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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 .
Synaptamide (Dehydroepiandrosteron; DHEA) is an endogenous metabolite and structural analogue of Anandamide. Synaptamide binds to both the cannabinoid-1 and 2 (CB1 and CB2) cannabinoid receptors and has anti-inflammatory properties. Synaptamide is the first small-molecule endogenousligand of an adhesion G protein-coupled receptor (aGPCR) .
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 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 .
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 .
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 .
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) .
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 .
BMS-681 is an orthosteric antagonist of CC chemokine receptor 2 (CCR2). BMS-681 restricts the movement of the extracellular end of TM6 by stabilizing TM7. TM7 and TM6 are the main components of the orthosteric binding site. BMS-681 can be used to study inflammatory neurodegenerative diseases and cancer .
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 .
Imidazoleacetic acid (Standard) is the analytical standard of Imidazoleacetic acid. This product is intended for research and analytical applications. Imidazoleacetic acid is an endogenousligand that stimulates imidazole receptors.
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 .
Arachidonoyl ethanolamide phosphate, an endocannabinoid, is an endogenousligand for cannabinoid receptors in the central nervous system (CB1 subtype) and peripheral immune cells (CB2 subtype) .
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 .
(E)-PHCCC is a positive allosteric modulator (PAM) for mGluR4, that enhances the activity of the receptor's endogenousligand (glutamate), and exhibits activity in the calcium mobilization assay in CHO cells with an EC50 of 3.2 μM .
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)
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 .
22-SLF is a PROTAC degrader, that degrades FK506-binding protein 12 (FKBP12) with a DC50 of 0.5 µM in a FBXO22 dependent manner. 22-SLF degrades other endogenous proteins, such as BRD4 and EML4-ALK fusion protein.(Pink: Ligand for target protein SLF (HY-114872); Black: Linker (HY-163821); Blue: Ligand for E3 ligase (HY-163826)) .
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 .
GDCNF-11 is a HIM-PROTAC GPX4 degrader based on the chaperone protein HSP90. GDCNF-11 promotes the ubiquitination and degradation of GPX4 through the HSP 90 chaperone complex, reduces endogenousGPX4 expression to induce ferroptosis in HT-1080 cells, and the DC50 value is 0.08 μM (Pink: Target protein ligand (HY-153748); Blue: HSP90 ligand (HY-10212); Black: Linker (HY-W169526)) .
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 .
OICR41114 (PROTAC 4) is a WDR5-targeting PROTAC degrader. OICR41114 degrades endogenous WDR5 with an EC50 and Dmax values of 40 nM and 49%, respectively. OICR41114 degrades HiBiT-tagged WDR5 in a proteasome-dependent manner . OICR41114 is composed of target protein ligand (red part) Dimethyl-F-OICR-9429-COOH (HY-141799), E3 ligase ligand (blue part) OICR-8268-acrylic acid (HY-169390) and PROTAC linker (black part) Amino-PEG9-amine (HY-140210). The conjugate of E3 ligase ligand and linker is OICR-8268-acrylic acid-amino-PEG9-amine (HY-169391).
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) .
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 .
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 .
2-Palmitoylglycerol (Standard) is the analytical standard of 2-Palmitoylglycerol. This product is intended for research and analytical applications. 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 .
(R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide (Compound 19) is the analogue of endogenous cannabinoid receptor ligand Anandamide (HY-10863). (R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide shows weak binding affinity for CB1 and CB2 with Kis of both 21 μM .
S-(+)-GABOB is an endogenousligand with antiepileptic activity. S-(+)-GABOB is a metabolite of GABA and may function as a neurotransmitter. S-(+)-GABOB behaves as a full agonist when bound to the ρ(1) wild-type receptor. S-(+)-GABOB acts as a competitive antagonist in the ρ(1) T244S mutant receptor .
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 .
5-Phenyllevulinic acid (4-Oxo-5-phenylpentanoic acid) is an endogenous fungal metabolite with inhibitory activity against the bacterium B. megaterium, the plant pathogenic fungus S. tritici, and the alga C. fusca. 5-Phenyllevulinic acid is also an intermediate in the synthesis of σ receptorligands. 5-Phenyllevulinic acid holds potential for research in the field of anti-infection studies .
PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a von Hippel-Lindau ligand-based SKG3 PROTAC composed of a PEG3-C4-OBn (HY-130620) alkyl linker, an SGK3 degrader (red structure), and a VHL ligand (HY-150803, blue structure). PROTAC SGK3 degrader-1 (0.3 μM) induced 50% endogenous SGK3 degradation within 2 hours, and 80% SGK3 degradation was observed at 8 hours, accompanied by loss of phosphorylation of NDRG1 (SGK3 substrate) .
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 .
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 .
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 .
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.
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 .
SBI-810 is a functionally selected β-arrestin-biased neurotensin receptor 1 (NTSR1) allosteric modulator. SBI-810 modulates NTSR1 G protein signaling in a G protein-specific manner in the presence of the endogenousligand, neurotensin (NT). SBI-810 fully antagonizes NT-induced activation of Gq, partially antagonizes NT-induced activation of Gi1 and is permissive of NTSR1 activation of GoA and G12 .
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 .
Ghrelin is an endogenousligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro. 80 μg/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats. JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 μg/kg.
(S)-VU0637120 is a Y4R antagonist that effectively reduces the binding response of its endogenousligand, pancreatic polypeptide (PP), on Y4R, with an IC50 value of 2.7 μM. (S)-VU0637120 binds to the allosteric site of Y4R, which is located in the core region of the Y4R transmembrane structure, near the binding pocket of pancreatic polypeptide (PP), with a KB value of 300-400 nM. (S)-VU0637120 holds potential for research in the field of metabolic diseases .
Abscisic acid (Standard) is the analytical standard of Abscisic acid. This product is intended for research and analytical applications. 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 Ca2+-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 .
Sintilimab (IBI308) is a safe and effectivel humanized IgG4 monoclonal antibody that binds to PD-1 with a KD value of 74 pM. Sintilimab blocks the interaction of PD-1 with its ligands (PD-L1 and PL-L2), consequently helping to restore the endogenous antitumour T-cell response. Sintilimab combined with prebiotics inhibits tumor volume and regulates immune cell subpopulation balance in lung adenocarcinoma mice. Sintilimab can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer .
[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 196 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 safe and effectivel humanized IgG4 monoclonal antibody that binds to PD-1 with a KD value of 74 pM. Sintilimab blocks the interaction of PD-1 with its ligands (PD-L1 and PL-L2), consequently helping to restore the endogenous antitumour T-cell response. Sintilimab combined with prebiotics inhibits tumor volume and regulates immune cell subpopulation balance in lung adenocarcinoma mice. 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 .
Imidazoleacetic acid (Standard) is the analytical standard of Imidazoleacetic acid. This product is intended for research and analytical applications. Imidazoleacetic acid is an endogenousligand that stimulates imidazole receptors.
2-Palmitoylglycerol (Standard) is the analytical standard of 2-Palmitoylglycerol. This product is intended for research and analytical applications. 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 .
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 .
Abscisic acid (Standard) is the analytical standard of Abscisic acid. This product is intended for research and analytical applications. 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 Ca2+-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/Apelin Protein, Human (HEK293, Fc) is the recombinant human-derived APLN protein, expressed by HEK293 , with C-hFc labeled tag.
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
![[Nphe1]Nociceptin(1-13)NH2](http://file.medchemexpress.eu/product_pic/hy-p1320.gif)
![[Nphe1]Nociceptin(1-13)NH2 TFA](http://file.medchemexpress.eu/product_pic/hy-p1320a.gif)
