glucose transporter

BAY-876 is an orally active, selective inhibitor of glucose transporter 1 (GLUT1, IC50= 2 nM), exhibiting over 130-fold greater selectivity for GLUT1 than GLUT2, GLUT3, and GLUT4. It also inhibits glycolytic metabolism and ovarian cancer growth.

WZB117 is a Glucose Transporter 1 (GLUT1) inhibitor. when IC50 of WZB117 approximate 10 μM, it inhibits lung cancer A549 cells and breast cancer MCF7 cells proliferation.

KL-11743 specifically blocks glucose metabolism, triggering an acute collapse in NADH pools and a striking accumulation of aspartate, indicating a dramatic shift toward oxidative phosphorylation in the mitochondria.

STF-31 is an inhibitor of glucose transporter 1 (GLUT1) with IC50 of 1 μM.

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

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

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.

Phloretin (NSC-407292) is a well-known inhibitor of eukaryotic urea transporters, blocks VacA-mediated urea and ion transport. Phloretin is a dihydrochalcone, a type of natural phenols. It can be found in apple tree leaves and the Manchurian apricot. It promotes potent antioxidative activities in peroxynitrite scavenging and the inhibition of lipid peroxidation. It has been found to inhibit the growth of several cancer cells and induce apoptosis of B16 melanoma and HL60 human leukemia cells.

Rhoifolin (Apigenin 7-O-neohesperidoside) is extracted from Turpinia arguya Seem dried leaves.

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

15-SAHSA, a branched fatty acid ester of hydroxy fatty acids (FAHFAs), is recognized for its involvement in metabolic regulation. This compound comprises stearic acid esterified to 5-hydroxy stearic acid and is notably influenced by dietary changes, such as fasting and high-fat consumption, with a link to insulin sensitivity. SAHSA levels are specifically found to be moderately increased in the serum of AG4OX mice, which are characterized by their glucose tolerance through the overexpression of the Glut4 glucose transporter in adipose tissue. Given the established functions of FAHFAs in enhancing glucose tolerance, prompting insulin secretion, and exerting anti-inflammatory properties, 5-SAHSA emerges as a potential bioactive lipid implicated in the management of metabolic syndrome and inflammation.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are lipids influenced by dietary changes, playing a crucial role in insulin sensitivity. These compounds typically consist of a C-16 or C-18 fatty acid (for example, palmitoleic, palmitic, oleic, or stearic acid) linked to a hydroxy fatty acid with the same carbon chain length. 13-PAHSA, a derivative where palmitic acid is esterified to 13-hydroxy stearic acid, is notably prevalent in the adipose tissue of glucose-tolerant AG4OX mice, which exhibit enhanced glucose transport via the overexpression of the Glut4 glucose transporter. This observation, along with the metabolic benefits seen from other FAHFAs—including improved glucose tolerance, stimulated insulin secretion, and anti-inflammatory properties—suggests that 13-PAHSA may function as a bioactive lipid beneficial in managing metabolic syndrome and inflammation.

13-OAHSA, a branched fatty acid ester of hydroxy fatty acids (FAHFAs), results from the esterification of oleic acid to 13-hydroxy stearic acid. It represents a significant component of the FAHFA family, most abundantly expressed in the serum of glucose-tolerant AG4OX mice that exhibit adipose tissue-specific overexpression of the Glut4 glucose transporter. Similar to other FAHFAs which are known to enhance glucose tolerance, stimulate insulin secretion, and exert anti-inflammatory effects, 13-OAHSA may play a pivotal role in managing metabolic syndrome and inflammation.

Dapagliflozin impurity is the enantiomer of Dapagliflozin, Dapagliflozin is a sodium glucose transporter 2 inhibitor.

YM-543, a sodium-glucose transporter 2 (SGLT-2) inhibitor, is used potentially for the treatment of type 2 diabetes.

GLUT1-IN-3 (Compd 4b), a compound under investigation for type 1 glucose transporter deficiency syndrome, effectively inhibits seizures [1].

CTPI-2 is an inhibitor of mitochondrial citrate carrier SLC25A1 with(KD : 3.5 μM). CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. CTPI-2 exhibits anti-tumor activity.CTPI-2 halts salient alterations of NASH reverting steatosis, preventing the evolution to steatohepatitis, reducing inflammatory macrophage infiltration in the liver and adipose tissue, and starkly mitigating obesity induced by a high-fat diet.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are newly identified endogenous lipids regulated by fasting and high-fat feeding and associated with insulin sensitivity. Structurally, these esters are comprised of a C-16 or C-18 fatty acid (e.g., palmitoleic, palmitic, oleic, or stearic acid) linked to either a C-16 or C-18 hydroxy substituent. 12-PAHSA is a FAHFA in which palmitic acid is esterified at the 12th carbon of hydroxy stearic acid. Among the FAHFA family members, PAHSAs are the most abundant in the adipose tissue of glucose tolerant AG4OX mice, which overexpress the Glut4 glucose transporter specifically in adipose tissue. 12-PAHSA is present at 2- to 3-fold higher levels in adipose tissue of AG4OX mice compared to wild type mice. Levels of 12-PAHSA are also higher in fasted wild-type mice compared to fed mice and are reduced upon high-fat diet-induced obesity in insulin-resistant mice.

(S)-Empagliflozin-d4 is a deuterated compound of (S)-Empagliflozin. (S)-Empagliflozin has a CAS number of 864070-44-0. Empagliflozin is a Sodium-Glucose Cotransporter 2 Inhibitor. The mechanism of action of empagliflozin is as a Sodium-Glucose Transporter 2 Inhibitor.

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.

13-SAHSA, a branched fatty acid ester of hydroxy fatty acids (FAHFAs), has been found to be involved in metabolic regulation, particularly in relation to fasting, high-fat feeding, and insulin sensitivity. This compound is a synthesis of stearic acid and 13-hydroxy stearic acid. Notably, 13-SAHSA levels are found to be moderately increased in the serum of AG4OX mice, which are characterized by their glucose tolerance and expression of the Glut4 glucose transporter specifically in their adipose tissue. Similar to other FAHFAs, 13-SAHSA is believed to play a significant role in enhancing glucose tolerance, stimulating insulin secretion, and exerting anti-inflammatory effects, indicating its potential importance in addressing conditions related to metabolic syndrome and inflammation.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) have emerged as significant regulators of metabolic processes, influenced by dietary changes such as fasting and high-fat diets, and are linked to improved insulin sensitivity in mice. These compounds typically feature a fatty acid chain, either C-16 or C-18 in length (for example, palmitoleic, palmitic, oleic, or stearic acid), esterified to a hydroxy fatty acid of similar length. A specific FAHFA, 12-POHSA, involves the esterification of palmitoleic acid to the 12th carbon of stearic acid. Notably, 12-POHSA levels are markedly higher in the serum of AG4OX mice, which exhibit enhanced glucose tolerance due to overexpression of the Glut4 glucose transporter in adipose tissue. Given the capacity of FAHFAs to enhance glucose tolerance, stimulate insulin secretion, and exert anti-inflammatory actions, 12-POHSA holds potential as a bioactive lipid implicated in managing metabolic syndrome and inflammation.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are endogenous lipids that are influenced by fasting and high-fat diets and linked to improved insulin sensitivity in mice. These compounds typically feature a chain of either 16 or 18 carbon atoms (for example, palmitoleic, palmitic, oleic, or stearic acid) esterified with a hydroxy fatty acid chain of similar length. One specific FAHFA, known as 5-OAHSA, consists of oleic acid bonded to the fifth carbon of hydroxy stearic acid. Within the FAHFA family, OAHSAs exhibit the highest serum levels in AG4OX mice, which are known for their glucose tolerance attributed to the overexpression of the Glut4 glucose transporter in adipose tissue.

MMV009085 is a potent inhibitor of the Plasmodium falciparum hexose transporter (Pf HT1), with potential as an anti-malarial agent. It also inhibits the human glucose transporter, demonstrating high potency with an IC50 of 2.6 μM in glucose uptake assays and an EC50 of 1.23±0.04 μM against the 3D7 strain of the malaria parasite [1].