Aleglitazar(R1439; RO-0728804) is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.IC50 Value: 2.8 nM(PPAR-α); 4.6 nM(PPAR-γ)Target: PPARα/γAleglitazar (R1439) is a dual peroxisome proliferator-activated receptor (PPAR) agonist, with affinity to PPARα and PPARγ. Aleglitazar is being developed for the treatment of type II diabetes; It is currently in phase III clinical trials. In preliminary clinical studies, Aleglitazar has been demonstrated to improve hyperglycemia and dyslipidemia in patients with type 2 diabetes mellitus. Aleglitazar has beneficial effects on both lipid and glucose parameters and may have a therapeutic role in modifying cardiovascular risk factors and improving glycemic control in patients with T2DM. Aleglitazar combines the lipid benefits of fibrates and the insulin-sensitizing benefits of thiazolidinediones.
3, 4-seco-4 (23),20(29) -Lupadiene-3,28-dioic acid (Compound 5) is a triterpenoid compound. 3, 4-seco-4 (23),20(29)-Lupadiene-3,28-dioic acid has a strong inhibitory effect on the production of superoxide anions, and the inhibitory rate is 86.9±2.8% at 1 μM[1].
C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss[1][2][3][4][5].
Acetyl-Hirudin (54-65) (sulfated) binds directly to thrombin-rHCII(L444R) and disrupts interactions between the N-terminal acidic domain of rHCII and anion-binding exosite I of thrombin that serves to stabilize the complex[1].
Creatine D3 hydrate is a deuterium labeled Creatine hydrate. Creatine hydrate is pivotal in energy metabolism of muscle and brain cells, both in physiological and in pathological conditions[1].
(±)-Leucine-13C-1 (DL-Leucine-13C-1) is the 13C-labeled (±)-Leucine. (±)-Leucine (DL-Leucine), an isomer of Leucine, chemosterilant and dietary additive. (±)-Leucine inhibits growth of Escherichia coli HfrH by 92.08%[1].
L-6424 inhibits T3 binding to α1-T3R and β1-T3R[1].
Hypoglycemic agent 1 acts as a therapeutic and/or prophylactic agent for diabetes. Hypoglycemic agent 1 has an action for lowering blood sugar[1].
Gastric mucin is a large glycoprotein which is thought to play a major role in the protection of the gastrointestinal tract from acid, proteases, pathogenic microorganisms, and mechanical trauma.
CPA inhibitor is a potent inhibitor for carboxypeptidase A (CPA).
BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes[1].
cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity[1].
Ganglioside GM3 sodium salt is a sialylated membrane-based glycosphingolipid that regulates insulin receptor signaling via direct association with the receptor. Ganglioside GM3 sodium salt possesses powerful effects on cancer development and progression[1][2].
7-Acetylintermedine is a hepatotoxic botanical pyrrolizidine alkaloid[1].
Farglitazar is a PPARγ agonist that has significant therapeutic benefits such as glycemic control in type 2 diabetic patients.
MSI-1701 is an analogue of MSI-1436 which can control weight gain and blood glucose level extracted from patent US 7410959 B1.
Rosiglitazone (BRL49653) is a potent thiazolidinedione insulin sensitizer. Rosiglitazone is a selective PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively.
GSK2324 (Compd 1c) is a FXR agonist for diabetes study, with an EC50 of 120 nM. GSK2324 exhibits t1/2 values of 84 min (mouse), 170 min (rat), 110 min (beagle) and 120 min (cyno), respectively[1].
Hydroxocobalamin hydrochloride is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the research of vitamin B12 deficiency including pernicious anemia[1][2].
MK196 (MK-196) is an investigational diuretic which has pronounced saluretic activity in the rat and dog as well as both uricosuric and saluretic activity in the chimpanzee.
Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling[1].
Pitavastatin Calcium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells.
HNMPA is a membrane impermeable insulin receptor tyrosine kinase inhibitor. HNMPA inhibits serine and tyrosine autophosphorylation by the human insulin receptor. HNMPA has no effect on protein kinase C or cyclic AMP-dependent protein kinase activities[1][2]
(R)-ND-336 is a potent and selective MMP-9 inhibitor with a Ki of 19 nM. (R)-ND-336 inhibits MMP-2 (Ki=127 nM) and MMP-14 (Ki=119 nM). (R)-ND-336 has the potential for diabetic foot ulcers (DFUs) research[1].
TUG-891 is a potent and selective agonist of the long chain free fatty acid (LCFA) receptor 4.
BPH-652 is a S. aureus dehydrosqualene synthase (CrtM) inhibitor, with a Ki of 1.5 nM and an IC50 of 100-300 nM (S. aureus pigment formation)[1].
Lacto-N-neodifucohexaose II (Compd 9) is a derivative of key human milk tetrasaccharide[1].
EP3 antagonist 4 (Compound 28) is an EP3 antagonist, with a Ki value of 2 nM for hEP. EP3 antagonist 4 shows low in vivo clearance, high oral AUC, and good bioavailability in the rat full PK studies. EP3 antagonist 4 can be used for research of beta cell dysfunction in diabetes[1].
(-)-Isodocarpin (Isodocarpin), a diterpenoid, is a potent melanogenesis inhibitor with an IC50 of 0.19 μM in B16 4A5 cells. (-)-Isodocarpin inhibits the expression of tyrosinase, tyrosine-related protein (TRP)-1, and TRP-2 mRNA[1].
Ferroportin-IN-1 is a ferroportin inhibitor extracted from patent WO2020123850A1 compound 23. Ferroportin-IN-1 can be used for the research of diseases caused by a lack of hepcidin or iron metabolism disorders[1].