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ROR

The RAR-related orphan receptors (RORs) are members of the nuclear receptor family of intracellular transcription factors. There are three forms of ROR, ROR-α, -β, and -γ and each is encoded by a separate gene RORA, RORB, and RORC respectively. The RORs are somewhat unusual in that they appear to bind as monomers to hormone response elements as opposed to the majority of other nuclear receptors which bind as dimers. They bind to DNA elements called ROR response elements (RORE).

Nobiletin
T2834478-01-3
Nobiletin (Hexamethoxyflavone) is a natural polymethoxylated flavone isolated from citrus peels with anti-inflammatory and anti-tumor activities. Nobiletin is practically insoluble (in water) and an extremely weak acidic compound (based on its pKa).
  • $52
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Cholesterol
T076057-88-5
Cholesterol (cholesteryl alcohol) is a natural product that is the major sterol in mammals and an agonist of estrogen-related receptor α (ERRα). Cholesterol is widely found in the cell membranes of animals and is also used in the synthesis of several important hormones and bile acids.
  • $45
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3-Oxo-5β-cholanoic acid
T135021553-56-6
3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid) is a bile acid metabolite that inhibits TH17 cell differentiation by directly binding to the transcription factor RORγt with a Kd of 1.13 μM.
  • $41
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Melatonin
T165973-31-4
Melatonin (Melatonine) is a natural hormone secreted by the pineal gland that activates melatonin receptors. Melatonin is a hormone that regulates the biological clock and also has antioxidant and anti-inflammatory activities.
  • $31
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Neoruscogenin
T3S125117676-33-4
1. Neoruscogenin represents a universal pharmacological tool for RORα research due to its specific selectivity profile versus other nuclear receptors.
  • $59
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GSK805
T73881426802-50-7
GSK805 is a potent, orally bioavailable and CNS-penetrant RORγt inhibitor.
  • $51
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T0901317
T6690293754-55-9
T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively; it inhibits nuclear factor κB (NF κB).
  • $32
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SR1001
T51631335106-03-0
SR 1001 is an inverse agonist for RORα RORγ (Kis: 172 111 nM).
  • $34
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Cedirogant
T96352055496-11-0
Cedirogant (ABBV-157) is an orally active, retinoid-related orphan receptor-γt (RORγt) inverse agonist used in psoriasis studies.
  • $89
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RORγt inverse agonist 13
T96232170477-75-3
RORγt inverse agonist 13 (Compound 3i) is a potent, orally active, and selective inverse agonist for RORγt with an IC50 of 63.8 nM, exhibiting improved drug-like properties[1].
  • $48
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SR3335
T5160293753-05-6
SR3335 (ML 176) is a selective inverse agonist of RORα that competitively inhibits the binding of 25-hydroxycholesterol to the ligand binding domain (Ki: 220 nM).
  • $31
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SR0987
T4670303126-97-8
SR0987 is a RORγt agonist,
  • $35
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Cabozantinib hydrochloride
T51641817759-42-4
Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).
  • $37
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SR1078
T45941246525-60-9
SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR)α γ.
  • $35
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ML 209
T375871334526-14-5In house
ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50= 1.1 μM in a reporter assay).1It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50= 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated na?ve cord blood human CD4+T cells into Th17 T helper cells.
  • $93
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RORγt Inverse agonist 6
T127531887161-80-9
RORγt Inverse agonist 6 is an agonist of RORγt inverse. RORγt Inverse agonist 6 can be used in research on Th17-driven autoimmune diseases.
  • $56
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XY101
T133622349368-16-5In house
XY101 is a selective, metabolically stable and orally available agonist of RORγ inverse(IC50 of 30 nM and a Kd of 380 nM).
  • $79
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S18-000003
T168322068119-11-7
S18-000003 is an effective orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t inhibitor (IC50: 29 nM). S18-000003 inhibits IL-17 production.
  • $52
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TMP-778
T13172L11422171-08-1
TMP-778 is a selective inverse agonist of RORγt.
  • $223
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XY018
T242131873358-87-2
XY018 is an orally available, selective and highly effective ROR-γ antagonist with antitumor activity, inhibits ROR-γ activity, inhibits tumor cell growth, and can be used to study drug-resistant prostate cancer.
  • $38
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GSK2981278
T40501474110-21-8
GSK2981278 (ROR gama modulator 1) is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma).
  • $30
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Bevurogant
T392501817773-66-2
Bevurogant is an antagonist of RORγt receptor and can be used in studies about the treatment of chronic inflammatory diseases.
  • $44
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Cintirorgon
TQ00072055536-64-4
Cintirorgon (LYC-55716) is a selective, oral agonist of RORγ, modulating gene expression in RORγ-expressing T lymphocyte immune cells.
  • $77
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SR2211
T169291359164-11-6
SR2211 is a specific modulator and an inverse agonist of RORγ(IC50 = 320 nM, Ki = 105 nM).
  • $44
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