GSK-3787 - CAS 188591-46-0
Catalog number: B0084-272130
Category: Inhibitor
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GSK-3787 is a potent and selective ligand for PPARdelta with good pharmacokinetic properties.
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B0084-272130 50 mg $198 In stock
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GSK-3787; GSK3787; GSK 3787.
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1.Peroxisome proliferator-activated receptor β/δ does not regulate glucose uptake and lactose synthesis in bovine mammary epithelial cells cultivated in vitro.
Lohakare J;Osorio JS;Bionaz M J Dairy Res. 2018 Aug;85(3):295-302. doi: 10.1017/S0022029918000365. Epub 2018 Jun 26.
The hypothesis of the study was that inhibition of PPARβ/δ increases glucose uptake and lactose synthesis in bovine mammary epithelial cells by reducing the expression of the glucose transporter mRNA destabiliser calreticulin. Three experiments were conducted to test the hypothesis using immortalised bovine mammary alveolar (MACT) and primary bovine mammary (PBMC) cells. In Experiment 1, the most effective dose to inhibit PPARβ/δ activity among two synthetic antagonists (GSK-3787 and PT-s58) was assessed using a gene reporter assay. In Experiment 2, the effect on glucose uptake and lactose synthesis was evaluated by measuring glucose and lactose in the media and expression of related key genes upon modulation of PPARβ/δ using GSK-3787, the synthetic PPARβ/δ agonist GW-501516, or a combination of the two in cells cultivated in plastic. In Experiment 3, the same treatments were applied to cells cultivated in Matrigel and glucose and lactose in media were measured. In Experiment 1 it was determined that a significant inhibition of PPARβ/δ in the presence or absence of fetal bovine serum was achieved with ≥ 1000 nm GSK-3787 but no significant inhibition was observed with PT-s58. In Experiment 2, inhibition of PPARβ/δ had no effect on glucose uptake and lactose synthesis but they were both increased by GW-501516 in PBMC.
2.JAZF1 regulates visfatin expression in adipocytes via PPARα and PPARβ/δ signaling.
Ming GF;Li X;Yin JY;Ai YH;Xu DM;Ma XH;Liu ZY;Liu HX;Zhou HH;Liu ZQ Metabolism. 2014 Aug;63(8):1012-21. doi: 10.1016/j.metabol.2014.05.006. Epub 2014 May 15.
OBJECTIVE: ;Current whole genome-wide association study has identified the association of JAZF1 with type 2 diabetes; its close relation with glucose and lipid metabolism has also been revealed. However, to date, JAZF1 remains a relatively new gene with unknown function.;MATERIALS/METHODS: ;We constructed JAZF1 overexpression vector and synthesized JAZF1 siRNA, then transfected them into 3T3-L1 adipocytes, investigated the relationship between the regulations of JAZF1, visfatin, and other adipokines, researched the specific function of JAZF1 in glucose and lipid metabolism.;RESULTS: ;This study found that the expression of JAZF1 was gradually but significantly upregulated during the induced differentiation of 3T3-L1 preadipocytes, and that the trend of its expression was consistent with that of visfatin. Further studies indicated that JAZF1 promoted the expressions of visfatin, PPARα, and PPARβ/δ in adipocytes but simultaneously inhibited the expressions of TAK1 and PPARγ. Luciferase reporter assay revealed that JAZF1 activated the transcription of visfatin, but ChIP assay results indicated that JAZF1 did not directly bind to visfatin PPRE. Our results also showed that the JAZF1 overexpression-increased visfatin expression was abolished by the addition of PPARα antagonist GW 6471 and PPARβ/δ antagonist GSK 3787 respectively.
3.A PPARδ-selective antagonist ameliorates IMQ-induced psoriasis-like inflammation in mice.
Wang X;Hao Y;Wang X;Wang L;Chen Y;Sun J;Hu J Int Immunopharmacol. 2016 Nov;40:73-78. doi: 10.1016/j.intimp.2016.08.027. Epub 2016 Aug 29.
PPARδ is highly expressed in skin, especially keratinocytes, and its expression is increased in psoriatic lesions. However, the potential role of PPARδ in the pathogenesis of psoriasis remains undefined. Mice treated with Imiquimod (IMQ) to induce psoriasis can be used to evaluate the pathogenesis of psoriasis, and this model has become one of the most important in vivo research tools for research on the disease. In the current study, we showed that PPARδ was highly expressed in the skin of IMQ-induced psoriasis mice. To further understand the impact of PPARδ in psoriasis, we used these mice in a series of experiments to evaluate the pathogenesis of psoriasis. We found that PPARδ was highly expressed in both psoriatic lesions and normal skin in IMQ-induced psoriasis mice. Furthermore, the expression of PPARδ-relevant lipases was also significantly increased. The PPARδ-selective antagonist GSK3787 ameliorated the observed inflammation in the skin of the experimental mice. Based on these results, PPARδ may be a potential target for the effective treatment of psoriasis.
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CAS 188591-46-0 GSK-3787

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