추천 제품
Quality Level
분석
≥98% (HPLC)
양식
powder
색상
white to beige
solubility
DMSO: >5 mg/mL
저장 온도
2-8°C
SMILES string
CC(=O)Nc1nc(C)c(s1)S(=O)(=O)Nc2ccc(cc2)C(O)(C(F)(F)F)C(F)(F)F
InChI
1S/C15H13F6N3O4S2/c1-7-11(29-12(22-7)23-8(2)25)30(27,28)24-10-5-3-9(4-6-10)13(26,14(16,17)18)15(19,20)21/h3-6,24,26H,1-2H3,(H,22,23,25)
InChI key
OZBSSKGBKHOLGA-UHFFFAOYSA-N
애플리케이션
SR1001 has been used as retinoic-acid receptor (RAR)-related orphan nuclear receptor gamma (RORγt) inhibitor to study its effects on interleukin 17 (IL-17) expression in itch cells , as a RAR-related orphan receptor alpha (RORα)- inhibitor to study its effects on RORα-dependent transcription of glucose-6-phosphatase (G6Pase) .
SR1001 has been used for inhibiting retinoid-related orphan receptor-γ t (RORγT) activation in Itch−/− mice.
생화학적/생리학적 작용
SR1001 is an antagonist of the nuclear retinoic acid receptor-related orphan receptors RORα and RORγt with no activity at LXR or RORβ. RORα and RORγt are essential for the development of TH17 cells, T-helper cells that produce interleukin-17 and have recently been shown to have pathological roles in various autoimmune diseases. SR1001 binds to the ligand-binding domain of RORα and RORγt to decrease affinity of the receptor for coactivators and increse affinity for co-repressors. It inhibited the differentiation and function of TH17 cells and suppressed the clinical severity of a mouse model of multiple sclerosis.
특징 및 장점
This compound is featured on the Nuclear Receptors (PPARs) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
신호어
Warning
유해 및 위험 성명서
Hazard Classifications
Acute Tox. 4 Oral - Eye Irrit. 2
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
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이미 열람한 고객
Nature immunology, 17(8), 997-1004 (2016-06-21)
Dysregulated expression of interleukin 17 (IL-17) in the colonic mucosa is associated with colonic inflammation and cancer. However, the cell-intrinsic molecular mechanisms by which IL-17 expression is regulated remain unclear. We found that deficiency in the ubiquitin ligase Itch led
The cAMP-dependent protein kinase downregulates glucose-6-phosphatase expression through ROR$\alpha$ and SRC-2 coactivator transcriptional activity
Molecular and Cellular Endocrinology, 419(8) (2016)
Molecular and cellular endocrinology, 419, 92-101 (2015-10-13)
Fasting hormones activate the cAMP/PKA signaling pathway and stimulate expression of hepatic gluconeogenic enzymes including glucose-6-phosphatase (G6Pase). Previously it was shown that steroid receptor coactivator 2 (SRC-2) knock-out mice exhibit fasting hypoglycemia and that SRC-2 coactivates RAR-related orphan receptor alpha
Journal of leukocyte biology, 100(1), 213-222 (2016-04-02)
IL-6 and IL-23 (IL-6/23) induce IL-17A (IL-17) production by a subpopulation of murine and human neutrophils, resulting in autocrine IL-17 activation, enhanced production of reactive oxygen species, and increased fungal killing. As IL-6 and IL-23 receptors trigger JAK1, -3/STAT3 and
Itch inhibits IL-17-mediated colon inflammation and tumorigenesis by ROR-gammat ubiquitination
Nature Immunology, 17(8), 997-997 (2016)
문서
Peroxisome proliferator activated receptors (PPARs) are ligand-activated transcription factors related to hormone receptors, influencing gene expression.
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