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SML0410

Sigma-Aldrich

PT-S58

≥98% (HPLC)

Synonym(s):

2-Thiophenecarboxylic acid, 3-[[[4-[(1,1-dimethylethyl)amino]-2-methoxyphenyl]amino]sulfonyl]-, methyl ester

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About This Item

Empirical Formula (Hill Notation):
C17H22N2O5S2
CAS Number:
1356497-92-1
Molecular Weight:
398.50
MDL number:
MFCD22666395
UNSPSC Code:
12352200
PubChem Substance ID:
329825405
NACRES:
NA.77

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL (warmed; clear solution)

storage temp.

2-8°C

SMILES string

COC1=CC(NC(C)(C)C)=CC=C1NS(C2=C(C(OC)=O)SC=C2)(=O)=O

InChI

1S/C17H22N2O5S2/c1-17(2,3)18-11-6-7-12(13(10-11)23-4)19-26(21,22)14-8-9-25-15(14)16(20)24-5/h6-10,18-19H,1-5H3

InChI key

JSUWAIOZKBYWCJ-UHFFFAOYSA-N

Biochem/physiol Actions

PT-S58 is a PPAR β/δ antagonist.
PT-S58 is a PPAR β/δ full antagonist, and a derivative of GSK0660. PT-S58 has a three-fold higher affinity for the receptor than GSK0660 and is a potent inhibitor of agonist-induced target gene expression. Unlike GSK0660, PT-S58 blocks the recruitment co-repressor molecules such as SMRT.

Features and Benefits

This compound is featured on the Nuclear Receptors (Non-Steroids) and Nuclear Receptors (PPARs) pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
072M4605V

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Lara Costantini et al.
Journal of clinical medicine, 9(8) (2020-08-07)
The treatment of solid cancers with pharmacological all-trans retinoic acid (ATRA) concentrations, even if it is a gold standard therapy for the acute promyelocytic leukaemia (APL), is not always effective due to some resistance mechanisms. Here the resistance to ATRA
Jayant Lohakare et al.
The Journal of dairy research, 85(3), 295-302 (2018-06-27)
The hypothesis of the study was that inhibition of PPARβ/δ increases glucose uptake and lactose synthesis in bovine mammary epithelial cells by reducing the expression of the glucose transporter mRNA destabiliser calreticulin. Three experiments were conducted to test the hypothesis
Jie Yu et al.
The Journal of clinical endocrinology and metabolism, 105(9) (2020-07-01)
Implantation is a reproductive bottleneck in women, regulated by fluctuations in ovarian steroid hormone concentrations. However, other nuclear receptor ligands are modifiers of endometrial differentiation leading to successful pregnancy. In the present study we analyzed the effects of peroxisome-proliferator-activated receptor

Articles

Nuclear Receptors: PPARs

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

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