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SML0322

Sigma-Aldrich

SR1001

≥98% (HPLC)

Synonim(y):

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

Wzór empiryczny (zapis Hilla):
C15H13F6N3O4S2
Numer CAS:
1335106-03-0
Masa cząsteczkowa:
477.40
Numer MDL:
MFCD23160036
Kod UNSPSC:
12352200
Identyfikator substancji w PubChem:
329825327
NACRES:
NA.77

Próba

≥98% (HPLC)

Postać

powder

kolor

white to beige

rozpuszczalność

DMSO: >5 mg/mL

temp. przechowywania

2-8°C

ciąg SMILES

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)

Klucz InChI

OZBSSKGBKHOLGA-UHFFFAOYSA-N

Zastosowanie

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.

Działania biochem./fizjol.

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.

Cechy i korzyści

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.
This page may contain text that has been machine translated.

Piktogramy

Exclamation mark
GHS07

Hasło ostrzegawcze

Warning

Zwroty wskazujące rodzaj zagrożenia

H302,H319

Klasyfikacja zagrożeń

Acute Tox. 4 Oral - Eye Irrit. 2

Kod klasy składowania

11 - Combustible Solids

Klasa zagrożenia wodnego (WGK)

WGK 3

Temperatura zapłonu (°F)

Not applicable

Temperatura zapłonu (°C)

Not applicable

Certyfikaty analizy (CoA)

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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

Ergosterol ≥75%

Sigma-Aldrich

E6510

Ergosterol

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)
Andre Madsen et al.
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
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.
Itch inhibits IL-17-mediated colon inflammation and tumorigenesis by ROR-gammat ubiquitination
Kathania M, et al.
Nature Immunology, 17(8), 997-997 (2016)
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Produkty

Nuclear Receptors: PPARs

Peroxisome proliferator activated receptors (PPARs) are ligand-activated transcription factors related to hormone receptors, influencing gene expression.

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