| Cat.No. | Name | Information |
|---|---|---|
| M7321 | SR 1001 | SR 1001 is a RORα/γ inverse agonist with Ki values of 172 and 111 nM, respectively. |
| M40961 | ESR-114 | ESR-114 is a RORγt inhibitor that can be used in studies related to psoriasis. |
| M40959 | AUR101 | AUR101 is an orally active RORγt inverse agonist for studies related to psoriasis. |
| M31061 | Vimirogant hydrochloride | Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant hydrochloride exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant hydrochloride inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. |
| M29661 | BMS-986251 | BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced models (preclinical models of psoriasis). |
| M29598 | FM26 | FM26 (compound 25) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM. FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells. |
| M29487 | Izumerogant | Izumerogant (IMU-935) is an inverse agonist of retinoid-related orphan receptor-gamma (RORγ). Izumerogant (compound 123) also potently inhibits IL-17A, IL-17F and IFN-γ activity with IC50s <50 nM. |
| M29259 | RORγt modulator 5 | RORγt modulator 5 is a RORγt modulator with a Ki value of <100 nM. RORγt modulator 5 has the potential for inflammatory, metabolic, autoimmune and other diseases mediated by RORy study (WO2017132432A1; compound 2). |
| M29140 | A-9758 | A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation. |
| M29048 | CD12681 | CD12681 (compound 14) is a potent and selective RORγ inverse agonist with IC50 of 19 nM and 10 nM for RORγ GAL4 and CD4-IL-17 cells, respectively. CD12681 decreases the IL-17 inflammatory cell recruitment. CD12681 has the potential for the research of psoriasis. |
| M29017 | JNJ-61803534 | JNJ-61803534 is a potent and orally active RORγt inverse agonist with an IC50 of 9.6 nM. JNJ-61803534 has anti-inflammatory activity. JNJ-61803534 inhibits IL-17A production in human CD4+ T cells under Th17 differentiation conditions. |
| M28975 | XY018 | XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD). |
| M28953 | TAK-828F | TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM). TAK-828F shows excellent RORγt isoforms selectivity (>5000-fold selectivity against human RORα and RORβ). |
| M28800 | GNE-0946 | GNE-0946 is a potent and selective RORγ( RORc) agonist with an EC50 value of 4 nM for HEK-293 cell. |
| M28798 | ARN-6039 | ARN-6039 is an orally available inverse agonist of RORγ for autoimmune demyelinating disease. |
| M28386 | TMP920 | TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM. |
| M28314 | MRL-871 | MRL-871 (compound 3) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 12.7 nM. MRL-871 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells. |
| M28302 | SR1555 | SR1555 is a specific retinoic acid receptor-related orphan nuclear receptor γ (RORγ) inverse agonist with an IC50 value of 1 μM. SR1555 not only inhibits TH17 cell development and function but also increases the frequency of T regulatory cells, as well as inhibits the expression of IL-17. SR1555 can be used for researching autoimmune diseases. |
| M28194 | (±)-ML 209 | (±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphan receptor RORγ antagonist with an IC50 of 1.1 μM. (±)-ML 209 inhibits RORγt transcriptional activity with an IC50 of 300 nM in HEK293t cells. (±)-ML 209 inhibits the transcriptional activity of RORγt, but not RORα in cells. (±)-ML 209 selectively inhibits murine Th17 cell differentiation without affecting the differentiation of naïve CD4+ T cells into other lineages, including Th1 and regulatory T cells. |
| M25373 | Zilovertamab | Zilovertamab (UC-961) is a humanised monoclonal antibody against ROR1 that blocks Wnt5a-induced ROR1 signalling. |
| M21134 | SHR168442 | SHR168442 is a modulator of RORγ with an IC50 value of 0.035 μM. It can be used as a skin-restricted topical compound for the study of psoriasis. |
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