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SR-1001 | ROR alpha gamma inverse agonist

SR-1001 (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 activity1. 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 model3. Protects against pathologic neovascularization in various mouse models of retinopathy4. Active in vivo

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

SR-1001 | 1335106-03-0 | Structure | Supplier

Catalog#  10-1290

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Catalog Number:
RORαγ inverse agonist
Chemical Name:
Molecular Weight:
Molecular Formula:
Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 40 mg/ml).
Physical Properties:
Cream solid
98% by TLC
NMR (Conforms)
Storage Temperature:
Stable for 2 years as supplied. Protect from moisture. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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