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L-α-lysophosphatidylinositol Soy sodium is an endogenousligand of GPR55. L-α-lysophosphatidylinositol Soy sodium is an endogenous lysophospholipid and endocannabinoid neurotransmitter that belongs to the class of lysophospholipids .
Neuropeptide S (Rat) is an endogenousligand 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 .
Urotensin II, mouse acetate is an endogenousligand for the orphan G-protein-coupled receptor GPR14 or SENR. Urotensin II, mouse acetate is a potent vasoconstrictor. Urotensin II, mouse acetate plays a physiological role in the central nervous system .
Enpatoran (M5049) hydrochloride is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran hydrochloride is inactive against TLR3, TLR4 and TLR9. Enpatoran hydrochloride can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran hydrochloride exhibits excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be used for both innate and adaptive autoimmunity blocking research .
Urotensin II, mouse is an endogenousligand for the orphan G-protein-coupled receptor GPR14 or SENR. Urotensin II, mouse is a potent vasoconstrictor. Urotensin II, mouse plays a physiological role in the central nervous system .
Urotensin II, mouse TFA is an endogenousligand 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 .
MRTX849 ethoxypropanoic acid incorporates a ligand for KRAS G12C, and a PROTAC linker. MRTX849 ethoxypropanoic acid can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (IC50s between 0.25 and 0.76 μM) .
R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenousligand diacyl glycerol .
(S)-Coriolic acid (13(S)-HODE), the product of 15-lipoxygenase (15-LOX) metabolism of linoleic acid, functions as the endogenousligand to activate PPARγ. (S)-Coriolic acid is an important intracellular signal agent and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial injury .
12S-HHT (12(S)-HHTrE) is an enzymatic product of prostaglandin H2 (PGH2) derived from cyclooxygenase (COX)-mediated arachidonic acid metabolism. 12S-HHT is an endogenousligand for BLT2 that fully activates BLT2 in vivo. 12S-HHT suppresses UV-induced IL-6 synthesis in keratinocytes, exerting an anti-inflammatory activity .
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenousligand 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 .
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) .
Neuropeptide Y (3-36) (human, rat), a neuropeptide Y (NPY) metabolite formed from dipeptidyl peptidase-4 (DPP4), is a selective Y2 receptor agonist. Neuropeptide Y (3-36) (human, rat) is a NPY metabolite formed from dipeptidyl peptidase-4 (DPP4). Neuropeptide Y (3-36) (human, rat) decreases release of norepinephrine via the Y2 receptor .
MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM) .
NTRC-824 (Compound 5) is a potent, selective and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagonist with an IC50 of 38 nM and a Ki of 202 nM. NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (Ki >30 μM) .
MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle, and this reduction is accompanied by an increase in insulin sensitivity. MEDICA16 is a selective agonist for GPR40 as well as selective partial agonists for GPR120 .
TSPO ligand-2 is a ligand of AUTAC1. AUTAC1 contains an p-fluorobenzylguanine (FBnG) and a Fumagillol moiety, which can silence endogenous MetAP2 in HeLa cells .
Xenopus orexin A is a neuropeptides that identified as an endogenousligands for an orphan G-protein-coupled receptor. Xenopus orexin A is a potent agonist of OX1R .
2-Arachidonoylglycerol-d8 is the deuterium labeled 2-Arachidonoylglycerol. 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
2-Arachidonoylglycerol-d5 is the deuterium labeled 2-Arachidonoylglycerol. 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
Xenopus orexin B is a neuropeptides that identified as an endogenousligands for an orphan G-protein-coupled receptor. Xenopus orexin B is a potent agonist of OX2R .
2-Arachidonoylglycerol-d11 is deuterium labeled 2-Arachidonoylglycerol.2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system[1].
JF526-Taxol (TFA) is a versatile scaffold for fluorogenic probes including ligands for self-labeling tags, stains for endogenous structures, and spontaneously blinking labels for super-resolution immunofluorescence .
Alamandine, a member of the renin-angiotensin system (RAS), a vasoactive peptide, is an endogenousligand of the G protein-coupled receptor MrgD. Alamandine targets to protect the kidney and heart through anti-hypertensive actions .
2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenousligand for GPR119 .
Enpatoran (M5049) is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research .
des-Gln14-Ghrelin is a second endogenousligand for the growth hormone secretagogue receptor. a). des-Gln14-ghrelin potently induces increases in [Ca 2+]i in CHO-GHSR62 cells, with an EC50 of 2.4 nM .
des-Gln14-Ghrelin TFA is a second endogenousligand for the growth hormone secretagogue receptor. a). des-Gln14-ghrelin potently induces increases in [Ca 2+]i in CHO-GHSR62 cells, with an EC50 of 2.4 nM .
NoxaBH3 is a cysteine-based cross-linked peptide with increased cell permeability and higher inhibitory activity against Mcl-1. NoxaBH3 binds to the endogenousCXCR4ligand to produce ubiquitin-Noxabh3 conjugate. NoxaBH3 is then delivered to cancer cells .
Nocistatin, a neuropeptide, is an endogenousligand 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 .
Ac4ManNDAz is a cell-permeable photocross-linking probe. Ac4ManNDAz can effectively compete with endogenous sialic acid for incorporation into cell surface glycoproteins and form cross-links with glycoprotein ligands under UV light irradiation. Ac4ManNDAz can be used to study interactions between glycoproteins .
C16-Sphingosine-1-phosphate is a derivative of Sphingosine-1-phosphate and also an endogenousligand for the EDG/S1P receptor. C16-Sphingosine-1-phosphate can be used in the research of angiogenesis, inflammation, and cardiovascular diseases .
Sialyl-Lewis X (sLeX) is a sialylated fucosylated tetrasaccharide, an endogenousantigen. Sialyl-Lewis X is a high-affinity ligand for selectins (E-, P-, and L-selectin) . Sialyl-Lewis X binds to ELAM-1 and CD62 and has the ability to inhibits CD62-mediated neutrophil recruitment to sites of inflammation .
Estrogen receptor antagonist 5 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 5 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 165) .
Estrogen receptor antagonist 6 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 6 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 166) .
AP5 is a potent, orlly active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenousligand (AgoPAM). AP5 demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 has the potential for type II diabetes research .
Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenousligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities .
Kisspeptin-54(human) (Metastin(human)) is an endogenousligand 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) hinders tumor metastasis and stimulates gonadotropin secretion .
A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration .
AP5 sodium is a potent, orall active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenousligand (AgoPAM). AP5 sodium demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 sodium has the potential for type II diabetes research .
BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM .
Obestatin(rat) TFA, encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) TFA suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenousligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) TFA has anti-inflammatory, anti-myocardial infarction and antioxidant activities .
Apelin-13 TFA is an endogenousligand for the G-protein coupled receptor angiotensin II protein J (APJ), activating this G protein-coupled receptor with an EC 50 value of 0.37 nM. Apelin-13 TFA has vasodilatory and antihypertensive effects. Apelin-13 TFA also can be used for researching type 2 diabetes and metabolic syndrome .
Kisspeptin-54(human) TFA (Metastin(human) TFA) is an endogenousligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) TFA binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) TFA hinders tumor metastasis and stimulates gonadotropin secretion .
APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure .
7α,25-Dihydroxycholesterol-d6 is deuterium labeled 7α,25-Dihydroxycholesterol. 7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenousligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenousligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenousligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
Sintilimab (IBI308) is a fully human IgG4 monoclonal antibody that binds to PD-1, thereby blocking the interaction of PD-1 with its ligands (PD-L1 and PL-L2) and consequently helping to restore the endogenous antitumour T-cell response. Sintilimab can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer .
Apelin-13 is an endogenousligand for the G-protein coupled receptor angiotensin II protein J (APJ), activating this G protein-coupled receptor with an EC 50 value of 0.37 nM. Apelin-13 is widely distributed in the central and peripheral nervous systems. Apelin-13 has vasodilatory and antihypertensive effects. Apelin-13 also can be used for researching type 2 diabetes and metabolic syndrome .
PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on von Hippel-Lindauligand. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate) .
Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H +-ATPase) and leads to the plasma membrane depolarization in a Ca 2+-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome .
Janelia Fluor 526, SE (JF526,SE) is a fluorogenic yellow fluorescent dye that contains NHS ester group. JF526 is a versatile scaffold for fluorogenic ligands, including labels for genetically encoded self-labeling protein tags and stains for endogenous structures . Janelia Fluor products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive ligand of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD) that binds to TTD, with a Kd of 88 nM. SETDB1-TTD-IN-1 increases SETDB1 methyltransferase activity. SETDB1-TTD-IN-1 can be used for the research of biological functions and disease associations of SETDB1-TTD .
SETDB1-TTD-IN-1 TFA is a potent, selective and endogenous binder competitive ligand of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD) that binds to TTD, with a Kd of 88 nM. SETDB1-TTD-IN-1 TFA increases SETDB1 methyltransferase activity. SETDB1-TTD-IN-1 TFA can be used for the research of biological functions and disease associations of SETDB1-TTD .
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC)endogenousligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC)endogenousligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenousligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands.
MCE designs a unique collection of 178 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.
JF526-Taxol (TFA) is a versatile scaffold for fluorogenic probes including ligands for self-labeling tags, stains for endogenous structures, and spontaneously blinking labels for super-resolution immunofluorescence .
Janelia Fluor 526, SE (JF526,SE) is a fluorogenic yellow fluorescent dye that contains NHS ester group. JF526 is a versatile scaffold for fluorogenic ligands, including labels for genetically encoded self-labeling protein tags and stains for endogenous structures . Janelia Fluor products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
Neuropeptide S (Rat) is an endogenousligand 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 .
Urotensin II, mouse acetate is an endogenousligand for the orphan G-protein-coupled receptor GPR14 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 endogenousligand 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 .
Neuropeptide Y (3-36) (human, rat), a neuropeptide Y (NPY) metabolite formed from dipeptidyl peptidase-4 (DPP4), is a selective Y2 receptor agonist. Neuropeptide Y (3-36) (human, rat) is a NPY metabolite formed from dipeptidyl peptidase-4 (DPP4). Neuropeptide Y (3-36) (human, rat) decreases release of norepinephrine via the Y2 receptor .
Urotensin II, mouse is an endogenousligand for the orphan G-protein-coupled receptor GPR14 or SENR. Urotensin II, mouse is a potent vasoconstrictor. Urotensin II, mouse plays a physiological role in the central nervous system .
Xenopus orexin A is a neuropeptides that identified as an endogenousligands 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 endogenousligands for an orphan G-protein-coupled receptor. Xenopus orexin B is a potent agonist of OX2R .
Alamandine, a member of the renin-angiotensin system (RAS), a vasoactive peptide, is an endogenousligand of the G protein-coupled receptor MrgD. Alamandine targets to protect the kidney and heart through anti-hypertensive actions .
26Rfa, Hypothalamic Peptide, human is a hypothalamic neuropeptide of the RFamide peptide family with orexigenic activity . 26RFa is an orexigenic neuropeptide identified as the endogenousligand of the orphan G protein-coupled receptor GPR103 .
Apelin-16, human, bovine is a biological active peptide. (Apelin is the endogenousligand for the G-protein-coupled APJ receptor. It is produced as a pre-proprotein of 77 amino acids.Apelin-16 is one of the active fragment of Apelin)
des-Gln14-Ghrelin is a second endogenousligand for the growth hormone secretagogue receptor. a). des-Gln14-ghrelin potently induces increases in [Ca 2+]i in CHO-GHSR62 cells, with an EC50 of 2.4 nM .
des-Gln14-Ghrelin TFA is a second endogenousligand for the growth hormone secretagogue receptor. a). des-Gln14-ghrelin potently induces increases in [Ca 2+]i in CHO-GHSR62 cells, with an EC50 of 2.4 nM .
NoxaBH3 is a cysteine-based cross-linked peptide with increased cell permeability and higher inhibitory activity against Mcl-1. NoxaBH3 binds to the endogenousCXCR4ligand to produce ubiquitin-Noxabh3 conjugate. NoxaBH3 is then delivered to cancer cells .
Nocistatin, a neuropeptide, is an endogenousligand 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 .
Neuromedin S (human) is a neuropeptide that contains 33 amino acids.? Neuromedin S (human)has been identified in the brain as an endogenousligand for the orphan G-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 .
Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenousligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities .
Kisspeptin-54(human) (Metastin(human)) is an endogenousligand 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) hinders tumor metastasis and stimulates gonadotropin secretion .
BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM .
Obestatin(rat) TFA, encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) TFA suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenousligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) TFA has anti-inflammatory, anti-myocardial infarction and antioxidant activities .
Apelin-13 TFA is an endogenousligand for the G-protein coupled receptor angiotensin II protein J (APJ), activating this G protein-coupled receptor with an EC 50 value of 0.37 nM. Apelin-13 TFA has vasodilatory and antihypertensive effects. Apelin-13 TFA also can be used for researching type 2 diabetes and metabolic syndrome .
Kisspeptin-54(human) TFA (Metastin(human) TFA) is an endogenousligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) TFA binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) TFA hinders tumor metastasis and stimulates gonadotropin secretion .
γ-2-MSH (41-58), amide is derived from γ-2-MSH. γ-2-MSH is a twelve amino acid peptide that is derived from the N-terminal fragment of proopiomelanocortin (POMC) and contains the His-Phe-Arg-Trp motif common to all melanocortin endogenous agonist ligands .
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenousligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenousligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
Apelin-13 is an endogenousligand for the G-protein coupled receptor angiotensin II protein J (APJ), activating this G protein-coupled receptor with an EC 50 value of 0.37 nM. Apelin-13 is widely distributed in the central and peripheral nervous systems. Apelin-13 has vasodilatory and antihypertensive effects. Apelin-13 also can be used for researching type 2 diabetes and metabolic syndrome .
Neuropeptide W-30 (rat) is an important stress mediator in the central nervous system that modulates the hypothalamus-pituitary-adrenal (HPA) axis and sympathetic outflow. Neuropeptide W-30 (rat) is an endogenousligand for the two structurally related orphan G-protein-coupled receptors (GPCRs) GPR7 and GPR8. NPW-30 activates and binds to both GPR7 and GPR8 at similar effective doses .
Neuropeptide W-30 (human) is an important stress mediator in the central nervous system that modulates the hypothalamus-pituitary-adrenal (HPA) axis and sympathetic outflow. Neuropeptide W-30 (human) is an endogenousligand for the two structurally related orphan G-protein-coupled receptors (GPCRs) GPR7 and GPR8. Neuropeptide W-30 (human) activates and binds to both GPR7 and GPR8 at similar effective doses .
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC)endogenousligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC)endogenousligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
Sintilimab (IBI308) is a fully human IgG4 monoclonal antibody that binds to PD-1, thereby blocking the interaction of PD-1 with its ligands (PD-L1 and PL-L2) and consequently helping to restore the endogenous antitumour T-cell response. Sintilimab can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer .
(S)-Coriolic acid (13(S)-HODE), the product of 15-lipoxygenase (15-LOX) metabolism of linoleic acid, functions as the endogenousligand to activate PPARγ. (S)-Coriolic acid is an important intracellular signal agent and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial injury .
12S-HHT (12(S)-HHTrE) is an enzymatic product of prostaglandin H2 (PGH2) derived from cyclooxygenase (COX)-mediated arachidonic acid metabolism. 12S-HHT is an endogenousligand for BLT2 that fully activates BLT2 in vivo. 12S-HHT suppresses UV-induced IL-6 synthesis in keratinocytes, exerting an anti-inflammatory activity .
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenousligand 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 .
2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenousligand for GPR119 .
Sialyl-Lewis X (sLeX) is a sialylated fucosylated tetrasaccharide, an endogenousantigen. Sialyl-Lewis X is a high-affinity ligand for selectins (E-, P-, and L-selectin) . Sialyl-Lewis X binds to ELAM-1 and CD62 and has the ability to inhibits CD62-mediated neutrophil recruitment to sites of inflammation .
Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H +-ATPase) and leads to the plasma membrane depolarization in a Ca 2+-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome .
APLN protein is an endogenous ligand for the apelin receptor (APLNR), drives receptor internalization, and dissociates more strongly from APLNR than (pyroglu)apelin-13. APLN Protein, Human (HEK293, Fc) is the recombinant human-derived APLN protein, expressed by HEK293 , with C-hFc labeled tag. The total length of APLN Protein, Human (HEK293, Fc) is 55 a.a., with molecular weight of 32-40 kDa.
APLN/Apelin protein is the endogenous ligand of APLNR and drives APLNR internalization. APLN/Apelin Protein, Mouse (HEK293, Fc) is the recombinant mouse-derived APLN/Apelin protein, expressed by HEK293 , with C-hFc labeled tag. The total length of APLN/Apelin Protein, Mouse (HEK293, Fc) is 55 a.a., with molecular weight of 55-65 kDa.
APLN/Apelin protein is the endogenous ligand of APLNR and drives APLNR internalization. APLN/Apelin Protein, Mouse (Biotinylated, HEK293, Fc-Avi) is the recombinant mouse-derived APLN/Apelin protein, expressed by HEK293 , with C-Avi, C-hFc labeled tag. The total length of APLN/Apelin Protein, Mouse (Biotinylated, HEK293, Fc-Avi) is 55 a.a., with molecular weight of 38-48 kDa.
2-Arachidonoylglycerol-d8 is the deuterium labeled 2-Arachidonoylglycerol. 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
2-Arachidonoylglycerol-d5 is the deuterium labeled 2-Arachidonoylglycerol. 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
2-Arachidonoylglycerol-d11 is deuterium labeled 2-Arachidonoylglycerol.2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system[1].
7α,25-Dihydroxycholesterol-d6 is deuterium labeled 7α,25-Dihydroxycholesterol. 7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenousligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly
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