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Merck
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安全性情報

SML0322

Sigma-Aldrich

SR1001

≥98% (HPLC)

別名:

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

実験式（ヒル表記法）:
C15H13F6N3O4S2
CAS番号:
1335106-03-0
分子量:
477.40
MDL番号:
MFCD23160036
UNSPSCコード:
12352200
PubChem Substance ID:
329825327
NACRES:
NA.77

品質水準

100

アッセイ

≥98% (HPLC)

フォーム

powder

色

white to beige

溶解性

DMSO: >5 mg/mL

保管温度

2-8°C

SMILES記法

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

関連するカテゴリー

アプリケーション

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.

生物化学的／生理学的作用

SR1001 is a RORα/RORγt antagonist with no activity at LXR or RORβ; suppressor of TH17 cell differentiation and autoimmunity.
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.

特徴および利点

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.

ピクトグラム

Exclamation mark
GHS07

シグナルワード

Warning

危険有害性情報

H302,H319

危険有害性の分類

Acute Tox. 4 Oral - Eye Irrit. 2

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable

適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

Jan Code

SML0322-VAR:
SML0322-BULK:
SML0322-25MG:
SML0322-5MG:

最新バージョンのいずれかを選択してください：

試験成績書（COA）

Lot/Batch Number
085M4609V
084M4616V
042M4609V

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Slide 1 of 5

1 of 5

SR9011 ≥98% (HPLC)

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

ノビレチン ≥97%

Sigma-Aldrich

N1538

ノビレチン

エルゴステロール ≥75%

Sigma-Aldrich

E6510

エルゴステロール

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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資料

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.

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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