ROR Antagonist

ROR Antagonists (20):

Cat. No.	Product Name	Effect	Purity

HY-10626

T0901317	Antagonist	99.93%
T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα. T0901317 activates FXR with an EC₅₀ of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.

HY-14413

SR3335	Antagonist	98.06%
SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a K_i of 220 nM.

HY-16998

SR2211	Antagonist	99.67%
SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a K_i of 105 nM and an IC₅₀ of ~320 nM.

HY-19770

GSK2981278	Antagonist	99.51%
GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.

HY-112706

PF-06747711	Antagonist	99.86%
PF-06747711 is a potent, selective, and orally active retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) inverse agonist, with an IC₅₀ of 4.1 nM. Anti-skin inflammatory activity.

HY-120384

AZD-0284	Antagonist	99.90%
AZD-0284 is a selective inverse agonist of the nuclear receptor RORγ. AZD-0284 has the potential for plaque psoriasis vulgaris and respiratory tract disorders treatment.

HY-102075A

TMP778	Antagonist	99.99%
TMP778 is a potent and selevtive RORγt inverse agonist, with an IC₅₀ of 7 nM in FRET assay.

HY-117819

TMP920	Antagonist	99.81%
TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC₅₀ of 0.03 μM.

HY-132810

Bevurogant	Antagonist	98.57%
Bevurogant (BI 730357) is a retinoid-related orphan receptor-gamma t (RORγt) antagonist. Bevurogant can be used for the research of chronic inflammatory diseases.

HY-145590

Retezorogant	Antagonist
Retezorogant is a retinoid-related orphan receptor γ (RORγ) antagonist, extracted from patent WO2016093342 A1.

HY-128353

ROR agonist-1	Antagonist
ROR agonist-1 is a potent and orally bioavailable inverse agonist of the retinoic acid receptor-related orphan receptor C2 (RORC2), inhibition of IL-17A production from human primary T_H 17 cells with a pIC₅₀ of 7.5.

HY-111748

RORγt Inverse agonist 2	Antagonist
RORγt Inverse agonist 2 is a selective, orally active RORγt inverse agonist with an EC₅₀ of 119 nM.

HY-130243

RORγt Inverse agonist 6	Antagonist	98.97%
RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.

HY-133128

FM26	Antagonist
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.

HY-128573

RORγt Inverse agonist 3	Antagonist	99.93%
RORγt Inverse agonist 3 is a potent, selective and orally active RORγ inverse agonist, with EC₅₀s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively.

HY-111509

TAK-828F	Antagonist
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).

HY-122737

RORγt Inverse agonist 8	Antagonist
RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC₅₀ of 19 nM for human RORγt-LBD.

HY-155542

RORγ antagonist 1	Antagonist
RORγ antagonist 1 (compound 22), a potent betulinic acid derivative, is an antagonist of RORγ (K_D=0.18 μM). RORγ antagonist 1 exhibits anti-proliferative activity in HPAF-II pancreatic cancer xenograft model. RORγ antagonist 1 inhibits RAS/MAPK and AKT/mTORC1 pathway, and induces caspase-dependent apoptosis in pancreatic cancer cells.

HY-102075B

TMP780	Antagonist	99.51%
TMP780 is an inverse agonist of RORγt with an IC₅₀ of 13 nM. RORγt is a tractable agent target for the treatment of cutaneous inflammatory disorders.

HY-120785A

SR1555 hydrochloride	Antagonist
SR1555 hydrochloride is the hydrochloride salt form of SR1555 (HY-120785). SR1555 hydrochloride is an inverse agonist for retinoic acid receptor-related orphan nuclear receptor γ (RORγ) with an IC₅₀ of 1 μM. SR1555 hydrochloride inhibits the development and function of pro-inflammatory TH17 cell, increases the frequency of anti-inflammatory T regulatory (Treg) cells. SR1555 hydrochloride can be used for research about autoimmune diseases.

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