Obermeier MT, Humphreys WG, Khanna A, Discenza L, Robertson JG, Wang A, Han S, Wetterau JR, Janovitz EB, Flint OP, Whaley JM, Washburn WN. Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes. J Med Chem. 2008 Mar 13; 51(5):1145-9.
[2] Han S, Hagan DL, Taylor JR, Xin L, Meng W, Biller SA, Wetterau JR, Washburn WN, Whaley JM. Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats. Diabetes. 2008 Jun; 57(6):1723-9.
[3] Bailey CJ, Iqbal N, T'joen C, List JF. Dapagliflozin monotherapy in drug-nave patients with diabetes: a randomized-controlled trial of low-dose range. Diabetes Obes Metab. 2012 Oct; 14(10):951-9.
| Cell experiment:[1] | |
Cell lines | Chinese hamster ovary cells stably expressing human SGLT2 and SGLT1 |
Reaction Conditions | 1.1 nM (EC50) |
Applications | Dapagliflozin inhibited accumulation of radiolabeled α-methyl-D-glucopyranoside, with EC50 values of 1.1 nM for human SGLT2 (hSGLT2) and 1.4 μM for hSGLT1. |
| Animal experiment:[1] | |
Animal models | Sprague-Dawley rats |
Dosage form | 0.1, 1.0, and 10 mg/kg Administered orally |
Applications | In normal rats, a single oral dose of 0.1, 1.0, and 10 mg/kg of dapagliflozin induced respective losses of 550, 1100, and 1900 mg of glucose per 200 g of body weight over 24 h. In streptozotocin-induced diabetic rats, a single oral dose of 0.1 mg/kg of dapagliflozin resulted in a 55% reduction in blood glucose level. The above correlation of SGLT2 inhibition, glucosuria, and blood glucose-lowering effects suggest that selective SGLT2 inhibition by dapagliflozin holds promise as a viable approach to treat type 2 diabetes. |
Note | The technical data provided above is for reference only. |
References: 1. Meng W, Ellsworth BA, Nirschl AA, et al. Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes. Journal of Medicinal Chemistry, 2008, 51(5): 1145-1149. | |
| 描述 | Dapagliflozin是一种有效的和选择性的hSGLT2抑制剂，EC50值为1.1 nM，比对hSGLT1的选择性高1200倍。 | |||||
| 靶点 | hSGLT2 | |||||
| IC50 | 1.1 nM (EC50) | |||||
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