| Catalog | Description | Size | Price (USD) | Qty |
|---|---|---|---|---|
| GBM-1290-5MG | SR-1001 | 5mg | $168.00 | |
| GBM-1290-25MG | SR-1001 | 25mg | $672.00 |
| Bioassays Specification | |
| Bio-Activity | RORag agonist |
| Chemical Name | N-(5-(N-(4-(1,1,1,3,3,3-Hexafluoro-2-hydroxypropan-2-yl)phenyl)sulphamoyl)-4-methylthiazol-2-yl)acetamide |
| Function / Pharmacology | A high affinity synthetic ligand for both RORα and RORγt acting as an inverse agonist. It binds specifically to the ligand-binding domain, inducing a conformational change which leads to diminished affinity for co-activators and increased affinity for co-repressors resulting in suppression of transcriptional activity1. It inhibits the development of murine TH17 cells2 and suppresses the expression of cytokines1. Suppresses insulitis and prevents hyperglycemia in a type 1 diabetes mouse model3. Protects against pathologic neovascularization in various mouse models of retinopathy4. Active in vivo |
| CAS# | 1335106-03-0 |
| MW | 477.39 |
| Molecular Formula | C15H13F6N6O4S2 |
| Solubility | Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 40 mg/ml). |
| Supplied | powder |
| Storage as supplied | -20°C |
| Ship temp | Ambient |
| References | 1) Solt et al. (2011) Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature, 472 491 2) Beurel et al. (2013) Inflammatory T helper 17 cells promote depression-like behavior in mice; Biol. Psychiatry, 73 622 3) Solt et al. (2015) ROR inverse agonist suppresses insulitis and prevents hyperglycemia in a mouse model of type 1 diabetes; Endocrinology, 156 869 4) Sun et al. (2015) Nuclear receptor RORα regulates pathologic retinal angiogenesis by modulating SOCS3-dependent inflammation; Proc. Natl. Acad. Sci. USA, 112 10401 |
| Protein Specification | |
| Purity | >98% |
| Bioassays Specification | |
| Bio-Activity | RORag agonist |
| Chemical Name | N-(5-(N-(4-(1,1,1,3,3,3-Hexafluoro-2-hydroxypropan-2-yl)phenyl)sulphamoyl)-4-methylthiazol-2-yl)acetamide |
| Function / Pharmacology | A high affinity synthetic ligand for both RORα and RORγt acting as an inverse agonist. It binds specifically to the ligand-binding domain, inducing a conformational change which leads to diminished affinity for co-activators and increased affinity for co-repressors resulting in suppression of transcriptional activity1. It inhibits the development of murine TH17 cells2 and suppresses the expression of cytokines1. Suppresses insulitis and prevents hyperglycemia in a type 1 diabetes mouse model3. Protects against pathologic neovascularization in various mouse models of retinopathy4. Active in vivo |
| CAS# | 1335106-03-0 |
| MW | 477.39 |
| Molecular Formula | C15H13F6N6O4S2 |
| Solubility | Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 40 mg/ml). |
| Supplied | powder |
| Storage as supplied | -20°C |
| Ship temp | Ambient |
| References | 1) Solt et al. (2011) Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature, 472 491 2) Beurel et al. (2013) Inflammatory T helper 17 cells promote depression-like behavior in mice; Biol. Psychiatry, 73 622 3) Solt et al. (2015) ROR inverse agonist suppresses insulitis and prevents hyperglycemia in a mouse model of type 1 diabetes; Endocrinology, 156 869 4) Sun et al. (2015) Nuclear receptor RORα regulates pathologic retinal angiogenesis by modulating SOCS3-dependent inflammation; Proc. Natl. Acad. Sci. USA, 112 10401 |
| Protein Specification | |
| Purity | >98% |
