sglt2

Empagliflozin (BI 10773) is an SGLT-2 inhibitor (IC50=3.1 nM) that is potent and selective, with more than 300-fold selectivity for SGLT-1 4 5 6. Empagliflozin is used for the treatment of type 2 diabetes.

Canagliflozin (JNJ 28431754AAA) is a selective SGLT2 inhibitor that inhibits CHO cells expressing mSGLT2, rSGLT2, and hSGLT2 (IC50=2 3.7 4.4 nM). Canagliflozin can be used for the treatment of type II diabetes mellitus (T2DM).

Dapagliflozin ((2S)-1,2-propanediol, hydrate) (BMS-512148 (2S)-1,2-propanediol, hydrate) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2), in development for treating type 2 diabetes mellitus (T2DM). It inhibits SGLT2, responsible for at least 90% of glucose reabsorption in the kidney.

Dapagliflozin (BMS-512148) is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

Ipragliflozin (ASP1941) is under investigation in Type 2 Diabetes and Diabetes Mellitus, Type 2.

PF-04971729 (Ertugliflozin (PF-04971729)) is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2).

Phlorizin (Phloridzin) is a non-selective SGLT inhibitor found in apple, for hSGLT1( Ki=300 nM) and hSGLT2( Ki=39 nM) .

Sotagliflozin (LP-802034) is an orally bioavailable inhibitor of the sodium-glucose co-transporter subtype 1 (SGLT1) and 2 (SGLT2), with potential antihyperglycemic activity.

Sergliflozin etabonate (KGT-1251) is an inhibitor of SGLT2 and can be used in studies about type 2 diabetes and obesity.

T-1095 is an inhibitor of renal glucose reabsorption and the expression of Na+-glucose cotransporters (SGLTs) and facilitative glucose transporter 2 (GLUT2).

Licogliflozin (LIK066) is an inhibitor of sodium-glucose cotransporter (SGLT1 and SGLT2).

Sergliflozin A is a selective SGLT2 inhibitor that induces diabetes in a dose-dependent manner. It reduces hyperglycemia.

SGLT1/2-IN-2 is a chemical compound with robust dual inhibitory properties, exhibiting potent activities against SGLT1 (IC50 = 96 nM) and SGLT2 (IC50 = 1.3 nM).

Canagliflozin D4 is a deuterium-labeled Canagliflozin. Canagliflozin is an SGLT2 inhibitor.

Tofogliflozin is a highly specific inhibitor of sodium/glucose cotransporter 2 (SGLT2) (Kis: 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2. IC50s: 2.9/14.9/6.4 nM (human/rat/mouse SGLT2)).

Mizagliflozin (GSK-1614235 free base) is a sodium-glucose transporter inhibitor( Ki of 27 nM for human SGLT1). Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic drug that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation.

Dapagliflozin-13C6 (glucitol-13C6) is the 13C labeled compound of Dapagliflozin. Dapagliflozin has a CAS number of 461432-26-8. Dapagliflozin is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

Kushenol X exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2).

Remogliflozin etabonate (GSK189075A) is a prodrug of regaliflozin and an inhibitor SGLT2 with Ki values of 1.95, 2.14, 8.57, and 43.1μM for hSGLT2, rSGLT2, rSGLT1, and hSGLT1, respectively.

Kushenol A is a kind of Adenosine 3', 5'-cyclic monophosphate(cAMP)phosphodiesterase inhibitiors, it shows selective alpha-glucosidase inhibitory activity. Kushenol A and kushenol C exhibit inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2).

Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) is a selective and orally active hSGLT2 inhibitor with an IC50 of 0.877 nM, suitable for studies on the treatment of type 2 diabetes mellitus.

SGL5213 is an oral active and low-absorbable inhibitor of sodium-dependent glucose cotransporter 1 (SGLT1)(hSGLT1 and hSGLT2 with IC50 values of 29 nM and 20 nM , respectively),and has potential to treat type 2 diabetes.

Bexagliflozin (EGT1442) is a potent, selective sodium glucose co-transporter 2 (SGLT2) inhibitor with IC50 values of 2 nM for human SGLT2 and 5.6 μM for human SGLT1.

Henagliflozin (SHR3824) is an effective, oral, and selective SGLT2 inhibitor that effectively inhibits human SGLT2 in vitro, but has very weak inhibitory effects on human SGLT1.

Velagliflozin proline hydrate, the clinical form of Velagliflozin, is an oral sodium-glucose cotransporter 2 (SGLT2) inhibitor exhibiting antidiabetic activity. By decreasing renal glucose reabsorption and promoting glycosuria, it effectively reduces blood sugar and insulin levels [1].

Luseogliflozin (TS 071) hydrate, a second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor, exhibits selective potency and oral activity, with an IC50 of 2.26 nM. This compound is utilized in research for the treatment of type 2 diabetes mellitus (T2DM).

Dapagliflozin-3-O-β-D-glucuronide is a metabolite of dapagliflozin . Dapagliflozin is a first generation selective sodium glucose cotransporter (SGLT) 2 inhibitor that blocks glucose transport.[1] Dapagliflozin is metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A9 to dapagliflozin-3-O-β-D-glucuronide, which is 2,600-fold less potent than the parent compound with regard to SGLT2 inhibition.[2]

SGLT inhibitor-1 is a potentsodium glucose co-transporter proteins (SGLTs) dual inhibitor(hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively).

Luseogliflozin, a potent and competitive inhibitor of sodium-dependent glucose cotransporter 2 (SGLT2), competitively inhibits human SGLT2-mediated glucose uptake with a Ki value of 1.10 nM.

HSK0935 is a highly selective and orally available SGLT2 inhibitor (IC50: 1.3 nM). It has antihyperglycemic activities.

YM-543, also known as ASP-543, is a selective SGLT2 inhibitor. Sodium-glucose cotransporter 2 (SGLT2) is a specifically expressed transporter in the kidney that plays an important role in renal glucose reabsorption, and its inhibition may present a novel therapeutic strategy for treating diabetes. YM543 potently and selectively inhibited mouse and human SGLT2 activities at nanomolar ranges. In vivo single oral administration of YM543 dose-dependently and significantly reduced blood glucose levels and improved glucose tolerance with a concomitant increase in urinary glucose excretion in KK/Ay type 2 diabetic mice, effects that were sustained even after 12 h.

Kushenol C is a good 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenger, and it exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2). Kushenol C shows antimicrobial activity against Staphylococcus aureus and Streptococcus mutan

Remogliflozin is an effective sodium-glucose transporter 2 inhibitor (Kis = 12.4 and 26 nM for human and rat SGLT2, respectively).

BMS-639432 is a potent sodium-glucose cotransporter type II (SGLT2) inhibitor.

SGLT1 2-IN-1 is a dual inhibitor of SGLT1 and SGLT2.

KGA-2727 is a potent and selective SGLT1 inhibitor, with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2 Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 for the treatment of diabete.

LX2761 is a chemically stable and effective inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 (IC50s: 2.2 nM and 2.7nM for hSGLT1 and hSGLT2). However, it shows specific SGLT1 inhibition in the gastrointestinal (GI) tract.

TA-1887 is a new type of selective inhibitor of sglt2 for the treatment of type 2 diabetes. It has a significant hypoglycemic effect in KK (HF-KK) mice fed a high-fat diet. TA-1887 has good pharmacokinetic characteristics and significantly increases UGE

Kushenol I is a GABAA receptor modulator, it exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2).Kushenol I is shown to be active against the plant pathogenic fungus Cladosporium cucumerinum.

Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific inhibitor of SGLT2, with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2, respectively.

Canagliflozin hemihydrate (TA 7284) is a drug of the gliflozin class or subtype 2 sodium-glucose transport inhibitors used for the treatment of type 2 diabetes. SGLT2 is responsible for at least 90% of renal glucose reabsorption (SGLT1 being responsible for the remaining 10%). Blocking this transporter causes up to 119 grams of blood glucose per day to be eliminated through the urine, corresponding to 476 kilocalories.

Ipragliflozin is a highly potent and selective SGLT2 inhibitor with an IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.

O-Desethyl Dapagliflozin (Empagliflozin-4) is a SGLT2 inhibitor, IC50=33nM.

Dapagliflozin D5 (BMS-512148 D5) is a deuterated form of Dapagliflozin, a competitive SGLT2 inhibitor.