GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively.IC50 value: 6.3/6.2/6.1 (pEC50, for human/mouse/rat FFA4)Target: FFA4The pEC50s for Human , Mouse and Rat FFA1/2/3 are ＜ 4.5. GSK137647A is evaluated against a panel of 65 targets in both full curve functional and binding assays and was shown to provide at least 100-fold selectivity against the panel which included 41 G-protein-coupled receptors (GPCRs), including additional members of the free fatty acid receptors (FFA1, FFA2, and FFA3). GSK137647A produces a concentration-dependent increase in glucose stimulated insulin secretion under high glucose conditions (25 mM).
Golocdacimab (MEDI6570) is a fully human anti-LOX-1 monoclonal antibody. Golocdacimab (MEDI6570) has the potential for the research of type 2 diabetes[1].
α-Glucosidase-IN-11 is a highly permeable competitive α-glucosidase inhibitor with the IC50 value of 0.56 μM. α-Glucosidase-IN-11 binds to Trp residues in α-glucosidase and regulates protein folding. α-Glucosidase-IN-11 can be used to regulate blood glucose levels[1].
Lecimibide (DuP 128) is a potent and specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor for antihyperlipidemia research[1][2].
OSMI-2 (Compound 1b) is a cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-2 increases detained intron splicing in cells[1].
Mogroside I A1, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities[1].
ACAT-IN-1 cis isomer is a potent ACAT inhibitor with an IC50 of 100 nM.
3α-Hydroxymogrol is a triterpenoid isolated from Siraitia grosvenorii Swingle, acts as a potent AMPK activator, and enhances AMPK phosphorylation[1].
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators[1][2][3].
α-Glucosidase-IN-22 (compound 7i), a benzimidazole, is a potent α-glucosidase inhibitor with an IC50 of 0.64 μM. α-Glucosidase-IN-22 is a potent anti-diabetic agent and has the potential for type 2 diabetes mellitus (T2DM) research[1].
Gymnemic acid I is a bioactive triterpene saponin found in Gymnema sylvestre. Gymnemic acid I decreases the apoptosis under the high glucose stress[1][2].
Eudebeiolide B is a compound that can be isolated from Salvia plebeia R. Br. Eudebeiolide B inhibits osteoclastogenesis by regulating RANKL-induced NF-κB, c-Fos and calcium signaling. Eudebeiolide B can be used for osteoclast-related diseases research[1].
Prostaglandin E1 (PGE1) is a potent vasodilator and activates the prostaglandin E1 (EP) receptor.
trans-4-Hydroxycyclohexanecarboxylic acid is a substrate for cyclohexanecarboxylic acid production. trans-4-Hydroxycyclohexanecarboxylic acid is the by-product of intestinal bacterial metabolism via urinary excretion[1].
Tyrosinase (Polyphenol oxidase) is a rate-limiting enzyme that controls the production of melanin and is encoded by TYR gene. Tyrosinase is mainly found in melanosomes synthesized by skin melanocytes[1].
3-O-cis-p-Coumaroyl maslinic acid (compound 16) is a natural compound isolated from the ethyl acetate extract of leaves of Miconia albicans.3-O-cis-p-Coumaroyl maslinic acid can inhibit PTP1B, with the IC50 of 0.46 μM, and shows antimicrobial activity on Gram-positive bacteria and yeasts[1][2].
AC1903 is a potent, specific TRPC5 channel inhibitor with IC50 of 14.7 uM; blocks riluzole-activated TRPC5 whole-cell current, but fails to block carbachol (CCh)-induced TRPC4 and OAG-induced TRPC6 currents, even at high micromolar concentrations; pecifically blocks TRPC5 channel activity in glomeruli of proteinuric rats, suppresses severe proteinuria and prevents podocyte loss in a transgenic rat model of FSGS.
LX-4211 is a potent dual SGLT2/1 inhibitor; Antidiabetic agents.IC50 value:Target: SGLT1/2LX4211 enhanced urinary glucose excretion by inhibiting SGLT2-mediated renal glucose reabsorption; markedly and significantly improved multiple measures of glycemic control, including fasting plasma glucose, oral glucose tolerance, and HbA(1c); and significantly lowered serum triglycerides. LX4211 also mediated trends for lower weight, lower blood pressure, and higher glucagon-like peptide-1 levels. In a follow-up single-dose study in 12 patients with T2DM, LX4211 (300 mg) significantly increased glucagon-like peptide-1 and peptide YY levels relative to pretreatment values, probably by delaying SGLT1-mediated intestinal glucose absorption [1]. LX4211-treated mice and SGLT1-/- mice also had increased GLP-1 AUC values, decreased glucose-dependent insulinotropic polypeptide (GIP) AUC values, and decreased blood glucose excursions during the 6 hours after a challenge with oral glucose alone [2].
Dehydrotumulosic acid, one of the effective constituents of Poria cocos, was isolated from the chloroform-soluble material of ethanol extract of the fungus. Poria cocos, a popular Chinese medicinal herb of fungal origin, has been included in many combinations with other CM herbs for its traditionally claimed activities of inducing diuresis, excreting dampness, invigorating the spleen and tranquilizing the mind and its modern pharmacological use of modulating the immune system of the body[1].
Dihydrotachysterol is a synthetic analog of vitamin D. Dihydrotachysterol can be used to for the research of hypocalcemia (lack of calcium in the blood) and hypoparathyroidism (lack of parathyroid hormone in the body) [1][2].
THR-β agonist 6 is an orally active, selective thyroid hormone receptor β (THR-β) agonist with EC50s of 0.03 μM and 0.22 μM for THR-β and THR-α, respectively. THR-β agonist 6 exhibits an xcellent liver-to-serum ratio of 93:1 in mice. THR-β agonist 6 has the potential for nonalcoholic steatohepatitis (NASH) research[1].
PDE4-IN-14 (Compound 1) is a PDE4 inhibitor that can be used in the study of PDE4-related diseases (such as inflammatory and immune diseases, cancer, and metabolic diseases, etc.)[1].
(2R)-SR59230A is the inactive isomer of SR59230A (HY-100672), and can be used as an experimental control. SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist[1] with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively[2].
Topterone is a topical antiandrogen.
Azilsartan mepixetil potassium (QR-01019K) is the antagonist of angiotensin II receptor. Azilsartan mepixetil potassium has stronger and longer blood pressure effect, more abvious and longer lasting heart rate lowering effect and high safety. Azilsartan mepixetil potassium has the potential for the research of hypertension, chronic heart failure and diabetic nephropathy (extracted from patent CN107400122A)[1].
Kemptide is a synthetic heptapeptide that acts as a specific substrate for cAMP-dependent protein kinase (PKA).
L-Hexanoylcarnitine is an acylcarnitine and is found to be associated with celiac disease.
C11 BODIPY 581/591 is a lipid-soluble ratiometric fluorescent indicator of lipid oxidation. Upon oxidation, its excitation maximum shifts from 581 to 500 nm and the emission maximum shifts from 591 to 510 nm. C11 BODIPY 581/591 has been used in the quantitation of ferroptosis.
(Pro3) GIP, human ((Pro3) Gastric Inhibitory Peptide, human) is an efficacious, stable and specific human GIP receptor (hGIPR) full agonist. (Pro3) GIP, human has high binding affinity for human GIPR with Ki/ Kd values of 0.90 nM. (Pro3) GIP, human can be used for the research of obesity-related diabetes[1][2].
Kushenol K, a flavonoid antioxidant isolated from the roots of Sophora flavescens. Kushenol K is a cytochrome P-450 3A4 (CYP3A4) inhibitor with a Ki value of 1.35 μM[1]. Kushenol K shows weak antiviral activity against HSV-2 (EC50 of 147 μM)[2]. Kushenol K also inhibits the activity of SGLT1 and SGLT2[3].