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human receptors

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205

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3

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P990774

    ASP-7266; TRAB-1; UPB-101

    Interleukin Related Inflammation/Immunology
    Verekitug (ASP-7266; TRAB-1; UPB-101) is a human monoclonal antibody targeting the thymic stromal lymphopoietin receptor (TSLPR), with a mean half-life of approximately 20 days. At doses of Verekitug ≥100 mg, complete and sustained TSLPR-specific occupancy is achieved, and the antibody does not bind to IL-7Rα. By inhibiting TSLP-driven inflammatory responses, Verekitug blocks TSLP-induced cell proliferation and TARC expression, while reducing fractional exhaled NO levels, blood eosinophil counts, and levels of IL-5 and IgE. Verekitug significantly improves scores for nasal polyps, nasal congestion and olfactory dysfunction, with favorable safety and good tolerability; potential adverse reactions include headache, upper respiratory tract infection, sinusitis and nasopharyngitis. Verekitug is used in relevant studies on asthma, chronic rhinosinusitis with nasal polyps and chronic obstructive pulmonary disease .
    Verekitug
  • HY-P11245A

    Amylin Receptor Metabolic Disease
    NN1213 acetate, a long-acting human amylin peptide analog, is a selective Amylin receptor agonist with EC50 values of 0.177 and 0.262 nM for hAMY3R and rAMY3R, respectively. NN1213 acetate significantly reduces food intake and fat mass. NN1213 acetate can reduce body weightin diet-induced obese rats. NN1213 acetate can be used for the research of obesity .
    NN1213 acetate
  • HY-P4070

    Insulin Receptor Metabolic Disease
    Insulin icodec is an Insulin (HY-P0035) analog that strongly but reversibly binds to albumin. Insulin icodec has long plasma half-life. Insulin icodec modulates insulin receptor activity, controls blood glucose levels, reduces HbA1c levels, and binds reversibly to human serum albumin. Insulin icodec can be used for the research of type 2 diabetes mellitus .
    Insulin icodec
  • HY-B1213
    Trimipramine maleate
    1 Publications Verification

    5-HT Receptor Bacterial Neurological Disease
    Trimipramine maleate is a 5-HT receptor antagonist, with blood-brain barrier permeability. Trimipramine maleate has pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine maleate has vascular activity and anxiolytic efficacy .
    Trimipramine maleate
  • HY-103175
    PSB36
    1 Publications Verification

    Adenosine Receptor Cardiovascular Disease Neurological Disease Inflammation/Immunology
    PSB36 is a highly selective A1 adenosine receptor antagonist, with a Ki of 0.12 nM and a Kd of 0.7 nM. Systemic administration of PSB36 reduces formalin- and Carrageenan (HY-125474)-induced edema in mice and decreases pain-related behaviors, with no local paw activity. PSB36 prolongs the APD90 of rat and human atria, produces a frequency-dependent prolongation of rat atrial ERP, increases the diastolic threshold of rat atria, and shortens the duration of atrial fibrillation episodes. PSB36 can be used in research related to inflammatory pain, inflammatory hyperalgesia, edema and atrial fibrillation .
    PSB36
  • HY-100656

    Dopamine Receptor 5-HT Receptor Neurological Disease
    Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC50 of 8.90 at human D2 receptors, a pEC50 of 8.09 at D3 receptors, and a pEC50 of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca 2+ release at 5-HT2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.
    Desmethyl cariprazine
  • HY-P99017

    ALD-403

    CGRP Receptor Neurological Disease
    Eptinezumab (ALD-403) is a human monoclonal antibody targeting the α and β subtypes of human calcitonin gene-related peptide (CGRP). Eptinezumab binds to the CGRP ligand and blocks its binding to endogenous CGRP receptors, thereby inhibiting receptor activation. Eptinezumab can be used in research related to migraine .
    Eptinezumab
  • HY-16751

    APD811

    Prostaglandin Receptor Cardiovascular Disease Endocrinology
    Ralinepag is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.
    Ralinepag
  • HY-B1095
    Chlormadinone acetate
    1 Publications Verification

    Progesterone Receptor Androgen Receptor Glucocorticoid Receptor GABA Receptor Neurological Disease Metabolic Disease
    Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABAA receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders .
    Chlormadinone acetate
  • HY-P1465

    Secretin (28-54), (human)

    Secretin Receptor Metabolic Disease Cancer
    Human secretin is a 27-amino acid residue C-terminally amidated peptide, which acts on human secretin receptors .
    Human secretin
  • HY-107580

    GPR109A Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    GPR109 receptor agonist-1 is a highly selective agonist of the human orphan G protein-coupled receptor GPR109b, and does not activate the mouse homologous receptor PUMA-G. GPR109 receptor agonist-1 functionally modulates the human GPR109b receptor via the cAMP signaling pathway, with an EC50 of 400 nM. GPR109 receptor agonist-1 inhibits isoproterenol (HY-B0468)-stimulated lipolysis in human subcutaneous adipocytes, with efficacy comparable to that of Niacin (HY-B0143), and does not act on β-adrenergic receptors. GPR109 receptor agonist-1 can be used in studies related to dyslipidemia and atherosclerosis .
    GPR109 receptor agonist-1
  • HY-P2159

    Opioid Receptor Endogenous Metabolite Neurological Disease
    Dynorphin A (1-8) is a ligand with preference for the κ-opioid receptor, and its IC50 value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke .
    Dynorphin A (1-8)
  • HY-P11245

    Amylin Receptor Metabolic Disease
    NN1213, a long-acting human amylin peptide analog, is a selective Amylin receptor agonist with EC50 values of 0.177 and 0.262 nM for hAMY3R and rAMY3R, respectively. NN1213 significantly reduces food intake and fat mass. NN1213 can reduce body weightin diet-induced obese rats. NN1213 can be used for the research of obesity .
    NN1213
  • HY-135542
    NBI-27914
    2 Publications Verification

    CRFR Others
    NBI-27914 is a highly selective, high-affinity non-peptide competitive antagonist of human corticotropin-releasing factor receptor 1 (CRFR1). NBI-27914 primarily binds to the His199 and Met276 sites in the transmembrane domain of the receptor .
    NBI-27914
  • HY-W010162

    L-Alanyl-L-alanine; Ala-Ala

    Amino Acid Derivatives Others
    H-Ala-Ala-OH is a substrate of human intestinal oligopeptide transporter (PEPT1/SLC15A1), with an IC50 of 0.25 mM and an EC50 of 0.08 mM against human PEPT1. When used as a dipeptide linker in antibody-drug conjugates (ADCs) loaded with glucocorticoid receptor regulator payloads, H-Ala-Ala-OH enables efficient intracellular payload release .
    H-Ala-Ala-OH
  • HY-159069

    Toll-like Receptor (TLR) TNF Receptor Connexin Infection Cancer
    Zymosan (ZM), 95% is a yeast cell wall-derived carbohydrate-rich preparation and immunomodulator. Zymosan (ZM), 95% binds to and activates TLR-2, TLR-4, and Dectin-1 receptor to trigger downstream signaling pathways. Zymosan (ZM), 95% upregulates TLR-2, TLR-4, and TNF-α mRNA expression, increases serum TNF-α levels, and stimulates splenocyte number and viability in mice. Zymosan (ZM), 95% attenuates melanoma growth progression, modulates macrophage marker gene expression, and mediates phagocytosis, ROS generation, and cytokine production. Zymosan (ZM), 95% reduces Connexin 43 protein and mRNA levels, inhibits gap junctional intercellular communication, and induces proinflammatory factor production in human corneal cells. Zymosan (ZM), 95% induces peritoneal inflammation in mice, functions as a drug carrier, and supports fibroblast cell attachment in hydrogel formulations. Zymosan (ZM), 95% can be used for the research of melanoma, tumors, fungal keratitis, ocular surface inflammatory disorders, and peritoneal inflammation .
    Zymosan (ZM), 95%
  • HY-15039

    Bradykinin Receptor Metabolic Disease Inflammation/Immunology Endocrinology
    SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
    SSR240612
  • HY-150204

    LPL Receptor Others
    ONO-0740556 is a potent Gi-coupled human lysophosphatidic acid receptor 1 (LPA1) agonist with an EC50 value of 0.26 nM .
    ONO-0740556
  • HY-147276

    JW1601

    Histamine Receptor Inflammation/Immunology
    Izuforant (JW1601) (Compound 24) is an orally active histamine H4 receptor (H4R) antagonist with an IC50 of 36 nM against human H4R. Izuforant also shows binding affinity of human serotonin 3 receptor (h5-HT3R) with an IC50 of 9.1 μM. Izuforant exhibits strong anti-pruritic and anti-inflammatory efficacies .
    Izuforant
  • HY-108648A

    2-Methylthioadenosine diphosphate; 2-Methylthio-ADP

    P2Y Receptor Neurological Disease
    2-MeSADP is a P2Y receptor agonist, with an EC50 of 5 nM for human P2Y12, EC50 values of 19 nM and 13 nM for human P2Y13, and an EC50 of 6.2 nM for mouse P2Y13. It shows slightly higher selectivity for P2Y12 over human P2Y13. 2-MeSADP triggers increases in intracellular calcium levels, Gi-mediated cAMP inhibition, adenylate cyclase inhibition and downstream signal transduction. 2-MeSADP can be used in research related to glaucoma .
    2-MeSADP
  • HY-110237

    P2X Receptor Calcium Channel Cardiovascular Disease
    BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
    BX430
  • HY-P1117
    MMK1
    1 Publications Verification

    Formyl Peptide Receptor (FPR) Calcium Channel Neurological Disease Inflammation/Immunology
    MMK1 is a potent and selective human formyl peptide receptor like-1 (FPRL-1/FPR2) agonist with EC50s of <2 nM and >10000 nM for FPRL-1 and FPR1, respectively. MMK1 is a potent chemotactic and calcium-mobilizing agonist. MMK1 potently activates phagocytic leukocytes and enhances Pertussis Toxin-sensitive production by human monocytes of proinflammatory cytokines IL-1b and IL-6. MMK1 exerts anxiolytic-like activity .
    MMK1
  • HY-142117

    Calcium Channel Chloride Channel Others
    Adenophostin A is an IP3 receptor (inositol 1,4,5-trisphosphate receptors) modulator and Ca 2+ releaser, with an IC50 of 1.3 nM, an EC50 of 1.4 nM, and a Ki of 0.18 nM in rats, and an IC50 of 0.95 nM in humans. Adenophostin A activates IP3 receptors, stimulates Ca 2+ release from intracellular stores and microsomes, inhibits the binding of [ 3H]IP3 to plasma membrane receptors, and activates chloride channels. Adenophostin A resists phosphorylation and dephosphorylation by IP3 metabolic enzymes to maintain its activity, and increases cytoplasmic [Ca 2+] levels via calcium mobilization from the endoplasmic reticulum of vascular smooth muscle cells. Adenophostin A is applicable to research related to hemorrhagic shock .
    Adenophostin A
  • HY-168906

    Bradykinin Receptor PI3K Akt TNF Receptor ERK Neurological Disease Inflammation/Immunology
    BI-113823 is an orally active, blood-brain barrier-permeable bradykinin B1 receptor antagonist, with a Ki value of 5.3 nM for human receptors and 13.3 nM for rat receptors. BI-113823 reduces inflammation-induced mechanical hyperalgesia, as well as the mechanical sensitivity of peripheral afferent nerves and spinal nociceptive-specific neurons. BI-113823 alleviates liver fibrosis and portal hypertension, and improves survival in chronic liver disease models. BI-113823 inhibits the activities of monocytes, neutrophils and hepatic stellate cells, as well as the PI3K/Akt signaling pathway. BI-113823 can be used in research related to inflammatory pain, liver fibrosis and portal hypertension .
    BI-113823
  • HY-P990552A

    PAI-1 Integrin Cancer
    huATN-658 is an inhibitor that specifically targets the DIII domain of human urokinase plasminogen activator receptor (uPAR). huATN-658 neutralizes uPAR function by blocking the interaction between uPAR and integrins, without interfering with the binding of uPA or vitronectin to uPAR. huATN-658 inhibits the proliferation and invasion of breast cancer cells, slows the growth of primary breast tumors, reduces breast cancer-induced bone lesions and decreases osteoclast activity. huATN-658 also alters the gene expression of the TGF-β receptor complex signaling pathway. huATN-658 exerts synergistic anticancer effects when combined with Zoledronic Acid (HY-13777), and does not cause physiological or behavioral abnormalities in immunodeficient mice. huATN-658 can be used in research related to breast cancer, metastatic breast cancer and breast cancer-induced bone disease .
    huATN-658
  • HY-N0475

    Hypolide; (+)-Triptophenolide

    Androgen Receptor Pyroptosis Caspase Bcl-2 Family Apoptosis Inflammation/Immunology Cancer
    Triptophenolide (Hypolide) is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC50 of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .
    Triptophenolide
  • HY-108659

    P2Y Receptor Inflammation/Immunology
    NF340 is a P2Y11 receptor inhibitor with a pIC50 of 7.3-7.7 against human P2Y11 receptor, and it exhibits high selectivity over other P2Y family receptors. NF340 binds to the ATP-binding amino acid residues of the P2Y11 receptor to inhibit its activity, block nociceptive activity, and reduce spinal dorsal horn P2Y11 receptor upregulation induced by spinal cord injury. NF340 attenuates the NFκB signaling pathway activated by IL-1β by decreasing IκBα phosphorylation, nuclear p65 accumulation and NFκB promoter activity. NF340 inhibits IL-1β-induced pro-inflammatory cytokine expression, reduces intracellular ROS and 4-HNE levels, and suppresses IL-1β-induced matrix metalloproteinase expression in primary fibroblast-like synoviocytes. NF340 inhibits ATP-induced elevation of intracellular calcium 2+ concentration and cell migration in human hepatocellular carcinoma cells. NF340 is applicable to the research of neuropathic pain, myocardial ischemia/reperfusion injury, inflammatory pain, rheumatoid arthritis and hepatocellular carcinoma .
    NF340
  • HY-P1030

    Neurokinin Receptor Endocrinology
    Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 receptor, with Ki of 0.175 nM and 560 nM for human NK1 receptor and human NK2 receptor, respectively.
    Hemokinin 1 (mouse)
  • HY-P991381

    PPMX-T003

    Transferrin Receptor Reactive Oxygen Species (ROS) Ferroptosis Cancer
    JST‑TfR09 (PPMX‑T003) is a human monoclonal antibody (mAb) targeting transferrin receptor 1 (TfR1/CD71). JST‑TfR09 blocks the binding of transferrin to TfR1, inhibits TfR1 internalization, and suppresses cellular iron uptake. JST‑TfR09 triggers ferritin degradation via activating the autolysosomal system, promotes ROS production and lipid peroxidation, and ultimately induces ferroptosis. JST‑TfR09 exhibits cytotoxicity toward human erythroblasts differentiated from hematopoietic stem cells. JST-TfR09 can be used in leukemia research. Recommended isotype control: Human IgG1 lambda, Isotype Control (HY-P99992) .
    JST-TfR09
  • HY-P99431

    Alomfilimab; SAR 445256

    CD28 Inflammation/Immunology Cancer
    KY-1044 (Alomfilimab; SAR 445256) is a fully human IgG1 antibody targeting inducible costimulatory receptor (ICOS). KY-1044 depletes ICOS high cells via antibody-dependent cellular cytotoxicity (ADCC) through the engagement of FcgRIIIa. KY-1044 act as a costimulatory molecule on cells expressing lower ICOS levels, such as CD8 + TEff cells (through FcgR-dependent clustering). KY-1044 exploit the differential expression of ICOS on T-cell subtypes to improve the intratumoral immune contexture and restore an antitumor immune response .
    KY-1044
  • HY-P1465A

    Secretin (28-54), (human) TFA

    Secretin Receptor Metabolic Disease Cancer
    Human secretin TFA is a 27-amino acid residue C-terminally amidated peptide, which acts on human secretin receptors .
    Human secretin TFA
  • HY-117694

    CGRP Receptor Neurological Disease Inflammation/Immunology
    MK-8825 is an orally active, selective CGRP receptor antagonist with a Ki value of 47 pM for human CGRP receptors and 17 nM for rat CGRP receptors. MK-8825 blocks CGRP-stimulated cAMP responses and exhibits competitive-like antagonism. MK-8825 can be used in the research of migraine and temporomandibular joint disorders .
    MK-8825
  • HY-P4665

    Melanocortin Receptor Inflammation/Immunology
    Ac-c-Pro-Pro-Lys-Asp-NH2 is a selective human melanocortin 5 receptor (hMC5R) antagonist with an IC50 of 10 nM .
    Ac-c[Cys-Glu-His-d-Phe-Arg-Trp-d-Cys]-Pro-Pro-Lys-Asp-NH2
  • HY-149056

    MAP4K Interleukin Related Cancer
    GNE-6893 is an orally active, selective HPK1 inhibitor with a Ki < 0.02 nM. GNE-6893 enhances T cell receptor signaling in primary human T cells. GNE-6893 increases IL2 production in stimulated primary human T cells. GNE-6893 can be used for the research of chronic refractory cancers .
    GNE-6893
  • HY-177425

    Cannabinoid Receptor Metabolic Disease
    AM11542 is a cannabinoid receptor 1 (CB1) agonist with a human CB1 Ki of 0.11 nM. AM11542 stabilizes the active conformational state of the CB1 receptor. AM11542 can be used for the research of obesity .
    AM11542
  • HY-19259

    Adenosine Kinase Neurological Disease
    GP3269 is a selective and orally active human adenosine kinase (AK) inhibitor with an IC50 of 11 nM against human adenosine kinase. GP3269 increases adenosine levels at epileptic foci, activates A1 receptors on excitatory neurons, and exhibits anticonvulsant activity in rats. GP3269 does not induce hemodynamic effects including changes in blood pressure or heart rate in rats. GP3269 can be used for epilepsy-related research .
    GP3269
  • HY-P991358

    LFA-102; X213

    Estrogen Receptor/ERR STAT Akt Cancer
    XOMA-213 (LFA-102; X213) is a human monoclonal antibody (mAb) targeting the prolactin receptor (PRLR), with a Kd value of 2 nM against the human target. XOMA-213 blocks PRL-induced cell proliferation and inhibits the activation of multiple PRLR ligands, including PRL and human growth hormone (hGH). XOMA-213 suppresses PRL-induced phosphorylation of Stat5, Akt and ERK1/2 in cells. XOMA-213 induces tumor regression, delays disease progression, and inhibits PRLR signaling as well as tumor growth. XOMA-213 can be used in research related to breast cancer .
    XOMA-213
  • HY-177291

    Microsomal Triglyceride Transfer Protein (MTP) Smo Hedgehog LDLR Cardiovascular Disease Cancer
    LAB687 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 0.9 nM for apolipoprotein B (apoB) secretion in HepG2 cells. LAB687 also acts as a Smoothened (Smo) antagonist, with IC50 values of 2.48 μM and 3.42 μM against mouse and human Smo receptors, respectively. LAB687 reduces triglyceride and low-density lipoprotein cholesterol (LDL-C) levels, and inhibits the Hedgehog signaling pathway. LAB687 can be used in studies related to Hedgehog-dependent cancers .
    LAB687
  • HY-P2496

    Endothelin Receptor Fluorescent Dye NF-κB COX Prostaglandin Receptor Apoptosis TNF Receptor Interleukin Related MMP Cardiovascular Disease Inflammation/Immunology Cancer
    Endothelin 1 (swine, human), Alexa Fluor 488-labeled is an Endothelin-1 conjugated with Alexa Fluor 488 (HY-D1304). Endothelin-1 is an endogenous vasoconstrictor and agonist of ETA/ETB receptor. Endothelin 1 (swine, human) exerts effects including promoting mitosis, angiogenesis, tumor invasion and metastasis, and inhibiting apoptosis. Endothelin 1 (swine, human) induces inflammation and oxidative stress by activating the NF-κB pathway. Endothelin 1 (swine, human), Alexa Fluor 488-labeled is specifically designed for fluorescence imaging, flow cytometry or receptor localization studies, and can be used in research related to sepsis, atherosclerosis, systemic inflammatory response syndrome, cancer and congestive heart failure .
    Endothelin 1 (swine, human), Alexa Fluor 488-labeled
  • HY-176192

    Toll-like Receptor (TLR) NF-κB p38 MAPK ERK IKK TNF Receptor Interleukin Related Inflammation/Immunology
    SMU-14a is a selective Toll-like receptor 3 (TLR3) inhibitor wirh an IC50 of 0.18 μM. SMU-14a reduces phosphorylation of p65, ERK, and TBK1 via NF-κB, MAPK, and IRF3 signaling pathways. SMU-14a inhibits IL-6 secretion in mouse peritoneal macrophages, downregulates TNF-α in human peripheral blood monocytes and decreases serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels. SMU-14a can be used for the research of acute hepatitis .
    SMU-14a
  • HY-N4267

    Calcium Channel Platelet-activating Factor Receptor (PAFR) UGT Leukotriene Receptor TNF Receptor PGE synthase Interleukin Related Cardiovascular Disease Infection Inflammation/Immunology
    Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca 2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases .
    Yangambin
  • HY-P3584

    (Pro3) Gastric Inhibitory Peptide, human

    Insulin Receptor Metabolic Disease
    (Pro3) GIP, human ((Pro3) Gastric Inhibitory Peptide, human) is an efficacious, stable and specific human GIP receptor (hGIPR) full agonist. (Pro3) GIP, human has high binding affinity for human GIPR with Ki/ Kd values of 0.90 nM. (Pro3) GIP, human can be used for the research of obesity-related diabetes .
    (Pro3) GIP, human
  • HY-103172

    P2Y Receptor Metabolic Disease
    8-Aminoadenine is an adenine receptor 1 (rAde1R) inhibitor with a Ki of 6.51 μM in rat and 0.0341 μM in human. 8-Aminoadenine inhibits isoprenaline-induced cAMP accumulation and adenine uptake in astrocytoma cells expressing rAde1R. 8-Aminoadenine serves as a lead structure for the development of adenine receptor ligands to elucidate the functions of the adenine receptor family .
    8-Aminoadenine
  • HY-B1213A

    5-HT Receptor Bacterial Neurological Disease
    Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .
    Trimipramine
  • HY-103405A

    Dopamine Receptor Neurological Disease
    NGD 94-1 (dimaleate) is a potent and selective dopamine D4 receptor antagonist. NGD 94-1 (dimaleate) shows high affinity for the cloned human D4.2 receptor (Ki = 3.6 nM). NGD 94-1 (dimaleate) modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD 94-1 (dimaleate) can be used for neurological disease research [1][2].
    NGD 94-1 dimaleate
  • HY-10419

    Thrombopoietin Receptor Cardiovascular Disease
    AH23848 (compound 6) is a competitive blocker of the thromboxane A2 receptor and an orally effective agent, with an IC50 value of 50 nM against human targets and a long duration of action.
    AH23848
  • HY-177275

    c-Kit Cancer
    c-Kit Receptor modulator-1 (Compound #22) is a c-Kit Receptor modulator. c-Kit Receptor modulator-1 can be used for malignant cancers such as canine mastocytoma, human gastrointestinal stromal tumor and small cell lung cancer research .
    c-Kit Receptor modulator-1
  • HY-W019787

    Opioid Receptor CXCR Neurological Disease
    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 .
    BAM-12P
  • HY-105346

    Neurokinin Receptor Neurological Disease
    WIN 51708 is a nonpeptide antagonist of neurokinin (NK)-1 receptor. WIN 51708 has a higher affinity for the rat NK-1 receptor compared to the human NK-1 receptor .
    WIN 51708
  • HY-103405

    Dopamine Receptor Neurological Disease
    NGD94-1 is a potent and selective dopamine D4 receptor antagonist. NGD94-1 shows high affinity for the cloned human D4.2 receptor (Ki = 3.6 nM). NGD94-1 modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD94-1 can be used for neurological disease research [1][2].
    NGD94-1

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