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{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_am, item.pr_size) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} | 现货 | 咨询 | - + |
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免费溶解
产品名称 | SGLT1 ↓ ↑ | SGLT2 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Phloretin | ✔ | 98% | |||||||||||||||||
Canagliflozin |
+++
hSGLT2, IC50: 3.7 nM mSGLT2, IC50: 2 nM |
95% | |||||||||||||||||
Empagliflozin |
++
SGLT2, IC50: 3.1 nM |
98% | |||||||||||||||||
Dapagliflozin |
++++
hSGLT2, EC50: 1.1 nM |
97% | |||||||||||||||||
Tofogliflozin (hydrate) |
+++
hSGLT2, IC50: 2.9 nM |
99%+ | |||||||||||||||||
Sotagliflozin |
+
SGLT1, IC50: 36 nM |
++++
SGLT2, IC50: 1.8 nM |
98% | ||||||||||||||||
Ipragliflozin |
++
hSGLT2, IC50: 7.4 nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | KGA-2727 stands as the first selective, potent, and orally active inhibitor of SGLT1, with Ki values of 97.4 nM for humans and 43.5 nM for rats. Its selectivity ratios (Ki for SGLT2/Ki for SGLT1) reach 140 for humans and 390 for rats, showcasing antidiabetic effectiveness[1]. |
体内研究 | In oral glucose tolerance tests on streptozotocin-induced diabetic rats, KGA-2727 mitigates the spike in plasma glucose following glucose ingestion, suggesting it enhances control over postprandial hyperglycemia[1]. In Zucker diabetic fatty (ZDF) rats, chronic treatment with KGA-2727 decreases plasma glucose and glycated hemoglobin levels. Additionally, KGA-2727 maintains glucose-stimulated insulin secretion, lowers urinary glucose output, and enhances the morphology of pancreatic islets and renal distal tubules in ZDF rats[1]. |
体外研究 | A Dixon plot analysis of KGA-2727 reveals linear inhibition for both human SGLT1 and SGLT2, indicating that KGA-2727 blocks these transporters competitively. It dose-dependently reduces Methyl-D-glucopyranoside (AMG) absorption via SGLT1 and SGLT2[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.86mL 0.37mL 0.19mL |
9.32mL 1.86mL 0.93mL |
18.64mL 3.73mL 1.86mL |
CAS号 | 666842-36-0 |
分子式 | C26H40N4O8 |
分子量 | 536.618 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 190 mg/mL(354.07 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 20 mg/mL(37.27 mM),配合低频超声,并水浴加热至45℃助溶 无水乙醇: 100 mg/mL(186.35 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 |
动物实验配方 |