SR1001 | RORα gamma inverse agonist

CAS:
1335106-03-0
Catalog Number:
10-1290
Activity:
RORα inverse 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
Molecular Weight:
477.39
Molecular Formula:
C15H13F6N6O4S2
Solubility:
Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 40 mg/ml).
Physical Properties:
Pale beige solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 2 years from date of purchase as supplied. Protect from moisture. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT

Available Options

size :PriceQuantity 
5 mg$80.00
25 mg$320.00

SR1001 (1335106-03-0) is 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 activity.1 SR-1001 inhibits the development of murine TH17 cells2 and suppresses the expression of cytokines1. Suppresses insulitis and prevents hyperglycemia in a type 1 diabetes mouse model.3 Protects against pathologic neovascularization in various mouse models of retinopathy.4 Active in vivo

References/Citations:

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

CAS:
1335106-03-0
Catalog Number:
10-1290
Activity:
RORα inverse 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
Molecular Weight:
477.39
Molecular Formula:
C15H13F6N6O4S2
Solubility:
Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 40 mg/ml).
Physical Properties:
Pale beige solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 2 years from date of purchase as supplied. Protect from moisture. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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