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.
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] LAURA A. SOLT. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand[J]. Nature, 2011, 472 7344: 491-494. DOI:10.1038/nature10075
[2] ELÉONORE BEUREL Richard S J Laurie E Harrington. Inflammatory T Helper 17 Cells Promote Depression-like Behavior in Mice[J]. Biological Psychiatry, 2013, 73 7: Pages 622-630. DOI:10.1016/j.biopsych.2012.09.021
[3] LAURA A SOLT. ROR inverse agonist suppresses insulitis and prevents hyperglycemia in a mouse model of type 1 diabetes.[J]. Endocrinology, 2015, 156 3: 869-881. DOI:10.1210/en.2014-1677
[4] YE SUN. Nuclear receptor RORα regulates pathologic retinal angiogenesis by modulating SOCS3-dependent inflammation.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2015, 112 33: 10401-10406. DOI:10.1073/pnas.1504387112
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