FFAR
The free fatty acid receptor (FFAR) is a G protein-coupled receptor (GPCR) activated by free fatty acids (FFAs), which play important roles not only as essential nutritional components but also as signaling molecules in numerous physiological processes. Free fatty acids (FFAs) are an important energy source for most body tissues, and are categorized by the length of their aliphatic tails; short-chain fatty acids (SCFAs) have less than 6 carbons, medium-chain fatty acids have 6–12 carbons, and long-chain fatty acids have 12 or more carbons. Five free fatty acid receptors (FFARs) have received considerable attention as a result of their physiological importance in various biological processes. Among the FFARs that have been identified, FFA1 (GPR40) and GPR120 are activated by medium- and long-chain FFAs, and GPR84 is activated by medium-chain FFAs. In contrast, FFA2 (GPR43) and FFA3 (GPR41) are activated by SCFAs. Each FFAR may act as a sensor for FFAs with selectivity for a particular FFA carbon chain length that is derived from food or food-derived metabolites. Physiological functions of FFARs have been reported to include the secretion of insulin and incretin hormones, adipocyte differentiation, anti-inflammatory effect, nerve activation, and taste preferences.
References
1.Hara T, et al. Rev Physiol Biochem Pharmacol. 2013;164:77–116.
References
1.Hara T, et al. Rev Physiol Biochem Pharmacol. 2013;164:77–116.
GPCR/G Protein
ACAT(3)
Angiotensin Receptor(27)
Antibacterial(545)
Bombesin Receptor(13)
Bradykinin Receptor(23)
Calcium Channel(197)
cAMP(16)
Cannabinoid Receptor(88)
CaSR(18)
CGRP Receptor(18)
Chemokine Receptor(104)
Cholecystokinin Receptor(24)
CRF Receptor(15)
Dopamine Receptor(182)
Endothelin Receptor(28)
FFAR(5)
Galanin Receptor(1)
GHSR(20)
Glucagon Receptor(51)
GPCR19(9)
GPR119(3)
Hedgehog (Hh)(35)
Histamine Receptor(139)
Imidazoline Receptor(1)
Leukotriene Receptor(15)
LHR(1)
LPA Receptor(19)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(8)
Melanocortin Receptor(28)
Melatonin Receptor(7)
Motilin Receptor(4)
Neurokinin Receptor(43)
Neuropeptide Y Receptor(44)
Neurotensin Receptor(11)
Orexin Receptor(16)
Other Targets(3)
OXTR(2)
P2Y Receptor(14)
PAR(28)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(79)
PTH Receptor(1)
S1P Receptor(35)
SGLT(26)
Somatostatin Receptor(16)
Urotensin Receptor(4)
Vasopressin Receptor(20)
FFAR
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LY2922470
产品货号 : M11781
cas no: 1423018-12-5
LY2922470 (LY-2922470) 是一种有效的、选择性的、口服的 GPR40 激动剂,EC50 为 7 nM;对 PPARα/β/γ (>10 uM) 无活性。 -
GLPG 0974
产品货号 : M11618
cas no: 1391076-61-1
GLPG 0974 是一种有效的、选择性游离脂肪酸受体 2 (FFA2、GPR43) 拮抗剂,IC50 为 95 nM。 -
PBI-4050 sodium
产品货号 : M11033
cas no: 1254472-97-3
PBI-4050(Setogepram,PBI4050)是一种中链脂肪酸的合成类似物,分别对 GPR40 和 GPR84 显示出激动剂和拮抗剂配体亲和力。 -
PBI-4050
产品货号 : M10026
cas no: 1002101-19-0
PBI-4050(Setogepram,PBI4050)是一种中链脂肪酸的合成类似物,分别对 GPR40 和 GPR84 显示出激动剂和拮抗剂配体亲和力。 -
Fasiglifam
产品货号 : M10006
cas no: 1000413-72-8
Fasiglifam (TAK-875) 是一种有效的,可口服的,具有选择性的 GPR40 激动剂,EC50 值为 14nM。