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GPR109 receptor agonist-1 (Compound 3a) is a highly selective agonist of the human orphan G-protein-coupled receptorGPR109b, with the pEC50 of 6.4. GPR109 receptor agonist-1 can be used for the research of cardio-metabolic diseases .
Apelin-12 is one of the most potent C-terminal fragments of the polypeptide that possesses a high affinity to orphanreceptorAPJreceptor. 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 .
7α,25-Dihydroxycholesterol intermediate-1 is an intermediate in the synthesis of 7α,25-Dihydroxycholesterol (HY-113962). 7α,25-Dihydroxycholesterol (7α,25-OHC) can be used as a ligand to target the orphan GPCR receptor EBI2 (GPR183). body, used to synthesize the corresponding PROTEACs .
RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R
ML-180 (SR1848) is a potent orphan nuclear receptorliver 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 .
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .
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 .
RORγt modulator 3 (Compound 23) is a modulator of retinoid-related orphanreceptor γt (RORγt). RORγt modulator 3 can be used for the research of RORyt mediated diseases such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer .
RORγt modulator 2 (Compound 21) is a modulator of retinoid-related orphanreceptor γt (RORγt) with the IC50 of <50 nM. RORγt modulator 2 can be used for the research of RORyt mediated diseases such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer .
Neuropeptide S (Rat) is an endogenous ligand of a previously orphan G-protein-coupled receptor now named NPS receptor. Neuropeptide S (Rat) can be used for the research of nervous system disease .
Xenopus orexin A is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. Xenopus orexin A is a potent agonist of OX1R .
Bevurogant (BI 730357) is a retinoid-related orphanreceptor-gamma t (RORγt) antagonist. Bevurogant can be used for the research of chronic inflammatory diseases .
Xenopus orexin B is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. Xenopus orexin B is a potent agonist of OX2R .
ASN06917370 is a former orphanreceptorGPR17 ligand for the study of neurodegenerative diseases. ASN06917370 has an EC50 of 268 pM in [35S]GTPyS experiments .
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 .
ROR agonist-1 is a potent and orally bioavailable inverse agonist of the retinoic acid receptor-related orphanreceptor C2 (RORC2), inhibition of IL-17A production from human primary TH 17 cells with a pIC50 of 7.5 .
FM26 (compound 25) is a potent and allosteric retinoic acid receptor-related orphanreceptor 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 .
Urotensin II, mouse is an endogenous ligand for the orphan G-protein-coupled receptorGPR14 or SENR. Urotensin II, mouse is a potent vasoconstrictor. Urotensin II, mouse plays a physiological role in the central nervous system .
Urotensin II, mouse acetate is an endogenous ligand for the orphan G-protein-coupled receptorGPR14 or SENR. Urotensin II, mouse acetate is a potent vasoconstrictor. Urotensin II, mouse acetate plays a physiological role in the central nervous system .
ASN04421891 is a potent GPR17 receptor modulator, with an EC50 of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 can be used for neurodegenerative diseases research .
PSN 375963 hydrochloride is a potent GPR119 agonist, with EC50s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 hydrochloride shows similar potency to the endogenous agonist oleoylethanolamide (OEA) .
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) .
SR1078 is a selective agonist of retinoic acid receptor-related orphanreceptor 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 .
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 .
MRL-871 (compound 3) is a potent and allosteric retinoic acid receptor-related orphanreceptor 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 .
Urotensin II, mouse TFA is an endogenous ligand for the orphan G-protein-coupled receptorGPR14 or SENR. Urotensin II, mouse TFA is a potent vasoconstrictor. Urotensin II, mouse TFA plays a physiological role in the central nervous system .
RORγt inverse agonist 31 (14g) is a potent retinoic acid receptor-related orphanreceptor γt (RORγt) inverse agonist, with an IC50 of 0.428 μM. RORγt inverse agonist 31 can alleviate the severity of Imiquimod (HY-B0180)-induced psoriasis in mice .
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 .
Izumerogant (IMU-935) is an inverse agonist of retinoid-related orphanreceptor-gamma (RORγ). Izumerogant (compound 123) also potently inhibits IL-17A, IL-17F and IFN-γ activity with IC50s <50 nM .
SB-612111 is a novel and potent opiate receptor-like orphanreceptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
SB-612111 hydrochloride hydrochloride is a novel and potent opiate receptor-like orphanreceptor (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 .
Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphanreceptors (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 .
OX04529 (compound 69) is a potent, selective and orally active agonist of GPR84. OX04529 inhibits FSK-induced cAMP production with an EC50 of 0.0185 nM. OX04529 displayed excellent potency, high G-protein signaling bias .
rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphanreceptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). rel-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. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
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.
BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptorNR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells .
BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptorNR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 hydrochloride impairs the anchorage-independent growth of KEAP1-mutant cancer cells .
S18-000003 is a potent, selective and orally active inhibitor of retinoic acid receptor-related orphanreceptor-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 .
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 .
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.
Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptorAPJ 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-17(human, bovine) is an endogenous orphan G protein-coupled receptorAPJ 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 .
7α,25-Dihydroxycholesterol-d6 is deuterium labeled 7α,25-Dihydroxycholesterol. 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
Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptorAPJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptorAPJ agonist. Apelin-36(rat, mouse) TFA 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) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ .
RORγt inverse agonist 30 (Compound 1) is a potent RORγt inverse agonist with the IC50 of 46 nM. Targeting the nuclear receptor RORγt is effective in autoimmune disorders .
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 .
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptorEBI2 (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 .
(±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphanreceptorRORγ 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 .
Apelin-36(human) is an endogenous orphan G protein-coupled receptorAPJ 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 .
ARI-1 is an inhibitor of receptor tyrosine kinase-like orphanreceptor 1 (ROR1) inhibitor. ARI-1 effectively inhibits aberrant ROR1 expression, which is associated with the development of non-small cell lung cancer (NSCLC) and EGFR-TKI-induced drug resistance. ARI-1 binds to the extracellular Frizzled domain of ROR1 and regulates PI3K/AKT/mTOR signaling in a ROR1-dependent manner. ARI-1 potently inhibits NSCLC cell proliferation and migration and has antitumor activity in vivo [1] .
Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptorAPJ 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 .
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 orphanreceptor 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.
Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo .
Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo .
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 orphanreceptor 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.
Apelin-12 is one of the most potent C-terminal fragments of the polypeptide that possesses a high affinity to orphanreceptorAPJreceptor. 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 .
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .
Orphan GPCR SP9155 agonist P550 (mouse, rat) (26RFa (mouse, rat)), a member of the RFamide peptide family with orexigenic effect, is the cognate ligand of the mouse orphanreceptor GPR103, also designated SP9155 or AQ27 .
Neuropeptide S (Rat) is an endogenous ligand of a previously orphan G-protein-coupled receptor now named NPS receptor. Neuropeptide S (Rat) can be used for the research of nervous system disease .
Xenopus orexin A is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. Xenopus orexin A is a potent agonist of OX1R .
Xenopus orexin B is a neuropeptides that identified as an endogenous ligands for an orphan G-protein-coupled receptor. Xenopus orexin B is a potent agonist of OX2R .
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 .
(Des-Bromo)-Neuropeptide B (1-23) (human) is an orphan G-protein coupled receptor agonist with Kis of 1.2 nM and 341 nM for GPR7 (NPBW1) and GPR8 (NPBW2), respectively .
Urotensin II, mouse is an endogenous ligand for the orphan G-protein-coupled receptorGPR14 or SENR. Urotensin II, mouse is a potent vasoconstrictor. Urotensin II, mouse plays a physiological role in the central nervous system .
26Rfa, Hypothalamic Peptide, human is a hypothalamic neuropeptide of the RFamide peptide family with orexigenic activity . 26RFa is an orexigenic neuropeptide identified as the endogenous ligand of the orphan G protein-coupled receptor GPR103 .
Urotensin II, mouse acetate is an endogenous ligand for the orphan G-protein-coupled receptorGPR14 or SENR. Urotensin II, mouse acetate is a potent vasoconstrictor. Urotensin II, mouse acetate plays a physiological role in the central nervous system .
Urotensin II, mouse TFA is an endogenous ligand for the orphan G-protein-coupled receptorGPR14 or SENR. Urotensin II, mouse TFA is a potent vasoconstrictor. Urotensin II, mouse TFA plays a physiological role in the central nervous system .
Neuromedin S (human) is a neuropeptide that contains 33 amino acids.? Neuromedin S (human)has been identified in the brain as an endogenous ligand for the orphanG-protein coupled receptor (GPCR) FM-4/TGR-1 and acts on the neuromedin U (NMU) receptor 2 (NMUR2) in the regulation of body weight homeostasis .
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.
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 .
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.
Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptorAPJ 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-17(human, bovine) is an endogenous orphan G protein-coupled receptorAPJ 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) TFA is an endogenous orphan G protein-coupled receptorAPJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptorAPJ agonist. Apelin-36(rat, mouse) TFA 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) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ .
Apelin-36(human) is an endogenous orphan G protein-coupled receptorAPJ 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) TFA is an endogenous orphan G protein-coupled receptorAPJ 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 .
Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo .
Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo .
Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphanreceptors (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 .
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptorEBI2 (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 .
NR1I2; Nuclear receptor subfamily 1 group I member 2; orphan nuclear receptor PAR1; orphan nuclear receptor PXR; Pregnane X receptor; Steroid and xenobiotic receptor; SXR
The PXR protein is a nuclear receptor that acts as a multifunctional transcription factor activated by a variety of endogenous and exogenous compounds. It regulates genes involved in the metabolism and secretion of substances, responding to ligands such as rifampicin, hypericin, gugulin, colupulone, isoflavones, pregnenolone and progesterone. PXR Protein, Human (His) is the recombinant human-derived PXR protein, expressed by E. coli , with N-6*His labeled tag. The total length of PXR Protein, Human (His) is 305 a.a., .
NR1I2; Nuclear receptor subfamily 1 group I member 2; orphan nuclear receptor PAR1; orphan nuclear receptor PXR; Pregnane X receptor; Steroid and xenobiotic receptor; SXR
The PXR protein is a nuclear receptor that acts as a multifunctional transcription factor activated by a variety of endogenous and exogenous compounds. It regulates genes involved in the metabolism and secretion of substances, responding to ligands such as rifampicin, hypericin, gugulin, colupulone, isoflavones, pregnenolone and progesterone. PXR Protein, Human is the recombinant human-derived PXR protein, expressed by E. coli , with tag free. The total length of PXR Protein, Human is 305 a.a., .
The RORa protein is a nuclear receptor that is critical for a variety of physiological processes including development, immunity, circadian rhythms, and metabolic pathways. RORa operates as a monomer, binding DNA to RORE and exhibiting intrinsic transcriptional activity. RORa Protein, Human (Sf9) is the recombinant human-derived RORa protein, expressed by Sf9 insect cells , with tag free. The total length of RORa Protein, Human (Sf9) is 253 a.a., .
The RORa protein is a nuclear receptor that is critical for a variety of physiological processes including development, immunity, circadian rhythms, and metabolic pathways. RORa operates as a monomer, binding DNA to RORE and exhibiting intrinsic transcriptional activity. RORa Protein, Human (Sf9, His) is the recombinant human-derived RORa protein, expressed by Sf9 insect cells , with N-8*His labeled tag. The total length of RORa Protein, Human (Sf9, His) is 253 a.a., .
GPRC5D Protein-VLP, Human (Biotinylated, HEK293) is available in solution form, no concentration information, recommended only for SPR analysis. HY-P77958 can be used in animal immunization, ELISA, PK assay.
ACKR3 is an atypical chemokine receptor that precisely controls chemokine levels and localization through high-affinity binding, operating independently of ligand-driven signaling. It acts as an interceptor, internalization receptor, and chemokine scavenger for CXCL11 and CXCL12/SDF1, inducing β-arrestin recruitment, ligand internalization, and MAPK pathway activation. ACKR3 Protein, Human (Cell-Free, His, SUMO) is the recombinant human-derived ACKR3 protein, expressed by E. coli Cell-free , with N-6*His, N-SUMO labeled tag. The total length of ACKR3 Protein, Human (Cell-Free, His, SUMO) is 362 a.a., with molecular weight of 57.5 kDa.
GPRC5D; G protein-coupled receptor, family C, group 5, member D; G-protein coupled receptor family C group 5 member D; orphan G-protein coupled receptor; MGC129713; MGC129714
GPRC5D Protein-VLP, Human (HEK293, C-His) is recommended for animal immunization, ELISA. It is not recommended for receptor-ligand interaction detection and SPR/BLI assay since there are other irrelevant membrane proteins of the host on the VLP envelope, and the receptor-ligand interaction will have strong background interference. High requirements for chips and experimental protocols are needed for SPR/BLI assays.
7α,25-Dihydroxycholesterol-d6 is deuterium labeled 7α,25-Dihydroxycholesterol. 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