Structure of TUG-891
CAS No.: 1374516-07-0
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
TUG-891 is a selective agonist of long chain free fatty acid (LCFA) receptor 4 (GPR120).
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
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CAS No. : | 1374516-07-0 |
Formula : | C23H21FO3 |
M.W : | 364.41 |
SMILES Code : | O=C(O)CCC1=CC=C(OCC2=CC(F)=CC=C2C3=CC=C(C)C=C3)C=C1 |
MDL No. : | MFCD22421654 |
InChI Key : | LPGBXHWIQNZEJB-UHFFFAOYSA-N |
Pubchem ID : | 57522038 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
BMMSCs | 0.5 µM | 3 days | Low concentrations of TUG-891 elevated P38 and increased adipogenesis | Sci Rep. 2015 Sep 14;5:14080 |
Mouse colonic mucosal cells | 300 nM | 10–15 minutes | To compare the pharmacology of FFA1 and FFA4 agonists, finding selective agonists more potent than GW9508 | Br J Pharmacol. 2017 Dec;174(23):4508-4522. |
DU145 cells | 1 µM | 15 minutes | Inhibits LPA-induced p70S6K phosphorylation | J Pharmacol Exp Ther. 2015 Feb;352(2):380-94 |
Brown adipocytes | 10 µM | 10 minutes | To investigate the effect of TUG-891 on mitochondrial membrane potential, results showed that TUG-891 caused mitochondrial depolarization. | EMBO Mol Med. 2018 Mar;10(3):e8047 |
BMMSCs | 50 µM | 14 days | High concentrations of TUG-891 promoted osteogenesis via the Ras-ERK1/2 cascade | Sci Rep. 2015 Sep 14;5:14080 |
MPC5 podocytes | 10 µM | 24 hours | To evaluate the protective effect of TUG-891 on high glucose-induced podocyte injury. Results showed that TUG-891 significantly suppressed the high glucose-induced increases in fibronectin, collagen IV, α-SMA, TGF-β1, and IL-6 expression, and reduced the phosphorylation of TAK1, IKKβ, NF-κB p65, JNK, and p38 MAPK. | Acta Pharmacol Sin. 2021 Feb;42(2):252-263 |
Bovine granulosa cells | 1, 10, 50 µM | 24 hours | DHA (10 and 50 μM) significantly increased cell proliferation; TUG-891 (1 and 50 μM) also increased cell proliferation | Reprod Biol Endocrinol. 2018 Apr 26;16(1):40 |
Bovine cumulus cells | 1 µM or 5 µM | 24 hours | Investigate the effect of TUG-891 on cumulus cells, results showed TUG-891 treatment increased blastocyst rate | J Ovarian Res. 2017 Nov 9;10(1):74 |
RAW264.7 murine macrophages | 100 µM | 24 hours | To assess the effects of TUG-891 on ROS-related protein expression, results showed increased Nrf2 nuclear translocation and HO-1 and NQO1 expression, and decreased Nox1 expression. | Int J Mol Sci. 2021 Sep 29;22(19):10544 |
Brown adipocytes | 10 µM | 30 minutes | To evaluate the effect of TUG-891 on the oxygen consumption rate (OCR) of brown adipocytes, results showed that TUG-891 significantly increased OCR. | EMBO Mol Med. 2018 Mar;10(3):e8047 |
RAW264.7 murine macrophages | 20–100 µM | 48 hours | To test the effects of TUG-891 on cell viability, results showed no effect on cell viability at all concentrations tested. | Int J Mol Sci. 2021 Sep 29;22(19):10544 |
RAW264.7 murine macrophages | 20–100 µM | 5 days | To evaluate the effects of TUG-891 on osteoclast formation, results showed significant reduction in osteoclast formation. | Int J Mol Sci. 2021 Sep 29;22(19):10544 |
PC-3 cells | 1 µM | 6 hours | Inhibits LPA- and EGF-induced cell migration | J Pharmacol Exp Ther. 2015 Feb;352(2):380-94 |
RAW264.7 cells | 3 µM | 60 minutes | TUG-891, as a selective agonist of GPR120, could reproduce the effect of EPA in RAW264.7 cells, suppressing LPS-induced Ccl2 expression. | J Neuroinflammation. 2020 Apr 24;17(1):129 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
ICR mice and C57BL/6 mice | Normal ICR mice and diet-induced obese (DIO) mice | Oral administration | 10, 20, 30, and 100 mg/kg | Single dose | Evaluate the hypoglycemic effect of TUG-891 in normal mice and DIO mice, results showed TUG-891 could reduce blood glucose levels in a dose-dependent manner and exhibited good anti-hyperglycemic effects in DIO mice | Molecules. 2021 Nov 16;26(22):6907 |
C57BL/6 mice | Ovariectomized model | Bone marrow cavity injection | 10, 30, 50 μmol/kg | Three times per week for 10 weeks | High doses of TUG-891 rescued oestrogen-deficient bone loss in vivo | Sci Rep. 2015 Sep 14;5:14080 |
Mice | Wild-type mice | Lingual application | 100 μM | Single dose, monitored for 30 min | TUG891 activated the tongue-brain-gut axis, increased pancreatobiliary secretions, reduced circulating LDL, and modulated fat preference. | J Lipid Res. 2020 Feb;61(2):133-142 |
ICR mice | Normal ICR mice | Oral | 20 mg/kg | Single dose | Evaluate the effect of TUG-891 on oral glucose tolerance in normal ICR mice | Int J Mol Sci. 2024 Oct 25;25(21):11476 |
ApoE-knockout mice | High-fat diet-induced liver steatosis model | Subcutaneous injection | 20 mg/kg | Three times a week for 16 weeks | To evaluate the effect of TUG-891 on liver steatosis, results showed that TUG-891 inhibited the progression of liver steatosis, reduced TG accumulation in the liver, and decreased plasma AST levels. | Cardiovasc Drugs Ther. 2024 Aug;38(4):667-678 |
ApoE-knockout mice | Atherosclerosis model | Subcutaneous injection | 20 mg/kg | Three times a week for 4 months | TUG-891 administration has led to the reduction of atherosclerotic plaque size and necrotic cores in an apoE-knockout mice model. TUG-891-treated mice were administered subcutaneously at a dose of 20 mg/kg three times a week for 4 months. The FFAR4 agonist reduced the content of pro-inflammatory M1-like macrophages content in atherosclerotic plaques, as evidenced by immunohistochemical phenotyping and molecular methods. In atherosclerotic plaque, the population of smooth muscle cells increased as evidenced by α-SMA staining. We observed changes in G-CSF and eotaxin markers in the plasma of mice; changes in the levels of these markers in the blood may be related to macrophage differentiation. Importantly, we observed a significant increase in M2-like macrophage cells in atherosclerotic plaque and peritoneum. | Int J Mol Sci. 2021 Sep 9;22(18):9772 |
Rats | Type 1 diabetes model rats | Oral | 20 mg/kg | Single dose, immediately before glucose load | TUG-891, a GPR120 agonist, ameliorated postprandial hyperglycemia but TAK-875, a GPR40 agonist, did not. | Front Pharmacol. 2023 Jul 31;14:1197743 |
Mice | Db/db diabetic mice model | Gavage | 35 mg/kg | Once daily for 4 weeks | To evaluate the protective effect of TUG-891 on diabetic nephropathy. Results showed that TUG-891 significantly improved urinary albumin excretion, protected against podocyte injury, reduced collagen deposition in the glomerulus, and inhibited the mRNA and protein expression of fibronectin, collagen IV, α-SMA, TGF-β1, and IL-6. Additionally, TUG-891 downregulated the phosphorylation of Smad3 and STAT3, alleviating glomerulosclerosis. | Acta Pharmacol Sin. 2021 Feb;42(2):252-263 |
C57Bl/6J mice | Wild-type and GPR120 knockout mice | Intraperitoneal injection | 35 mg/kg | Once daily for 2.5 weeks | To evaluate the effect of TUG-891 on body weight and fat oxidation, results showed that TUG-891 reduced body weight and fat mass, and increased fat oxidation. | EMBO Mol Med. 2018 Mar;10(3):e8047 |
C57BL/6 mice | Intraventricular hemorrhage model | Intraperitoneal injection | 35 mg/kg | Once at 1, 24, and 48 hours | TUG-891 protects neurons by inhibiting endoplasmic reticulum stress and pyroptosis, improving neurological function | Neural Regen Res. 2023 Oct;18(10):2278-2284 |
Mice | Cisplatin-induced acute kidney injury model | Oral gavage | 35 mg/kg/day | Once daily for six days | To investigate the effect of TUG-891 on cisplatin-induced acute kidney injury, results showed that TUG-891 improved renal function and pathological damage, and reduced the expression of cellular senescence markers | Signal Transduct Target Ther. 2022 Nov 30;7(1):384 |
Rats | PCOS-IR rat model | Intraperitoneal injection | 9.1 × 6.3/kg /day | Once daily for four weeks | TUG-891 improved insulin resistance and chronic inflammation in PCOS-IR rats by upregulating GPR120 expression | Int J Mol Sci. 2024 Oct 17;25(20):11146 |
Tags: TUG-891 | TUG891 | TUG 891 | Free Fatty Acid Receptor | FFAR | inhibitor | 1374516-07-0 |
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