|N-[4-[2,2,2-三氟-1-羟基-1-(三氟甲基)乙基]苯基]-2-噻吩磺酰胺|CsnPharm

CAS No.: 293753-05-6

N-(4-(1,1,1,3,3,3-Hexafluoro-2-hydroxypropan-2-yl)phenyl)thiophene-2-sulfonamide Catalog No. CSN18188

Synonyms: ML 176

SR3335 can selectively bind to RORα and competitively inhibit the binding of 25-hydroxycholesterol to the ligand binding domain with Ki of 220 nM.

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实验方案

技术信息

生物活性

描述The RORs have been characterized as constitutively active receptors displaying the ability to activate transcription in the absence of a ligand. The retinoic acid receptor-related orphan receptor α (RORα) is an orphan receptor that has been demonstrated to play an important role in regulation of metabolism ^[3]. SR3335 is a selective RORα inverse agonist that directly binds to RORα with a Ki of 220 nM ^[3]. In a cell-based chimeric receptor Gal4 DNA-binding domain-NR ligand binding domain cotransfection assay, SR3335 significantly inhibits the constitutive transactivation activity of RORα (IC50=480 nM)(partial inverse agonist activity), but has no effect on the activity of LXRα and RORγ ^[3]. Pharmacokinetic studies indicate that SR3335 displays reasonable exposure following an i.p. injection into mice. The ability of SR3335 is assessed to suppress gluconeogenesis using a diet induced obesity (DIO) mouse model where the mice where treated with 15 mg/kg b.i.d., i.p. for 6-days followed by a pyruvate tolerance test. SR3335 treated mice displays lower plasma glucose levels following the pyruvate challenge consistent with suppression of gluconeogenesis. Importantly, mice treated with SR3335 displayed no difference in body weight or food intake after 7-days of treatment with SR3335 ^[3].
作用机制SR3335 is a selective RORα synthetic ligand, directly binds to RORα, but not other RORs, and functions as a selective partial inverse agonist of RORα in cell-based assays.
参考文献

[1] Pasha M. Khan, Bahaa El-Dien M, et al. Small molecule amides as potent ROR-γ selective modulators. Bioorganic & Medicinal Chemistry Letters. 2013, 23 (2):532-536.
[2] Kumar N, Kojetin DJ, et al. Identification of SR3335 (ML-176): a synthetic RORα selective inverse agonist. ACS Chem Biol. 2011 Mar 18;6(3):218-22.
[3] Kumar N, Kojetin DJ, Solt LA, Kumar KG, Nuhant P, Duckett DR, Cameron MD, Butler AA, Roush WR, Griffin PR, Burris TP. Identification of SR3335 (ML-176): a synthetic RORα selective inverse agonist. ACS Chem Biol. 2011 Mar 18;6(3):218-22. doi: 10.1021/cb1002762. Epub 2010 Dec 6. PMID: 21090593; PMCID: PMC3076127.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4671 mL
- 12.3354 mL
- 24.6709 mL
- 5 mM
- 0.4934 mL
- 2.4671 mL
- 4.9342 mL
- 10 mM
- 0.2467 mL
- 1.2335 mL
- 2.4671 mL

技术信息

CAS号

293753-05-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H9F6NO3S2

运输

蓝冰

分子量

405.34

别名

ML 176

溶解度

DMSO	100.0 mg/mL (246.7 mM)

动物实验配方

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N-(4-(1,1,1,3,3,3-Hexafluoro-2-hydroxypropan-2-yl)phenyl)thiophene-2-sulfonamide Catalog No. CSN18188

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