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Merck
모든 사진(1)

문서

SML0322

Sigma-Aldrich

SR1001

≥98% (HPLC)

동의어(들):

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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모든 사진(1)

About This Item

실험식(Hill 표기법):
C15H13F6N3O4S2
CAS Number:
1335106-03-0
Molecular Weight:
477.40
MDL number:
MFCD23160036
UNSPSC 코드:
12352200
PubChem Substance ID:
329825327
NACRES:
NA.77

분석

≥98% (HPLC)

형태

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.

픽토그램

Exclamation mark
GHS07

신호어

Warning

유해 및 위험 성명서

H302,H319

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

시험 성적서(COA)

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문서 라이브러리 방문

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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문서

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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