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SML0322

SR1001

Name: SR1001
Brand: SIGMA

≥98% (HPLC), retinoic-acid receptor (RAR)-related orphan nuclear receptor gamma (RORγt) inhibitor, powder

Synonym(s):

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

Empirical Formula (Hill Notation):

C₁₅H₁₃F₆N₃O₄S₂

CAS Number:

1335106-03-0

Molecular Weight:

477.40

UNSPSC Code:

12352200

PubChem Substance ID:

329825327

NACRES:

NA.77

MDL number:

MFCD23160036

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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Product Name

SR1001, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: >5 mg/mL

storage temp.

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

Related Categories

Bioactive Small Molecules

Application

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.

Biochem/physiol Actions

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.

Features and Benefits

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.

pictograms

GHS07

signalword

Warning

hcodes

H302,H319

pcodes

P264 - P280 - P301 + P312 - P305 + P351 + P338 - P337 + P313 - P501

Hazard Classifications

Acute Tox. 4 Oral - Eye Irrit. 2

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Itch inhibits IL-17-mediated colon inflammation and tumorigenesis by ROR-γt ubiquitination.

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)

Itch inhibits IL-17-mediated colon inflammation and tumorigenesis by ROR-gammat ubiquitination

Kathania M, et al.

Nature Immunology, 17(8), 997-997 (2016)

JAK/STAT regulation of Aspergillus fumigatus corneal infections and IL-6/23-stimulated neutrophil, IL-17, elastase, and MMP9 activity.

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

The cAMP-dependent protein kinase downregulates glucose-6-phosphatase expression through RORα and SRC-2 coactivator transcriptional activity.

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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Nuclear Receptors: PPARs

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

Global Trade Item Number

SKU	GTIN
SML0322-5MG	04061832954776
SML0322-25MG	04061832954769

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