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Merck
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SML0322

Sigma-Aldrich

SR1001

≥98% (HPLC)

Sinonimo/i:

N-(5-(N-(4-(1,1,1,3,3,3-Hexafluoro-2-hydroxypropan-2-yl)phenyl)sulphamoyl)-4-methylthiazol-2-yl)acetamide

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About This Item

Formula empirica (notazione di Hill):
C15H13F6N3O4S2
Numero CAS:
1335106-03-0
Peso molecolare:
477.40
Numero MDL:
MFCD23160036
Codice UNSPSC:
12352200
ID PubChem:
329825327
NACRES:
NA.77

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to beige

Solubilità

DMSO: >5 mg/mL

Temperatura di conservazione

2-8°C

Stringa SMILE

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)
OZBSSKGBKHOLGA-UHFFFAOYSA-N

Applicazioni

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.

Azioni biochim/fisiol

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.

Caratteristiche e vantaggi

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.

Pittogrammi

Exclamation mark
GHS07

Avvertenze

Warning

Indicazioni di pericolo

H302,H319

Classi di pericolo

Acute Tox. 4 Oral - Eye Irrit. 2

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

Cerca il Certificati d'analisi (COA) digitando il numero di lotto/batch corrispondente. I numeri di lotto o di batch sono stampati sull'etichetta dei prodotti dopo la parola ‘Lotto’ o ‘Batch’.

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Sigma-Aldrich

Sigma-Aldrich

SML2067

SR9011

4-P-PDOT ≥98% (HPLC)

Sigma-Aldrich

SML1189

4-P-PDOT

REV-ERB Agonist II, SR9009 The REV-ERB Agonist II, SR9009 controls the biological activity of REV-ERB. This small molecule/inhibitor is primarily used for Biochemicals applications.

Sigma-Aldrich

554726

REV-ERB Agonist II, SR9009

Nobiletin ≥97%

Sigma-Aldrich

N1538

Nobiletin

Patricia R Taylor et al.
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
Mahesh Kathania et al.
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
Madsen A, et al.
Molecular and Cellular Endocrinology, 419(8) (2016)
Zhengguang Wang et al.
Oncotarget, 8(7), 11105-11113 (2017-01-05)
Retinoid-related orphan receptor α (RORα) is a nuclear receptor, which regulates inflammation and immune responses, lipid metabolism and circadian rhythm. Although RORα suppresses breast tumor invasion, it is unknown whether RORα is dysregulated in gastric cancer leading to cellular survival.
Ye Sun et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 31(10), 4492-4502 (2017-06-25)
Pathological proliferation of retinal blood vessels commonly causes vision impairment in proliferative retinopathies, including retinopathy of prematurity. Dysregulated crosstalk between the vasculature and retinal neurons is increasingly recognized as a major factor contributing to the pathogenesis of vascular diseases. Class
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Articoli

Nuclear Receptors (PPARs)

Peroxisome proliferator activated receptors (PPARs) are members of the nuclear hormone receptor superfamily of ligand-activated transcription factors that are related to retinoid, steroid and thyroid hormone receptors.

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