SR-1903 is a RORγ and PPARγ inverse agonist (IC50 for RORγ and PPARγ are ∼100 nM and 209 nM, respectively) and LXR agonist (EC50 is 154 nM). SR-1903 exerts anti-inflammatory and anti-diabetic effects in collagen-induced arthritis and diet-induced obesity mouse models.

Physicochemical Properties

Molecular Formula	C27H27F6N3O
Molecular Weight	523.51
CAS #	1414248-06-8
SMILES	FC(C(C(F)(F)F)(C1C=CC(=CC=1)C1C=CC(=CC=1C)CN1CCN(CC2C=CN=CC=2)CC1)O)(F)F
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	RORγ ~100 nM (IC50); PPARγ 209 nM (IC50)
ln Vitro	SR1903 (10 μM) attenuates LPS signaling and inhibits TREM-1 gene expression in macrophages [1]. SR1903 increases the expression of LXR target genes in RAW264.7 macrophages, including genes involved in macrophage cholesterol efflux (ABCG1 and SCD) and lipid metabolism genes (ACACA and FASN) [1].
ln Vivo	SR1903 (20 mg/kg, ip, twice a day, for 16 days) improves arthritis symptoms and prevents thymocyte loss in mice with collagen-induced arthritis (CIA)[1]. SR1903 (20 mg/kg, ip, for 14 days) improves metabolic parameters in mice with diet-induced obesity (DIO) and protects against obesity-related thymic involution[1].
Animal Protocol	Animal/Disease Models: 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] Doses: 20 mg/kg Route of Administration: Intraperitoneal injection (i.p.), twice-a-day for a total of 16 days Experimental Results: 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/Disease Models: Diet-induced obese (DIO) mouse (Male, 22 weeks of age, fed a high fat diet (60% kCal % fat))[1] Doses: 20 mg/kg Route of Administration: Intraperitoneal injection (i.p.), 14 days Experimental Results: 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.
References	[1]. Unique Polypharmacology Nuclear Receptor Modulator Blocks Inflammatory Signaling Pathways. ACS Chem Biol. 2019, 14(5):1051-1062.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.9102 mL	9.5509 mL	19.1018 mL
	5 mM	0.3820 mL	1.9102 mL	3.8204 mL
	10 mM	0.1910 mL	0.9551 mL	1.9102 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.