SGLT2 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
s5566 Dapagliflozin propanediol monohydrate

Dapagliflozin propanediol belongs to the class of orally administered antidiabetic agents designated as sodiumglucose cotransporter 2 (SGLT2) inhibitors.

Selective
S5413 Ertugliflozin

Ertugliflozin (MK-8835, PF-04971729) is a potent and selective sodium-dependent glucose cotransporter 2 inhibitor with IC50 values of 0.877 nM for h-SGLT2 and 1000-fold higher for h-SGLT1.

Selective hSGLT2, IC50: 0.877 nM
S4431 Ertugliflozin L-pyroglutamic acid

Ertugliflozin (MK-8835, PF-04971729) L-pyroglutamic acid is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2) with IC50 of 0.877 nM for h-SGLT2. Ertugliflozin has the potential for the treatment of type 2 diabetes mellitus.

Selective h-SGLT2, IC50: 0.877 nM
S1548 Dapagliflozin (BMS-512148)

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。

Selective hSGLT2, EC50: 1.1 nM
S8103 Sotagliflozin (LX4211)

Sotagliflozin (LX4211)是一种口服的双重SGLT1/SGLT2抑制剂,IC50分别为 36 nM 和 1.8 nM。Phase 3。

Selective SGLT2, IC50: 1.8 nM
S5901 Canagliflozin hemihydrate

Canagliflozin hemihydrate is the hemihydrate form of canagliflozin, which is a SGLT2 inhibitor with IC50 of 2.2 nM for hSGLT2 in a cell-free assay, exhibits 413-fold selectivity over hSGLT1.

Selective mSGLT2, IC50: 2 nM; hSGLT2, IC50: 4.4 nM
S2760 Canagliflozin (JNJ 28431754)

Canagliflozin是一种高效的,选择性SGLT2抑制剂,作用于hSGLT2,无细胞试验中IC50为2.2 nM,比作用于hSGLT1选择性高413倍。

Selective mSGLT2, IC50: 2 nM; hSGLT2, IC50: 4.4 nM; rSGLT2, IC50: 3.7 nM
S8558 Tofogliflozin(CSG 452)

Tofogliflozin是一种新型的sodium-glucose co-transporter 2(SGLT2)抑制剂,对hSGLT2和hSGLT1的IC50值分别为2.9 nM和8444 nM。

Selective hSGLT2, IC50: 2.9 nM
S8022 Empagliflozin (BI 10773)

Empagliflozin (BI 10773)是一种有效的,选择性SGLT-2抑制剂,IC50为3.1 nM,比作用于SGLT-1, 4, 5和6选择性高300倍以上。Phase 3。

Selective SGLT2, IC50: 3.1 nM
S0994 Ipragliflozin L-Proline

Ipragliflozin L-Proline is an orally active and selective inhibitor of SGLT2 with IC50 of 7.38 nM, 6.73 nM and 5.64 nM for human SGLT2, rat SGLT2 and mouse SGLT2, respectively.

Selective human SGLT2, IC50: 7.38 nM; rat SGLT2, IC50: 6.73 nM; mouse SGLT2, IC50: 5.64 nM
S8637 Ipragliflozin (ASP1941)

Ipragliflozin (ASP1941)是一种高度选择性的sodium-glucose cotransporter 2 (SGLT2)抑制剂,对hSGLT2的IC50值为7.4 nM,对SGLT2的选择性是对SGLT1的选择性的254倍。

Selective hSGLT2, IC50: 7.4 nM; rat SGLT2, IC50: 6.73 nM; mouse SGLT2, IC50: 5.64 nM
S0993 Remogliflozin etabonate (GSK189075)

Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity inhibitor of sodium glucose cotransporter (SGLT2) with Ki of 1950 nM, 2140 nM, 43100 nM, 8570 nM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.

Selective rSGLT2, Ki: 2140 nM; hSGLT2, Ki: 1950 nM
S2343 Phlorizin

Phlorizin 是有毒的2'-葡萄糖苷根皮素,属于二氢查尔酮,是一种黄酮类化合物。

Pan hSGLT2, Ki: 39 nM
S2342 Phloretin (RJC 02792)

Phloretin 是一种二氢查尔酮,含有多元酚。

Pan