SR 1001
SR 1001 Basic information
- Product Name:
- SR 1001
- Synonyms:
-
- SR 1001
- SR1001,N-{4-Methyl-5-[4-(2,2,2-trifluoro-1-hydroxy-1-trifluoroMethyl-ethyl)-phenylsulfaMoyl]-thiazol-2-yl}-acetaMide
- N-(5-(N-(4-(1,1,1,3,3,3-Hexafluoro-2-hydroxypropan-2-yl)phenyl)sulphamoyl)-4-methylthiazol-2-yl)acetamide
- N-(5-{[4-(1,1,1,3,3,3-Hexafluoro-2-hydroxy-2-propanyl)phenyl]sulfamoyl}-4-methyl-1,3-thiazol-2-yl)acetamide
- N-[4-Methyl-5-[[[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]amino]sulfonyl]-2-thiazolylacetamide
- SR-1001;SR 1001
- Acetamide, N-[4-methyl-5-[[[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]amino]sulfonyl]-2-thiazolyl]-
- SR1001 >=98% (HPLC)
- CAS:
- 1335106-03-0
- MF:
- C15H13F6N3O4S2
- MW:
- 477.4
- Mol File:
- 1335106-03-0.mol
SR 1001 Chemical Properties
- Density
- 1.640±0.06 g/cm3(Predicted)
- storage temp.
- Sealed in dry,2-8°C
- solubility
- DMSO: >5mg/mL
- pka
- 5.90±0.50(Predicted)
- form
- powder
- color
- white to beige
- 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.
SR 1001 Usage And Synthesis
Description
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
Uses
SR 1001 is a selective RORc inverse agonist.
Definition
ChEBI: SR 1001 is a sulfonamide.
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
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