sr 1

StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor.

Anti-c-Kit/CD117 Antibody (SR-1) is a mouse IgG2a, κ chimeric antibody that specifically targets human c-Kit/CD117. The recommended isotype control for this antibody is Mouse IgG2a kappa, Isotype Control.

SSR 180 is a potent and subtype-selective α7 agonist with applications in the study of Alzheimer;s disease and schizophrenia.

SR 146131 is a potent and selective agonist of the nonpeptide receptor.

SR 142948-C3-NHMe is the methylated form of SR 142948.

SR 11302 is an inhibitor of activator protein-1 (AP-1).

SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.References1. Chang, M.R., Ciesla, A., Strutzenberg, T.S., et al. Unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem. Biol. 14(5), 1051-1062 (2019). SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity. References1. Chang, M.R., Ciesla, A., Strutzenberg, T.S., et al. Unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem. Biol. 14(5), 1051-1062 (2019).

SR 142948 dihydrochloride is a selective, orally active, non-peptide neurotensin receptor (NT) antagonist, featuring IC50 values of 1.19 nM, 0.32 nM, and 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. It effectively inhibits NT-induced inositol monophosphate formation in HT-29 cells (IC50 = 3.9 nM) and blocks NT-induced hypothermia, analgesia, and steering behavior in vivo. Furthermore, it demonstrates blood-brain barrier permeability, positioning it as a potential tool for psychiatric disorder research [1] [2].

SR 11023, an orally active PPAR γ antagonist, exhibits an IC 50 value of 109 nM and is significant in diabetes research [1].

SR 142948 TFA is an orally active, selective non-peptide neurotensin receptor (NT) antagonist, displaying IC50 values of 1.19 nM in h-NTR1-CHO cells, 0.32 nM in HT-29 cells, and 3.96 nM in adult rat brain. In HT-29 cells, it counteracts NT-induced inositol monophosphate formation with an IC50 of 3.9 nM. It blocks NT-induced hypothermia, analgesia, and turning behavior in vivo and can cross the blood-brain barrier, making it useful for research in psychiatric disorders.

SR 140333 is a NK1 receptor antagonist.

SR 142948 is a neurotensin (NT) receptor antagonist.

SR 1555 is a novel RORγ-specific synthetic ligand.

SR 16584 is a selective α3β4 nAChR antagonist (IC50 = 10.2 μM, Ki = 0.508) that can attenuate the contractile effects induced by epibatidine.

NK3 receptor antagonist

SR 16832 is a dual-site PPARγ inhibitor. It also inhibits the binding of endogenous ligands and transcriptional activity of PPARγ, more effectively than the orthosteric covalent antagonist GW 9662 and T 0070907.

SR 12460 is a lead NBD mimic, inhibiting the interaction between IKKβ and NEMO, suppressing TNF-α and LPS-induced NF-κB activation, and reducing LPS-induced acute pulmonary inflammation in mice.

SR 19881 is a full agonist of ERRγ(EC50 value of 0.39 μM in a binding assay and an EC50 value of 4.7 μM in a cell-based assay).

SSR 146977 hydrochloride is a potent, selective antagonist of the tachykinin NK 3 receptor, and it can be utilized in research on psychiatric disorders and airway inflammation [1].

SR13668 is a potent indole analog derived from indole-3-methanol (I3C), renowned for its natural anti-cancer properties but limited by poor metabolic characteristics. Designed to enhance the anti-cancer efficacy of I3C, SR13668 effectively inhibits Akt activation stimulated by growth factors. It exhibits strong oral anti-cancer activity across various cancer types, demonstrating both high safety and robust inhibitory effects.

GSK864 is an IDH1 mutant inhibitor that inhibits IDH1 mutants R132C, R132H, and R132G, and is used in the study of cardiovascular and oncology diseases.

SR10067 is a potent, selective, and brain-penetrant agonist of Rev-Erbβ (IC50 = 160 nM) and Rev-Erbα (IC50 = 170 nM) with anxiolytic activity.

SR1664 is a potent and selective PPARγ inhibitor with potential antidiabetic activity. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity.

Nelivaptan (SR 149415) is a vasopressin V1b receptor antagonist that can eliminate CHS-induced GE damage and inhibit [3H]AVP binding in a competitive manner.