Product Introduction:
GW0742 is a high affinity PPAR-β/δ agonist reduces lung inflammation induced by bleomycin instillation in mice.
A high throughput screening campaign was conducted to identify small molecules with the ability to inhibit
the interaction between the vitamin DÂ receptor (VDR) and steroid receptor coactivator.
These inhibitors represent novel molecular probes to modulate gene regulation mediated by VDR. The peroxisome proliferator-activated receptor δ (PPARδ) agonist GW0742 was among the identified VDR-coactivator inhibitors and has been characterized herein as a pan nuclear receptor antagonist at concentrations higher than 12.1 µM.
The highest antagonist activity for GW0742 was found for VDR and the androgen receptor (AR). Surprisingly, GW0742 behaved as PPAR agonist/antagonist activating transcription at lower concentration and inhibiting this effect at higher concentrations. A unique spectroscopic property of GW0742 was identified as well. In the presence of rhodamine-derived molecules, GW0742+ increased fluorescence intensity and fluorescence polarization at an excitation wavelength of 595 nm and emission wavelength of 615 nm in a dose dependent manner.
The GW0742-inhibited NR-coactivator binding resulted in a reduced expression of five different NR target genes in LNCaP cells in the presence of agonist. Especially VDR target genes CYP24A1, IGFBP-3 and TRPV6 were negatively regulated by GW0742. GW0742 is the first VDR ligand inhibitor lacking the secosteroid structure of VDR ligand antagonists. Nevertheless, the VDR-meditated downstream process of cell differentiation was antagonized by GW0742 in HL-60 cells that were pretreated with the endogenous VDR agonist 1,25-dihydroxyvitamin D3.
Function:
ENDUROBOL is a selective agonist ( activator ) of the PPARδ receptor . It displays high affinity ( Ki = 1 nM ) and potency ( EC50 = 1 nM ) for PPARδ with > 1000 fold selectivity over PPARα and PPARγ .
It activates AMP-activated protein kinase and stimulates glucose uptake in skeletal muscle tissue , and GW 501516 has been demonstrated to reverse metabolic abnormalities in obese men with pre-diabetic metabolic syndrome , most likely by stimulating fatty acid oxidation . It has been proposed as a potential treatment for obesity and related conditions , especially when used in conjunction with a synergistic compound AICAR , as the combination has been shown to significantly increase exercise endurance in human .
Product Name: GW0742, GW610742
CAS: 317318-84-6
Molecular Formula:C21H17F4NO3S2
Formula Weight:471.5
Appearance: White fine powder
Assay: 99% min by HPLC
Related Products:
| Product Name | CAS No. | Purity |
| MK-2866 Ostarine enobosarm GTx-024 |
1202044-20-9 | 99%min |
| MK-677 Ibutamoren Nutrobal |
159752-10-0 | 99%min |
| S4 Andarine S-4 |
401900-40-1 | 99%min |
| GW501516 Cardarine |
317318-70-0 | 99%min |
| LGD-4033 ligandrol Anabolicum |
1165910-22-4 | 99%min |
| LGD-3303 | 1196133-39-7 | 99%min |
| YK-11 | Â 1370003-76-1 | 99%min |
| SR9009 Stenabolic |
1379686-30-2 | 99%min |
| RAD140 Testolone |
1182367-47-0 | 99%min |
| GW0742 | 317318-84-6 | 99%min |
| SR9011 | 1379686-29-9 | 99%min |
| S-23 | 1010396-29-8 | 99%min |
| ACP105 | Â 899821-23-9 | 99%min |
| AC262356 | 870888-46-3 | 99%min |
| aicar | 2627-69-2 | 99%min |
Packing:
| 1kg/bag | N.W 1KG, G.W 1.1KG, packed in an aluminum foil bag |
| 5kg/carton | N.W 1KG, G.W 1.1KG, packed in 5Â aluminum foil bag |
| 25kg/drum | N.W 25KG, G.W 28KG, packed in a cardboard-drum with 2 plastic-bags inside; Drum Size: 510mm high, 360mm diameter |
Shipping:
| BY Express | By Air | By Sea |
| Suitable for for package under 45kgs | Suitable for package more than 45kgs | Suitable for package more than 500kgs |
| about 3~7 days | about 3~7 days | about 7~45 days |
| Door to Door | Port to Port | Port to Port |
| High Cost | Medium Cost | Low Cost |
Our Company:
Wuhan W&Z Biotech Co,.Ltd is a high-tech enterprise which focus on the R&D, production, sales and service of biomedical and large health field. It has strong scientific research strength, modern management system and high-quality marketing team.
W&Z, located in Wuhan, the national key science and education base, cooperates with Wuhan University, Huazhong University of Science and Technology and other well-known universities, forming a good R&D and production team. in our R & D team, there are five experts in fields.
W&Z focus on provide CRO and CMO services for customers on one-stop intermediates, APIs and green technology. We have established modern R&d laboratories in Wuhan Optical Valley, have two partner factories in Shandong and Sichuan. Besides supplying standard products with mature technology, we also do customize under customer`s personalized needs.
We will uphold the quality first, service-oriented, integrity-based purpose, committed to provide more and more, better and better services to the global customers.
Contact Us!
If you have any further questions or need a sample,Please do not hesitate to contact us.
Product Introduction:
GW0742 is a high affinity PPAR-β/δ agonist reduces lung inflammation induced by bleomycin instillation in mice.
A high throughput screening campaign was conducted to identify small molecules with the ability to inhibit
the interaction between the vitamin DÂ receptor (VDR) and steroid receptor coactivator.
These inhibitors represent novel molecular probes to modulate gene regulation mediated by VDR. The peroxisome proliferator-activated receptor δ (PPARδ) agonist GW0742 was among the identified VDR-coactivator inhibitors and has been characterized herein as a pan nuclear receptor antagonist at concentrations higher than 12.1 µM.
The highest antagonist activity for GW0742 was found for VDR and the androgen receptor (AR). Surprisingly, GW0742 behaved as PPAR agonist/antagonist activating transcription at lower concentration and inhibiting this effect at higher concentrations. A unique spectroscopic property of GW0742 was identified as well. In the presence of rhodamine-derived molecules, GW0742+ increased fluorescence intensity and fluorescence polarization at an excitation wavelength of 595 nm and emission wavelength of 615 nm in a dose dependent manner.
The GW0742-inhibited NR-coactivator binding resulted in a reduced expression of five different NR target genes in LNCaP cells in the presence of agonist. Especially VDR target genes CYP24A1, IGFBP-3 and TRPV6 were negatively regulated by GW0742. GW0742 is the first VDR ligand inhibitor lacking the secosteroid structure of VDR ligand antagonists. Nevertheless, the VDR-meditated downstream process of cell differentiation was antagonized by GW0742 in HL-60 cells that were pretreated with the endogenous VDR agonist 1,25-dihydroxyvitamin D3.
Function:
ENDUROBOL is a selective agonist ( activator ) of the PPARδ receptor . It displays high affinity ( Ki = 1 nM ) and potency ( EC50 = 1 nM ) for PPARδ with > 1000 fold selectivity over PPARα and PPARγ .
It activates AMP-activated protein kinase and stimulates glucose uptake in skeletal muscle tissue , and GW 501516 has been demonstrated to reverse metabolic abnormalities in obese men with pre-diabetic metabolic syndrome , most likely by stimulating fatty acid oxidation . It has been proposed as a potential treatment for obesity and related conditions , especially when used in conjunction with a synergistic compound AICAR , as the combination has been shown to significantly increase exercise endurance in human .
Product Name: GW0742, GW610742
CAS: 317318-84-6
Molecular Formula:C21H17F4NO3S2
Formula Weight:471.5
Appearance: White fine powder
Assay: 99% min by HPLC
Related Products:
| Product Name | CAS No. | Purity |
| MK-2866 Ostarine enobosarm GTx-024 |
1202044-20-9 | 99%min |
| MK-677 Ibutamoren Nutrobal |
159752-10-0 | 99%min |
| S4 Andarine S-4 |
401900-40-1 | 99%min |
| GW501516 Cardarine |
317318-70-0 | 99%min |
| LGD-4033 ligandrol Anabolicum |
1165910-22-4 | 99%min |
| LGD-3303 | 1196133-39-7 | 99%min |
| YK-11 | Â 1370003-76-1 | 99%min |
| SR9009 Stenabolic |
1379686-30-2 | 99%min |
| RAD140 Testolone |
1182367-47-0 | 99%min |
| GW0742 | 317318-84-6 | 99%min |
| SR9011 | 1379686-29-9 | 99%min |
| S-23 | 1010396-29-8 | 99%min |
| ACP105 | Â 899821-23-9 | 99%min |
| AC262356 | 870888-46-3 | 99%min |
| aicar | 2627-69-2 | 99%min |
Packing:
| 1kg/bag | N.W 1KG, G.W 1.1KG, packed in an aluminum foil bag |
| 5kg/carton | N.W 1KG, G.W 1.1KG, packed in 5Â aluminum foil bag |
| 25kg/drum | N.W 25KG, G.W 28KG, packed in a cardboard-drum with 2 plastic-bags inside; Drum Size: 510mm high, 360mm diameter |
Shipping:
| BY Express | By Air | By Sea |
| Suitable for for package under 45kgs | Suitable for package more than 45kgs | Suitable for package more than 500kgs |
| about 3~7 days | about 3~7 days | about 7~45 days |
| Door to Door | Port to Port | Port to Port |
| High Cost | Medium Cost | Low Cost |
Our Company:
Wuhan W&Z Biotech Co,.Ltd is a high-tech enterprise which focus on the R&D, production, sales and service of biomedical and large health field. It has strong scientific research strength, modern management system and high-quality marketing team.
W&Z, located in Wuhan, the national key science and education base, cooperates with Wuhan University, Huazhong University of Science and Technology and other well-known universities, forming a good R&D and production team. in our R & D team, there are five experts in fields.
W&Z focus on provide CRO and CMO services for customers on one-stop intermediates, APIs and green technology. We have established modern R&d laboratories in Wuhan Optical Valley, have two partner factories in Shandong and Sichuan. Besides supplying standard products with mature technology, we also do customize under customer`s personalized needs.
We will uphold the quality first, service-oriented, integrity-based purpose, committed to provide more and more, better and better services to the global customers.
Contact Us!
If you have any further questions or need a sample,Please do not hesitate to contact us.
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