GSK-3787 - CAS 188591-46-0
Catalog number: B0084-272130
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C15H12ClF3N2O3S
Molecular Weight:
392.78059
COA:
Inquire
Targets:
PPAR
Description:
GSK-3787 is a potent and selective ligand for PPARdelta with good pharmacokinetic properties.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-272130 50 mg $198 In stock
Bulk Inquiry
Synonyms:
GSK-3787; GSK3787; GSK 3787.
MSDS:
Inquire
InChIKey:
JFUIMTGOQCQTPF-UHFFFAOYSA-N
InChI:
InChI=1S/C15H12ClF3N2O3S/c16-12-4-1-10(2-5-12)14(22)20-7-8-25(23,24)13-6-3-11(9-21-13)15(17,18)19/h1-6,9H,7-8H2,(H,20,22)
Canonical SMILES:
C1=CC(=CC=C1C(=O)NCCS(=O)(=O)C2=NC=C(C=C2)C(F)(F)F)Cl
Current Developer:
GlaxoSmithKline.
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related PPAR Products


DG172 dihydrochloride
(CAS: 1361504-77-9)

The dihydrochloride salt form of DG-172, a piperazin drrivative, is a PPARβ/δ inverse agonist that could promote cell differentiation of dendritic induced by GM...

CAS 1639792-20-3 Saroglitazar (Magnesium)

Saroglitazar (Magnesium)
(CAS: 1639792-20-3)

Saroglitazar magnesium is a dual PPAR agonist with potent predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, res...

CAS 475479-34-6 Aleglitazar

Aleglitazar
(CAS: 475479-34-6)

Aleglitazar is a potent dual agonist of peroxisome proliferator-activated receptor (PPAR) α/γ.

CAS 927961-18-0 Lanifibranor

Lanifibranor
(CAS: 927961-18-0)

Lanifibranor is a peroxisome proliferator-activated receptors (PPAR) agonist.

CAS 111-58-0 Oleylethanolamide

Oleylethanolamide
(CAS: 111-58-0)

Oleylethanolamide is an endogenous agonist for PPARα with an EC50 value of 120 nM in a transactivation assay. Oleylethanolamide is also a selective GPR55 agonis...

CAS 824932-88-9 GFT505

GFT505
(CAS: 824932-88-9)

Elafibranor is an agonist of the peroxisome proliferator-activated receptor-α and peroxisome proliferator-activated receptor-δ. It induces resolution of nonalco...

CAS 155141-29-0 Rosiglitazone maleate

Rosiglitazone maleate
(CAS: 155141-29-0)

Rosiglitazone exhibits insulin-sensitising activity 60- to 200-fold higher than that of troglitazone, englitazone, or piogliazone in rodent models of insulin re...

CAS 848259-27-8 Pemafibrate

Pemafibrate
(CAS: 848259-27-8)

Pemafibrate is a Peroxisome proliferator-activated receptor alpha agonist. It can decrease the secretion of inflammatory markers without affecting cell prolifer...

CAS 637-07-0 Clofibrate

Clofibrate
(CAS: 637-07-0)

Clofibrate is a fibric acid derivative used in the treatment of hyperlipoproteinemia type III and severe hypertriglyceridemia.

CAS 213411-84-8 BM152054

BM152054
(CAS: 213411-84-8)

BM152054, a thiazolidinedione, revealed to be potent PPARg-activators in transient transfection assays in vitro.

CAS 702680-17-9 CP 775146

CP 775146
(CAS: 702680-17-9)

CP 775146 is a high affinity PPARα agonist and show hypolipidemic activity in vivo.

CAS 1675-54-3 BADGE

BADGE
(CAS: 1675-54-3)

BADGE is a PPARγ antagonist with selectivity over PPARδ and PPARα. It inhibits adipocyte differentiation, and induces apoptosis in cancer cells. BADGE also exhi...

CAS 213411-83-7 Edaglitazone

Edaglitazone
(CAS: 213411-83-7)

Edaglitazone is a potent and selective PPARγ agonist (EC50 = 35.6 and 1053 nM for PPARγ and PPARα cofactor recruitment respectively). Edaglitazone enhances insu...

CAS 353280-43-0 S26948

S26948
(CAS: 353280-43-0)

S26948 is a selective PPARγ agonist (EC50 = 8.83 nM). It promotes normal adipocyte differentiation and exhibits a lipid-lowering effect, decreasing the risk of ...

CAS 313516-66-4 T0070907

T0070907
(CAS: 313516-66-4)

T0070907 was identified as a potent and selective PPARgamma antagonist. T0070907 blocked PPARgamma function in both cell-based reporter gene and adipocyte diffe...

CAS 1133819-87-0 MSDC-0602

MSDC-0602
(CAS: 1133819-87-0)

MSDC-0602 is an insulin sensitizer that has the potential to treat diabetes and other inflammatory diseases. It exhibits low affinity for binding and activation...

CAS 199113-98-9 Balaglitazone

Balaglitazone
(CAS: 199113-98-9)

The Rs for the separations were 3.5 for balaglitazone enantiomers, 3.5 for pioglitazone enantiomers, and 3.7 for rosiglitazone. The squared correlation coeffici...

CAS 79558-09-1 L-165041

L-165041
(CAS: 79558-09-1)

L-165041 is a cell permeable PPARδ agonist which induces adipocyte differentiation in NIH-PPARδ cells. It displays more than 100-fold selectivity for both mouse...

CAS 1014691-61-2 GSK0660

GSK0660
(CAS: 1014691-61-2)

GSK0660 is a selective PPARδ antagonist. GSK0660 blocks the effect of TNFα on the expressions of cytokines involved in leukocyte recruitment, including CCL8, CC...

CAS 223132-38-5 Inolitazone dihydrochloride

Inolitazone dihydrochloride
(CAS: 223132-38-5)

In vitro, the IC50 for growth inhibition is approximately 0.8 nM while anaplastic thyroid carcinoma (ATC) tumor growth was inhibited three- to fourfold in nude ...

Chemical Structure

CAS 188591-46-0 GSK-3787

Quick Inquiry

Verification code

Featured Items