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Merck
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SML0322

Sigma-Aldrich

SR1001

≥98% (HPLC)

Szinonimák:

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

Tapasztalati képlet (Hill-képlet):
C15H13F6N3O4S2
CAS-szám:
1335106-03-0
Molekulatömeg:
477.40
MDL-szám:
MFCD23160036
UNSPSC kód:
12352200
PubChem Substance ID:
329825327
NACRES:
NA.77

Minőségi szint

100

Teszt

≥98% (HPLC)

Forma

powder

szín

white to beige

oldhatóság

DMSO: >5 mg/mL

tárolási hőmérséklet

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)

Nemzetközi kémiai azonosító kulcs

OZBSSKGBKHOLGA-UHFFFAOYSA-N

Alkalmazás

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.

Biokémiai/fiziológiai hatások

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.

Tulajdonságok és előnyök

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.

Piktogramok

Exclamation mark
GHS07

Figyelmeztetés

Warning

Figyelmeztető mondatok

H302,H319

Veszélyességi osztályok

Acute Tox. 4 Oral - Eye Irrit. 2

Tárolási osztály kódja

11 - Combustible Solids

WGK

WGK 3

Lobbanási pont (F)

Not applicable

Lobbanási pont (C)

Not applicable

Válasszon a legfrissebb verziók közül:

Analitikai tanúsítványok (COA)

Lot/Batch Number
085M4609V
084M4616V
042M4609V

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Sigma-Aldrich

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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

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

Nuclear Receptors: PPARs

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

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