| Identification | Back Directory | [Name]
SR 1001 | [CAS]
1335106-03-0 | [Synonyms]
SR 1001
SR-1001;SR 1001
SR1001 >=98% (HPLC)
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
SR1001,N-{4-Methyl-5-[4-(2,2,2-trifluoro-1-hydroxy-1-trifluoroMethyl-ethyl)-phenylsulfaMoyl]-thiazol-2-yl}-acetaMide
Acetamide, N-[4-methyl-5-[[[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]amino]sulfonyl]-2-thiazolyl]- | [Molecular Formula]
C15H13F6N3O4S2 | [MDL Number]
MFCD23160036 | [MOL File]
1335106-03-0.mol | [Molecular Weight]
477.4 |
| Chemical Properties | Back Directory | [density ]
1.640±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO: >5mg/mL | [form ]
powder | [pka]
5.90±0.50(Predicted) | [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. |
| Hazard Information | Back Directory | [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. | [in vivo]
SR1001 effectively suppresses the clinical severity of autoimmune disease in mice. Administration of SR1001 to C57BL/6 mice suppresses the expression of hepatic ROR target genes, Cyp7b1, Rev-erbα, and Serpine 1[1]. SR1001 a RORα inverse agonist eliminats the circadian pattern of expression of citrate synthase mRNA in mice[2]. | [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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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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