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Orphan

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105

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34

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Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0155
    Nobiletin
    Maximum Cited Publications
    27 Publications Verification

    ROR Reactive Oxygen Species (ROS) Apoptosis Autophagy Neurological Disease Inflammation/Immunology Cancer
    Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis .
    Nobiletin
  • HY-N2148
    Cytosporone B
    10+ Cited Publications

    Csn-B; Dothiorelone G

    Nuclear Hormone Receptor 4A/NR4A Cancer
    Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77/NR4A1 agonist with an EC50 of 0.278 nM.
    Cytosporone B
  • HY-14422
    SR1078
    10+ Cited Publications

    ROR Cancer
    SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription .
    SR1078
  • HY-113962
    7α,25-Dihydroxycholesterol
    3 Publications Verification

    7α,25-OHC

    EBI2/GPR183 Endogenous Metabolite Inflammation/Immunology
    7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells .
    7α,25-Dihydroxycholesterol
  • HY-113342
    7-Ketocholesterol
    5 Publications Verification

    Endogenous Metabolite p38 MAPK Cardiovascular Disease Metabolic Disease
    7-Ketocholesterol is an oxidation product of cholesterol, widely present in atherosclerotic plaques, and has a stronger atherogenic effect than cholesterol. 7-Ketocholesterol can inhibit the rate-limiting enzymes involved in bile acid and cholesterol synthesis, such as cholesterol 7α-hydroxylase and HMG-CoA reductase. 7-Ketocholesterol exhibits pro-inflammatory effects both in vivo and in vitro and can induce cell apoptosis (apoptosis) .
    7-Ketocholesterol
  • HY-162617

    Cannabinoid Receptor Inflammation/Immunology Cancer
    PSB-KK1415 is a selective agonist for human orphan G protein-coupled receptor GPR18, with EC50 of 19.1 nM .
    PSB-KK1415
  • HY-115613
    ML-180
    5 Publications Verification

    SR1848

    Orphan Nuclear Receptor Cancer
    ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist with an IC50 of 3.7 μM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC50>10 μM). ML-180 has the potential for LRH-1-dependent cancers .
    ML-180
  • HY-111492
    DIM-C-pPhOCH3
    1 Publications Verification

    Nuclear Hormone Receptor 4A/NR4A Cancer
    DIM-C-pPhOCH3 is a Nur77 agonist. Nerve growth factor-induced Bα (NGFI-Bα, Nur77) is an orphan nuclear receptor.
    DIM-C-pPhOCH3
  • HY-135572

    Orphan Nuclear Receptor Neurological Disease Cancer
    TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity .
    TLX agonist 1
  • HY-P2210

    GPR171 Metabolic Disease
    BigLEN(mouse) is a potent and selective agonist of orphan G protein-coupled receptor 171 (GPR171), with a Kd of ∼0.5 nM. BigLEN(mouse) can be used to regulate responses associated with food intake and metabolism .
    BigLEN(mouse)
  • HY-156190A

    Orphan Nuclear Receptor Cancer
    NR2F2-IN-1 (free base) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F2-IN-1 (free base) substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F2-IN-1 (free base) directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .
    NR2F2-IN-1 free base
  • HY-P1066

    Apelin Receptor (APJ) HIV Infection
    Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
    Apelin-17(human, bovine)
  • HY-114146

    Orphan GPCR Neurological Disease Metabolic Disease
    CID 1375606 is a surrogate agonist of orphan G protein-coupled receptor GPR27.
    CID 1375606
  • HY-132810

    BI 730357

    ROR Inflammation/Immunology Cancer
    Bevurogant (BI 730357) is a retinoid-related orphan receptor-gamma t (RORγt) antagonist. Bevurogant can be used for the research of chronic inflammatory diseases .
    Bevurogant
  • HY-P1022
    Kisspeptin-54(human)
    3 Publications Verification

    Metastin(human)

    GnRH Receptor Endocrinology Cancer
    Kisspeptin-54(human) (Metastin(human)) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) inhibits tumor metastasis and stimulates the secretion of gonadotropin (LH) and testosterone .
    Kisspeptin-54(human)
  • HY-139534
    ARI-1
    1 Publications Verification

    ROR Apoptosis Akt mTOR PARP Cancer
    ARI-1 is a receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor. ARI-1 blocks the PI3K/AKT/mTOR signaling pathway in a ROR1-dependent manner. ARI-1 upregulates cleaved-PARP and p-P38. ARI-1 induces Apoptosis. ARI-1 has anticancer activity against non-small cell lung cancer .
    ARI-1
  • HY-126037
    (±)-ML 209
    1 Publications Verification

    ROR Inflammation/Immunology
    (±)-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 .
    (±)-ML 209
  • HY-113058

    Endogenous Metabolite Metabolic Disease
    3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
    3-Hydroxyoctanoic acid
  • HY-P1064

    Apelin Receptor (APJ) HIV Infection Cardiovascular Disease Metabolic Disease
    Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
    Apelin-36(human)
  • HY-112706

    ROR Inflammation/Immunology
    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 .
    PF-06747711
  • HY-145627

    BA3021; Anti-ROR2 ADC; CAB-ROR2-ADC

    Antibody-Drug Conjugates (ADCs) Microtubule/Tubulin Cancer
    Ozuriftamab vedotin (BA3021), an antibody-drug conjugate (ADC), is a conditionally active biologic (CAB) anti-receptor tyrosine kinase orphan receptor 2 (ROR2) humanized monoclonal antibody Ozuriftamab (HY-145626) conjugated to VcMMAE (HY-15575). Ozuriftamab vedotin has antitumor activities .
    Ozuriftamab vedotin
  • HY-163087

    Orphan GPCR Neurological Disease Metabolic Disease
    PT-91 is an agonist of GPR27. PT-91 exhibits high metabolic stability and brain exposure in mice .
    PT-91
  • HY-18618A
    SB-612111 hydrochloride
    2 Publications Verification

    Opioid Receptor Neurological Disease Inflammation/Immunology
    SB-612111 hydrochloride hydrochloride is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 hydrochloride exhibits selectivity for μ-,?κ- and?δ-receptors with Ki values of?57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
    SB-612111 hydrochloride
  • HY-151539

    LIM Kinase (LIMK) Neurological Disease
    TH470 is a highly selective LIMK1/2 (LIM kinase1/2) inhibitor (LIMK1 IC50=9.8 nM; LIMK2 IC50=13 nM), and can be used in orphan disease research .
    TH470
  • HY-135065

    Trace Amine-associated Receptor (TAAR) Metabolic Disease
    3-Iodothyronamine (hydrochloride) is an endogenous and rapid-acting derivative of thyroid hormone. 3-Iodothyronamine potently activates an orphan G protein-coupled receptor in vitro (TAAR1) and induced hypothermia in vivo on a rapid time scale. 3-Iodothyronamine can be used for the research of congestive heart failure .
    3-Iodothyronamine hydrochloride
  • HY-119366

    ROR Inflammation/Immunology
    S18-000003 is a potent, selective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), with an IC50 of <30 nM towards human RORγt in competitive binding assays. S18-000003 shows selectivity for RORγt over other ROR family members (IC50>10 μM). S18-000003 can be used for the research of psoriasis with low risk of thymic aberrations .
    S18-000003
  • HY-101777

    GPR139 Neurological Disease
    TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM .
    TC-O 9311
  • HY-P1164A

    Urotensin Receptor Cardiovascular Disease
    Urotensin II (114-124), human TFA, an 11-amino acid residue peptide, is a potent vasoconstrictor and agonist for the orphan receptor GPR14.
    Urotensin II (114-124), human TFA
  • HY-W150866

    Hexylparaben

    ROR Inflammation/Immunology
    Hexyl 4-hydroxybenzoate (Hexylparaben) is a retinoic acid-related orphan receptor RORγ(t) agonist with an EC50 of 144 nM. Hexyl 4-hydroxybenzoate is used in the study of autoimmune diseases .
    Hexyl 4-hydroxybenzoate
  • HY-108258

    GPR119 Endocrinology
    PSN 375963 is a potent GPR119 agonist, with EC50s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 shows similar potency to the endogenous agonist oleoylethanolamide (OEA) .
    PSN 375963
  • HY-119464
    MRL-871
    1 Publications Verification

    ROR Cancer
    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 .
    MRL-871
  • HY-111509

    ROR Inflammation/Immunology
    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) .
    TAK-828F
  • HY-P1349A
    Orexin B, rat, mouse TFA
    1 Publications Verification

    Rat orexin B TFA; Orexin B (mouse) TFA

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    Orexin B, rat, mouse (Rat orexin B) TFA is an endogenous orexin receptor agonist. Orexin B, rat, mouse TFA binds and activates two closely related orphan G protein-coupled receptors OX1-R and OX2-R. Orexin B, rat, mouse TFA stimulates food intake and energy expenditure and plays a significant role in sleep-wakefulness regulation .
    Orexin B, rat, mouse TFA
  • HY-P1065

    Apelin Receptor (APJ) HIV Infection Cardiovascular Disease Metabolic Disease
    Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ .
    Apelin-36(rat, mouse)
  • HY-13682B
    Mifamurtide sodium
    5 Publications Verification

    MTP-PE sodium; L-MTP-PE sodium; CGP 19835 sodium

    NOD-like Receptor (NLR) Inflammation/Immunology Cancer
    Mifamurtide sodium (MTP-PE sodium), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide sodium is a specific ligand for NOD2 and acts as an insulin sensitizer. Mifamurtide sodium has potential for use in rare disease and osteosarcoma research .
    Mifamurtide sodium
  • HY-13682C
    Mifamurtide TFA
    5 Publications Verification

    MTP-PE TFA; L-MTP-PE TFA; CGP 19835 TFA

    NOD-like Receptor (NLR) Inflammation/Immunology Cancer
    Mifamurtide TFA (MTP-PE TFA), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide TFA is a specific ligand for NOD2 and acts as an insulin sensitizer. Mifamurtide TFA has potential for use in rare disease and osteosarcoma research .
    Mifamurtide TFA
  • HY-156190

    Orphan Nuclear Receptor Cancer
    NR2F2-IN-1 (CIA1) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F2-IN-1 substantially inhibits COUP-TFII-driven NGFIA reporter expression. NR2F2-IN-1 directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .
    NR2F2-IN-1
  • HY-P1064A

    HIV Apelin Receptor (APJ) Infection Cardiovascular Disease Metabolic Disease
    Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
    Apelin-36(human) TFA
  • HY-111323

    ROR Neurological Disease
    ASN06917370 is a former orphan receptor GPR17 ligand for the study of neurodegenerative diseases. ASN06917370 has an EC50 of 268 pM in [35S]GTPyS experiments .
    ASN06917370
  • HY-P1525

    MCH (salmon)

    MCHR1 (GPR24) Cardiovascular Disease Neurological Disease Metabolic Disease Endocrinology
    Melanin Concentrating Hormone, salmon is a 19-amino-acid neuropeptide initially identified in the pituitary gland of teleost fish, which regulates food intake, energy balance, sleep state, and the cardiovascular system. Melanin-concentrating hormone is a ligand for an orphan G protein-coupled receptor (SLC-1/GPR24) and MCHR2.
    Melanin Concentrating Hormone, salmon
  • HY-P1525A

    MCH (salmon) TFA

    MCHR1 (GPR24) Cardiovascular Disease Neurological Disease Metabolic Disease Endocrinology
    Melanin Concentrating Hormone, salmon TFA (MCH (salmon) TFA) is a 19-amino-acid neuropeptide initially identified in the pituitary gland of teleost fish, which regulates food intake, energy balance, sleep state, and the cardiovascular system. Melanin-concentrating hormone is a ligand for an orphan G protein-coupled receptor (SLC-1/GPR24) and MCHR2.
    Melanin Concentrating Hormone, salmon TFA
  • HY-120785

    ROR Inflammation/Immunology
    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 .
    SR1555
  • HY-162640

    ROR Cancer
    LDR102 (Compound 19h) is an inhibitor for receptor tyrosine kinase-like orphan receptor 1 (ROR 1) with Ki of 0.10 μM. LDR102 inhibits proliferation of cancer cells H1975, A549 and MDA-MB-231, with IC50 of 0.36 μM, 1.37 μM and 0.47 μM. LDR102 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
    LDR102
  • HY-125111

    GPR55 Cannabinoid Receptor Neurological Disease Metabolic Disease Cancer
    PSB-SB-487 is a potent GPR55 antagonist and CB2 agonist with an IC50 value of 0.113 µM for GPR55, and a Ki value of 0.292 µM for human CB2. PSB-SB-487 can be used for researching diabetes, Parkinson’s disease, neuropathic pain, and cancer .
    PSB-SB-487
  • HY-172769

    Histone Methyltransferase Cancer
    CM112 is a selective protein arginine methyltransferase 1 (PRMT1) degrader by tethering hydrophobic tag, adamantane, to MS023 with a 5-PEG linker. CM112 induces the degradation of PRMT1 in various solid cancer cell lines. CM112 can also target the nonenzymatic function of PRMT1 by downregulating the stability of the orphan receptor TR3. CM112 is promising for research of cancers .
    CM112
  • HY-P2537
    Apelin-12
    2 Publications Verification

    HIV Apelin Receptor (APJ) Others
    Apelin-12 is one of the most potent C-terminal fragments of the polypeptide that possesses a high affinity to orphan receptor APJ receptor. Apelin-12 is involved in the regulation of body fluid homeostasis and in the central control of feeding. Apelin-12 blocks HIV-1 entry through APJ receptor. Apelin-12 exerts neuroprotective effect .
    Apelin-12
  • HY-P1483A

    Urotensin Receptor Cardiovascular Disease Neurological Disease
    Urotensin II, mouse TFA is an endogenous ligand for the orphan G-protein-coupled receptor GPR14 or SENR. Urotensin II, mouse TFA is a potent vasoconstrictor. Urotensin II, mouse TFA plays a physiological role in the central nervous system .
    Urotensin II, mouse TFA
  • HY-16983

    ROR Inflammation/Immunology
    GNE-3500 is a selective, orally active antagonist for Retinoic Acid Receptor-Related Orphan Receptor C (RORc, also known as RORγ or NR1F3) with an EC50 of 12 nM. GNE-3500 exhibits good pharmacokinetic characteristics in rats .
    GNE-3500
  • HY-133128

    ROR Cancer
    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 .
    FM26
  • HY-122054A

    Keap1-Nrf2 Cancer
    BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 hydrochloride impairs the anchorage-independent growth of KEAP1-mutant cancer cells .
    BPK-29 hydrochloride

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