2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage
  3. ROR PPAR LXR
  4. SR-1903

SR-1903 is an inverse agonist of RORγ and PPARγ (IC50 of ∼100 nM and 209 nM for RORγ and PPARγ, respectively) and a LXR agonist. SR-1903 exhibits anti-inflammatory and anti-diabetic efficacy in collagen-induced arthritis and diet-induced obesity mouse models.

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SR-1903 Chemical Structure

SR-1903 Chemical Structure

CAS No. : 1414248-06-8

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SR-1903 Related Antibodies

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Description

SR-1903 is an inverse agonist of RORγ and PPARγ (IC50 of ∼100 nM and 209 nM for RORγ and PPARγ, respectively) and a LXR agonist. SR-1903 exhibits anti-inflammatory and anti-diabetic efficacy in collagen-induced arthritis and diet-induced obesity mouse models[1].

IC50 & Target[1]

RORγ

~100 nM (IC50)

PPARγ

209 nM (IC50)

In Vitro

SR1903 (10 μM) attenuates LPS (HY-D1056) signaling in macrophages, with suppression of TREM-1 gene expression[1].
SR1903 increases expression of LXR target genes, including genes involved in macrophage cholesterol efflux (ABCG1 and SCD) and lipid metabolism (ACACA and FASN) in macrophage RAW264.7[1].

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

SR-1903 Related Antibodies
In Vivo

SR1903 (20 mg/kg, i.p., twice-a-day for a total of 16 days) ameliorates arthritic symptoms and prevents thymocyte loss in collagen-induced arthritis (CIA) mice[1].
SR1903 (20 mg/kg, i.p., 14 days) improves metabolic parameters and protects against obesity-associated thymic degeneration in diet-induced obese (DIO) mice[1].

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

Animal Model: Collagen-induced arthritis (female DBA/1J mice were injected with chicken type II collagen on day 1, and then each animal received a boost injection of collagen on day 21)[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection (i.p.), twice-a-day for a total of 16 days
Result: Demonstrated a reduction in arthritis clinic score at the conclusion of the study (day 34).
Did not cause enlargement of the liver.
Had enhanced thymocyte differentiation and survival compared to mice treated with either the selective LXR agonist GW3965 or the dual LXR agonist/RORγ inverse agonist T0901317.
Animal Model: Diet-induced obese (DIO) mouse (Male, 22 weeks of age, fed a high fat diet (60% kCal % fat))[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection (i.p.), 14 days
Result: Improved fasting glucose levels and reduced total cholesterol and low density lipoprotein (LDL).
Improved both fasting and fed insulin levels.
Showed 15% weight loss and 17% reduction in fat mass after 14 days.
Reduced food intake.
Reduced leptin resistance and repressed Socs3 (suppressor of cytokine signaling-3) expression.
Molecular Weight

523.51

Formula

C27H27F6N3O
CAS No.
SMILES

OC(C(F)(F)F)(C(F)(F)F)C1=CC=C(C2=CC=C(CN3CCN(CC4=CC=NC=C4)CC3)C=C2C)C=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SR-1903 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SR-19031414248-06-8SR1903SR 1903RORPPARLXRRAR-related orphan receptorPeroxisome proliferator-activated receptorsLiver X receptorAnti-inflammatoryArthritisObesityAntidiabeticRAW264.7DBA/1JDIO.Inhibitorinhibitorinhibit

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