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GPCR/G Protein

Melanin-concentrating Hormone Receptor (MCHR)

(11)

Melanocortin Receptor

Neuropeptide Y Receptor

Prostaglandin Receptor

(182)

Protease-activated Receptor

SGLT

Sodium-dependent glucose cotransporters (or sodium-glucose linked transporter, SGLT) are a family of glucose transporter found in the intestinal mucosa (enterocytes) of the small intestine (SGLT1) and the proximal tubule of the nephron (SGLT2 in PCT and SGLT1 in PST). They contribute to renal glucose reabsorption. In the kidneys, 100% of the filtered glucose in the glomerulus has to be reabsorbed along the nephron (98% in PCT, via SGLT2). If the plasma glucose concentration is too high (hyperglycemia), glucose is excreted in urine (glucosuria) because SGLT are saturated with the filtered glucose. Glucose is never secreted by a healthy nephron.

Filter HomeSignaling PathwaysGPCR/G ProteinSGLT

Canagliflozin

T1782842133-18-0

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).

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Sotagliflozin

T35471018899-04-1

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

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Empagliflozin

T1766864070-44-0

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.

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Dapagliflozin

T2389461432-26-8

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

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Enavogliflozin

T388431415472-28-4

Enavogliflozin (DWP-16001) is an orally available small molecule and sodium glucose transporter 2 inhibitor.

$158

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Remogliflozin etabonate

T34286442201-24-3

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.

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Bexagliflozin

T72171118567-05-7

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.

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Ertugliflozin

T49991210344-57-2

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

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Sergliflozin A

T68174360775-96-8In house

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

$112

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Mizagliflozin

T16083666843-10-3

Mizagliflozin is an orally active, selective SGLT1 inhibitor with a Ki value of 27 nM for human SGLT1. Mizagliflozin is 303 times more selective for SGLT1 than for SGLT2. Mizagliflozin is an anti-diabetic drug that can improve postprandial blood sugar fluctuations and may have the potential to improve chronic constipation.

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Ipragliflozin

T2385761423-87-4

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

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Tofogliflozin (hydrate)

T50161201913-82-7

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.

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Dapagliflozin ((2S)-1,2-propanediol, hydrate)

T4460960404-48-2

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.

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O-Desethyl Dapagliflozin

T67849864070-37-1

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

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KGA-2727

T15656666842-36-0

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.

$135

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T-1095

T9590209746-59-8

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

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Leachianone A

TN185697938-31-3

Leachianone A (Isokurarinone) is a potential antitoxic agent, it shows inhibitory effects on cadmium- Induced cytotoxicity.

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Canagliflozin hemihydrate

T1782L928672-86-0

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.

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Ertugliflozin L-pyroglutamic acid

T152441210344-83-4

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.

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Sergliflozin etabonate

T28757408504-26-7

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

$195

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SGL5213

T128921240305-17-2

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.

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10-14 weeks

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Licogliflozin

T157521291094-73-9In house

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

$862

6-8 weeks

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Picraline

TN47842671-32-1

A series of a hydroxy substituted derivatives 21-28 at C-17 of the Picraline-type alkaloids have been derived as having potent SGLT inhibitory activity.

$660

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LY2794193

T158072173037-97-1

LY2794193 is a highly effective and selective agonist of the mGlu3 receptor (hmGlu3 Ki=0.927 nM,EC50=0.47 nM; hmGlu2 Ki=412 nM,EC50=47.5 nM).

$523

10-14 weeks

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IRAK inhibitor 4 trans

T11671

IRAK inhibitor 4 is a compound that functions as an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4). It specifically targets and inhibits the activity of IRAK4. The (trans) form of IRAK inhibitor 4 refers to its specific molecular configuration.

$396

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Kushenol C

TN439999119-73-0

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

$1,329

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Velagliflozin

T17221946525-65-1

Velagliflozin is an orally available inhibitor of sodium-glucose cotransporter 2.

$2,120

8-10 weeks

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HSK0935

T155051638851-44-1

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

$1,420

6-8 weeks

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SGLT inhibitor-1

T128932247314-23-2

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).

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10-14 weeks

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