1. Metabolic Enzyme/Protease
  2. ROR
  3. SR3335

SR3335 (Synonyms: ML 176)

Cat. No.: HY-14413 Purity: 99.43%
Handling Instructions

SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a Ki of 220 nM.

For research use only. We do not sell to patients.

SR3335 Chemical Structure

SR3335 Chemical Structure

CAS No. : 293753-05-6

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10 mM * 1 mL in DMSO USD 112 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 112 In-stock
Estimated Time of Arrival: December 31
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5 mg USD 102 In-stock
Estimated Time of Arrival: December 31
10 mg USD 182 In-stock
Estimated Time of Arrival: December 31
50 mg USD 792 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
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Based on 4 publication(s) in Google Scholar

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Description

SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a Ki of 220 nM[1][2].

IC50 & Target

Ki: 220 nM (RORα)[1]

In Vitro

SR3335 is a selective RORα partial inverse agonist. In a biochemical radioligand binding assay using [3H]25-hydroxycholesterol as a label it is clear that unlabeled SR3335 dose-dependently competes for binding to the RORα LBD. The Ki is calculated as 220 nM using the Cheng-Prusoff equation. 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[1].
SR3335 suppresses the expression of endogenous RORα target genes in HepG2 cells that are involved in hepatic gluconeogenesis including glucose-6-phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK)[2].
SR3335 also blocks IL-25 and IL-33-induced ILC2 proliferation and IL-13 production ex vivo[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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[1].
SR3335 (15 mg/kg/day; ip for 7 days) reduces rhinovirus (RV)-induced lung ILC2s in immature mice (RV infection of 6-day-old BALB/c mice)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

405.34

Formula

C₁₃H₉F₆NO₃S₂

CAS No.
SMILES

O=S(C1=CC=CS1)(NC2=CC=C(C(C(F)(F)F)(C(F)(F)F)O)C=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (246.71 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4671 mL 12.3353 mL 24.6706 mL
5 mM 0.4934 mL 2.4671 mL 4.9341 mL
10 mM 0.2467 mL 1.2335 mL 2.4671 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.17 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.17 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.17 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

HEK293 cells are maintained in Dulbecco’s modified Eagle’s medium (DMEM) supplemented with 10% fetal bovine serum at 37°C under 5% CO2. HepG2 cells are maintained and routinely propagated in minimum essential medium supplemented with 10% fetal bovine serum at 37°C under 5% CO2. 24 h prior to transfection, cells are plated in 96-well plates at a density of 15×103 cells/well. Transfections are performed using LipofectamineTM 2000. 16 h post-transfection, the cells are treated with vehicle or SR3335. 24 h post-treatment, the luciferase activity is measured using the Dual-GloTM luciferase assay system. The values indicated represent the means±S.E. from four independently transfected wells. The experiments are repeated at least three times[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
30 week old Diet induced obese (DIO) C57BL/6 male mice are purchased from Jackson Laboratories that are maintained on a 65% Kcal high-fat diet from weaning. DIO mice are treated twice per day (07:00h and 18:00h) with 15 mg/kg SR3335 or vehicle for 6 days i.p. Pyruvate tolerance test is conducted on day 6 of the treatment. Food is removed from mice in the morning after SR3335 injection, fasted for 6 hours and the pyruvate tolerance test is conducted at 13:00h. Time 0 blood glucose is measured taken from the tail nip and the pyruvate challenge is initiated by injection of 2g/kg of pyruvate i.p. followed by measuring blood glucose at 15, 30 and 60 min following the injection. Blood glucose is measured by one touch ultra glucose-meter.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

SR3335ML 176SR 3335SR-3335ML176ML-176RORRAR-related orphan receptorInhibitorinhibitorinhibit

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SR3335
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