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FFA3 agonist 1 is an agonist of free fatty acid receptor 3 (FFA3). FFA3 agonist 1 regulates the health effect of intestinal microbiota by activating FFA3 .
SCH-900271 is an orally active, potent nicotinic acid receptor (NAR) agonist with an EC50 of 2 nM in the hu-GPR109a assay. SCH-900271 exhibits dose-dependent inhibition of plasma free fatty acid (FFA). SCH-900271 has an improved therapeutic window to flushing .
TUG-770 is a potent, selective and orally active GPR40/FFA1 agonist with an EC50 of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research . TUG-770 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pKi of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ .
AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC50s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC50<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist .
TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes .
FFA1 agonist-1 (Compound 17a) is an orally active fatty acid receptor 1 (FFA1) agonist with an EC50 of 0.75 μM. FFA1 agonist-1 can be used for type 2 diabetes mellitus research .
Metabolex-36 is a FFA4 agonist developed by Metabolex (now Cymabay Therapeutics) and used in multiple studies to investigate the function of FFA4. Metabolex-36 was used in conjunction with AstraZeneca compounds (AZ-423 and AZ-670) to investigate FFA4 function in pancreatic delta cells. Metabolex-36 has a pEC50 of 5.9 for FFA4 and a pEC50 of less than 4.0 for FFA1. Compound B was used to investigate the role of FFA4 in growth hormone-releasing peptide (ghrelin) secretion and somatostatin release and was used with FFA4 KO mice. Compound B had an EC50 of 15 nM for FFA4 in an IP3 accumulation assay in FFA4-transfected COS7 cells and was up to 1000-fold selective for FFA1. Compound B inhibited baseline ghrelin secretion from primary gastric mucosal cells but had no effect on cells from FFA4 KO mice. Oral administration of Compound B reduced plasma ghrelin levels in mice under starvation conditions. Compound B also inhibited somatostatin release from primary gastric epithelial cells but had no effect on cells from FFA4 KO mice.
GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4(FFA4) agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC50 values < 4.5 for all three species for FFA1, FFA2, and FFA3, respectively. GSK137647A has anti-inflammatory activity. GSK137647A induces insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response .
ZLY032 is a dual FFA1/PPARδ agonist with the activity of improving glucose and lipid metabolism, alleviating liver fibrosis, and potentially inhibiting metabolic disorders.
TUG-1387 is a analog of both AH-7614 and TUG-1506 that has no activity at FFA4. TUG-1387 can serve as negative control for studies assessing FFA4 function.
AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [ 3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents .
(S)-GLPG0974 is the isomer of GLPG0974 (HY-12940), and can be used as an experimental control. GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC50 of 9 nM.
TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM. TUG-424 may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity . TUG-424 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
GS-9667 (CVT 3619), a novel N 6-5'-substituted adenosine analog, is a selective, partial agonist of the A1 adenosine receptor (A1AdoR). GS-9667 binds to adipocyte membranes with high (KH=14 nM) and low (KL=5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC50 values of 6 nM and 44 nM, respectively. GS-9667 inhibits lipolysis and has the potential for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA) .
AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 calcium hydrate inhibits specific [ 3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 calcium hydrate could enhance insulin secretion and lower glucose levels in rodents . AMG 837 (calcium hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
HWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC50 of 18.9 nM) with moderate PPARδ activity (EC50 of 570.9 nM) . HWL-088 improves glucose and lipid metabolism, and has anti-diabetic effects .
GPR120 modulator 1 is a G protein coupled receptor 120 (GPR120) modulator extracted from patent US8394841B2, compound example F1. GPR120 modulator 1 can be used for the research of diseases associated with abnormal or deregulated GPR120, such as diabetes .
GPR120 modulator 2 is a G protein coupled receptor 120 (GPR120) modulator extracted from patent US8394841B2, compound example F13. GPR120 modulator 2 can be used for the research of diseases associated with abnormal or deregulated GPR120, such as diabetes .
Myricetin-3-O-β-D-xylopyranosyl-(1→2)-β-D-glucopyranoside is a natural product that can be obtained from sphaerophysa salsula. Myricetin-3-O-β-D-xylopyranosyl-(1→2)-β-D-glucopyranoside inhibits triglyceride (TG) accumulation in 3T3-L1 adipocytes .
CPL207280 is an orally active GPR40/FFA1 agonist with an antidiabetic effect. CPL207280 can effectively enhance glucose-stimulated insulin secretion and improve glucose tolerance in MIN6 pancreatic β-cells as well as in healthy Wistar Han rats and diabetic rat models. CPL207280 can be used for the research of type 2 diabetes .
AMG7703 is a selective and allosteric agonists of FFA2 (GPR43), the receptor for short-chain fatty acids (SCFAs), acetate, and propionate. AMG7703 can be used to research for in inflammatory and metabolic .
AZ1729 is a potent free fatty acid 2 receptor (FFA2) activator, acting as a direct allosteric agonist and as a positive allosteric modulator. AZ1729 increases the activity of the endogenously produced short chain fatty acid propionate in Gi-mediated pathways, but not at those transduced by Gq/G11. AZ1729 induces inhibition of isoproterenol-induced lipolysis in mouse adipocytes. AZ1729 also can Induce migration of human neutrophils. AZ1729 can be used for researching the signaling pathways of the physiological roles of FFA2 .
Rafabegron (AJ-9677) is a specific beta3-adrenoceptor agonist. Rafabegron can reduce blood glucose, insulin, FFA, and triglyceride levels in diabetic and obese mouse models .
Acipimox (K-9321), a nicotinic acid analogue, is an antilipolytic compound. Acipimox stimulates leptin releas, inhibits lipolysis and suppresses systemic levels of free fatty acids (FFAs) and improves insulin sensitivity .
Acipimox-d4 is the deuterium labeled Acipimox. Acipimox (K-9321), a nicotinic acid analogue, is an antilipolytic compound. Acipimox acutely inhibits lipolysis and suppresses systemic levels of free fatty acids (FFAs) and improves insulin sensitivity .
TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes . TUG-499 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis .
(-)-Lyoniresinol 9'-O-glucoside is an inhibitor of ROS. (-)-Lyoniresinol 9'-O-glucoside reduces lipid accumulation and lipid metabolic disorders in FFAs-exposed HepG2 cells. (-)-Lyoniresinol 9'-O-glucoside inhibits high glucose-induced reactive oxygen species production .
Acipimox (Standard) is the analytical standard of Acipimox. This product is intended for research and analytical applications. Acipimox (K-9321), a nicotinic acid analogue, is an antilipolytic compound. Acipimox stimulates leptin releas, inhibits lipolysis and suppresses systemic levels of free fatty acids (FFAs) and improves insulin sensitivity .
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
Niga-ichigoside F1, an orally active ursane triterpenoid, has antihyperlipidemic and antioxidant activities. Niga-ichigoside F1 can prevent high-fat diet (HFD)-induced hepatic steatosis .
Trimetazidine-d8 (dihydrochloride) is the deuterium labeled Trimetazidine dihydrochloride. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor[1][2][3][4].
Trimetazidine (dihydrochloride) (Standard) is the analytical standard of Trimetazidine (dihydrochloride). This product is intended for research and analytical applications. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
PPARδ agonist 10 (compound 7) is an orally active, selective, and partial agonist of PPARδ, with EC50 values of 0.053 μM and 0.30 µM for hPPARδ(LBD)-GAL4 and mPPARδ, respectively. PPARδ agonist 10 is a partial PPARδ agonist in transactivation assay but a full agonist on free fatty acids (FFA) oxidation in muscle cells both in vitro and in vivo. PPARδ agonist 10 can be used for dyslipidemia research .
Trimetazidine (Standard) is the analytical standard of Trimetazidine. This product is intended for research and analytical applications. Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor .
GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities .
Feprazone (DA2370; Prenazone), an analogue of Phenylbutazone (HY-B0230), is a nonsteroidal anti-inflammatory agent with analgesic and antipyretic activities. Feprazone acts by inhibiting the activity of cyclooxygenase (COX)-2. Feprazone ameliorates free fatty acid (FFA)-induced oxidative stress by reducing the production of mitochondrial reactive oxygen species (ROS). Feprazone can decrease the expression of MMP-2 and MMP-9. Besides, Feprazone can suppress adipogenesis and increase lipolysis in differentiating 3 T3-L1 cells. Feprazone also can be used to research atherosclerosis and obesity .
Feprazone (Standard) is the analytical standard of Feprazone. This product is intended for research and analytical applications. Feprazone (DA2370; Prenazone), an analogue of Phenylbutazone (HY-B0230), is a nonsteroidal anti-inflammatory agent with analgesic and antipyretic activities. Feprazone acts by inhibiting the activity of cyclooxygenase (COX)-2. Feprazone ameliorates free fatty acid (FFA)-induced oxidative stress by reducing the production of mitochondrial reactive oxygen species (ROS). Feprazone can decrease the expression of MMP-2 and MMP-9. Besides, Feprazone can suppress adipogenesis and increase lipolysis in differentiating 3 T3-L1 cells. Feprazone also can be used to research atherosclerosis and obesity .
Fatty acids (FAs) are the main components of lipids. The synthesis of fatty acids mainly involves the Triglyceride (TG) cycle and De Novo Lipogenesis (DNL). Fatty acids which exist widely in organisms are components of cell membranes and play an indispensable role in cell signaling. In addition, FFAs can be taken up from circulating plasma by all mitochondria-containing cells, and they are metabolized by β-oxidation and the citric acid cycle to release large amounts of energy in the form of ATP. Abnormal fatty acid metabolism is associated with the occurrence and development of cardiovascular diseases, diabetes, fatty liver, hyperthyroidism, and other diseases.
MCE offers a unique collection of fatty acid compounds. Fatty Acids Compound Library is an important tool for the study of energy metabolism and drug development of metabolism-related diseases.
Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis .
Niga-ichigoside F1, an orally active ursane triterpenoid, has antihyperlipidemic and antioxidant activities. Niga-ichigoside F1 can prevent high-fat diet (HFD)-induced hepatic steatosis .
Myricetin-3-O-β-D-xylopyranosyl-(1→2)-β-D-glucopyranoside is a natural product that can be obtained from sphaerophysa salsula. Myricetin-3-O-β-D-xylopyranosyl-(1→2)-β-D-glucopyranoside inhibits triglyceride (TG) accumulation in 3T3-L1 adipocytes .
(-)-Lyoniresinol 9'-O-glucoside is an inhibitor of ROS. (-)-Lyoniresinol 9'-O-glucoside reduces lipid accumulation and lipid metabolic disorders in FFAs-exposed HepG2 cells. (-)-Lyoniresinol 9'-O-glucoside inhibits high glucose-induced reactive oxygen species production .
Trimetazidine-d8 (dihydrochloride) is the deuterium labeled Trimetazidine dihydrochloride. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor[1][2][3][4].
Acipimox-d4 is the deuterium labeled Acipimox. Acipimox (K-9321), a nicotinic acid analogue, is an antilipolytic compound. Acipimox acutely inhibits lipolysis and suppresses systemic levels of free fatty acids (FFAs) and improves insulin sensitivity .
GPR43 Antibody is an unconjugated, approximately 37 kDa, rabbit-derived, anti-GPR43 polyclonal antibody. GPR43 Antibody can be used for: ELISA, IHC-P, IHC-F, ICC, IF expriments in human, mouse, and predicted: rat background without labeling.
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