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The retinoic acid-related orphan receptor (ROR) subgroup of nuclear receptors consists of three members, RORα, -β and -γ (NR1F1-3 or RORA-C). RORs regulate several important physiological processes and have been implicated in a number of pathologies. RORα is critical for cerebellar development and bone formation, while RORβ regulates functions in the brain and retina. RORγ plays a key role in lymph node development and thymopoiesis. Furthermore, both RORα and RORγ are involved in regulating various metabolic pathways, inflammatory responses and immune functions, including Th17 cell differentiation.

The retinoic acid receptor-related orphan receptors α and γ (RORα and RORγ), are key regulators of helper T (Th)17 cell differentiation, which is involved in the innate immune system and autoimmune disorders. RORα/γ are members of the nuclear hormone receptor superfamily, which contains a signature type II zinc finger DNA binding motif and a hydrophobic ligand binding pocket.

Cat. No.	Product Name	CAS No.	Information
H9588	Retezorogant	1950570-48-5	Retezorogant is a retinoid-related orphan receptor γ (RORγ) antagonist.
H9453	Bevurogant	1817773-66-2	Bevurogant is a novel potent retinoid-related orphan receptor-gamma t (RORγt) antagonist.
H8809	Cedirogant	2055496-11-0	Cedirogant is a retinoid-related orphan receptor-γt (RORγt) antagonist with IC50 of value of < 0.1 μM.
H5980	VTP-43742	1802706-04-2	VTP-43742 (Vimirogant, VTP43742) is a highly potent, selective, oral RORγt inverse agonist with IC50 values of 3.7 nM, for the treatment of autoimmune disorders, including multiple sclerosis and psoriasis.
H5979	TMP778	1422053-04-0	TMP778 (TMP-778) is a potent, selective RORγt inhibitor with IC50 of 7 nM in FRET assays and 63 nM in IL-17 promoter assays, with no inverse agonist activity; blocks human Th17 and Tc17 cell differentiation and also acutely modulates IL-17A production and inflammatory Th17-signature gene expression (IL17a, IL17f, IL22, IL26, CCR6, and IL23) in mature human Th17 effector/memory T cells; inhibits IL-17A production in both human and mouse γδ T cells, also inhibits IL-23-induced IL-17A production; attenuates IMQ-induced skin inflammation in vivo.
H5978	TAK-828F	1854901-94-2	TAK-828F (TAK-828) is a potent, selective, orally available RORγt inverse agonist with binding IC50 of 1.9 nM and reporter IC50 of 6.0 nM, displays excellent selectivity (>5,000-fold) against other ROR isoforms and nuclear receptors; shows robust and dose-dependent inhibition of IL-17A expression after oral administration at 0.3, 1 and 3 mg/kg bid in the mouse IL-23-induced cytokine expression model; also demonstrates dose-dependent inhibition of RORγt regulated gene expression such as IL-17F, IL-22, and IL23 receptor, but no effect against IFN-γ expression; significantly reduces the development of clinical symptoms in mouse experimental autoimmune encephalomyelitis model.
H5977	SR2211	1359164-11-6	SR2211 (SR-2211) is a potent, selective RORγ inverse agonist (Ki=105 nM, IC50=320 nM) that potently inhibits production of IL-17 in cells; displays weak activity for LXRα, has no impact on the transcriptional activity of RORα and FXR; modulates the expression of IL 17A and IL-23R in EL-4 cells, significantly decreases IL-17A and IL-17F production in the BT co-culture system at 0.37-10 uM; reduces inflammatory cytokine production in LPS-stimulated RAW 264.7 cells, suppresses joint inflammation in the CIA experimental model.
H5976	SR1555 hydrochloride	2309312-90-9	SR1555 is a selective RORγ inverse agonist (IC50=1.5 uM) that suppresses T(H)17 cells and stimulates T regulatory cells; SR1555 is devoid of LXR, FXR, and RORα activity, displaces [3H]T0901317 from the ligand binding domain (LBD) of RORγ with IC50 of 1 uM; represses the expression of RORγ while leading to increased expression of FGF21 and adipoQ in pre-adipocyctes, inhibits activation of hormone-sensitive lipase and increased fatty acid oxidation in obese diabetic mice.
H5975	SR1555	1386439-51-5	SR1555 is a selective RORγ inverse agonist (IC50=1.5 uM) that suppresses T(H)17 cells and stimulates T regulatory cells; SR1555 is devoid of LXR, FXR, and RORα activity, displaces [3H]T0901317 from the ligand binding domain (LBD) of RORγ with IC50 of 1 uM; represses the expression of RORγ while leading to increased expression of FGF21 and adipoQ in pre-adipocyctes, inhibits activation of hormone-sensitive lipase and increased fatty acid oxidation in obese diabetic mice.
H5974	SR1001	1335106-03-0	SR1001 is a higly potent, specific, inverse agonist of both RORα and RORγt with binding Ki of 172 and 111 nM, does not binds RORβ and devoid of LXR activity; inhibits the development of murine T(H)17 cells by inhibition of IL-17A gene expression and protein production, also inhibits the expression of cytokines when added to differentiated murine or human T(H)17 cells; modulates the expression of ROR target genes by decreasing coactivator recruitment (SRC2); effectively suppresses the clinical severity of autoimmune disease in mice.

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