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reduces side effects

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0527A
    Amitriptyline hydrochloride
    Maximum Cited Publications
    8 Publications Verification

    Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
    Amitriptyline hydrochloride
  • HY-109017

    VBP15

    Glucocorticoid Receptor Mineralocorticoid Receptor NF-κB Inflammation/Immunology
    Vamorolone (VBP15) is a first-in-class, orally active dissociative steroidal anti-inflammatory agent and membrane-stabilizer. Vamorolone improves muscular dystrophy without side effects. Vamorolone shows potent NF-κB inhibition and substantially reduces hormonal effects .
    Vamorolone
  • HY-B0527
    Amitriptyline
    Maximum Cited Publications
    8 Publications Verification

    Serotonin Transporter Trk Receptor Sodium Channel 5-HT Receptor Histamine Receptor Adrenergic Receptor mAChR Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
    Amitriptyline
  • HY-P10709

    Collagen Cardiovascular Disease Cancer
    CREKA peptide is a selective non-covalent binding agent targeting fibrin, type IV collagen, and fibronectin, often used as a targeting ligand to modify delivery carriers. CREKA peptide specifically recognizes fibrin, fibronectin, and type IV collagen that are excessively deposited in the tumor microenvironment or fibrotic tissue, mediating the targeted accumulation of the carrier at the lesion site and promoting drug internalization into target cells (such as cancer cells and activated hepatic stellate cells). CREKA peptide can enhance targeted delivery efficiency, increase drug concentration at the lesion site, and reduce systemic side effects .
    CREKA peptide
  • HY-155008
    PROTAC HK2 Degrader-1
    2 Publications Verification

    PROTACs Hexokinase Cancer
    PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research .
    PROTAC HK2 Degrader-1
  • HY-B0237

    DL-Aminoglutethimide

    Cytochrome P450 Neurological Disease Endocrinology Cancer
    Aminoglutethimide (DL-Aminoglutethimide) is an orally active anticonvulsant with various endocrine-related side effects. Aminoglutethimide blocks multiple steroid hormone synthesis pathways by inhibiting several cytochrome P-450-dependent hydroxylases, such as aromatase, cholesterol side-chain cleavage enzyme, 11-hydroxylase, and 18-hydroxylase, with IC50 values of 0.3, 3.5, 120, and 20 μM, respectively. Aminoglutethimide reduces cortisol levels. Aminoglutethimide can be used in research on Cushing's syndrome, breast cancer, and other conditions .
    Aminoglutethimide
  • HY-160955

    Phosphatase Neurological Disease
    Z218484536 is a selective and brain-penetrant phosphoserine phosphatase (PSPH) inhibitor. Z218484536 binds to PSPH with a Kd value of approximately 0.23 μM. Z218484536 reduces L-serine and D-serine levels in astrocytes. Z218484536 is able to suppress spontaneous epileptic seizures without causing serious side effects. Z218484536 also shows good anti-epileptic effects in the temporal lobe epilepsy (TLE) model .
    Z218484536
  • HY-145404
    Mitragynine pseudoindoxyl
    1 Publications Verification

    Opioid Receptor Metabolic Disease
    Mitragynine pseudoindoxyl is a potent orally active agonist of the μ-opioid receptor (MOR-1, Ki=0.8 nM) and an antagonist of the δ-opioid receptor (DOR-1, Ki=3.0 nM). Mitragynine pseudoindoxyl has moderate affinity for the κ-opioid receptor (KOR-1, Ki=24 nM) and does not recruit β-arrestin-2, acting through G protein-mediated signaling pathways without β-arrestin-2-related activation. Mitragynine pseudoindoxyl produces potent analgesic activity through a mixed μ-agonist/δ-antagonist mechanism, with low side effects such as physical dependence, respiratory depression, and constipation, and no rewarding or aversive behaviors. Mitragynine pseudoindoxyl reduces hyperactivity, inhibits GI transit, and enhances characteristics, making it a potential analgesic .
    Mitragynine pseudoindoxyl
  • HY-P1723
    Spexin
    2 Publications Verification

    Neuropeptide Q

    Neuropeptide Y Receptor Apoptosis Ferroptosis Autophagy Cardiovascular Disease Neurological Disease
    Spexin (Neuropeptide Q) is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin can function through both central and peripheral actions. Spexin upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
    Spexin
  • HY-125961

    FGFR Glycosyltransferase Cancer
    T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 μM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream) .
    T3Inh-1
  • HY-W145481A

    Carob galactomannan

    Sirtuin Inflammation/Immunology
    D-Galacto-D-mannan (Carob galactomannan) is an orally active Dectin-2 agonist. D-Galacto-D-mannan exerts antioxidant activity against hydroxyl radical generation. D-Galacto-D-mannan activates Dectin-2 to trigger downstream signaling pathways, promote the expression of immunoregulatory molecules, coordinate innate and adaptive immune responses, and inhibit excessive inflammatory responses by upregulating the expression of Sirtuin 1. When used as a vaccine adjuvant, D-Galacto-D-mannan induces cellular and humoral immune responses, promotes IFNγ secretion, increases antibody levels and virus neutralization titers, and elevates the levels of immunoglobulin G and A. D-Galacto-D-mannan can serve as an adjuvant for foot-and-mouth disease vaccines, enhance the vaccine-mediated ability of hosts to defend against viral infection in mice, and reduce local side effects at the inoculation site in pigs. D-Galacto-D-mannan can be used in the research of inflammatory and immune diseases, such as foot-and-mouth disease .
    D-Galacto-D-mannan
  • HY-B0527AR
    Amitriptyline hydrochloride (Standard)
    4 Publications Verification

    Reference Standards Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline hydrochloride (Standard)
  • HY-145736A

    Drug-Linker Conjugates for ADC Apoptosis Cancer
    β-Glucuronide-dPBD-PEG5-NH2 TFA is the β-glucuronide-linked pyrrolobenzodiazepine dimer, which binds to the prenylated antibody for synthesis of antibody-drug conjugate (ADC) cIRCR201-dPBD.β-glucuronide-linkage as a cleavable linker. β-Glucuronide-dPBD-PEG5-NH2 TFA, as a proagent of cIRCR201-dPBD, reduces side effects. β-Glucuronide-dPBD-PEG5-NH2 TFA can induce apoptosis and arrest cell cycle. β-Glucuronide-dPBD-PEG5-NH2 TFA has antitumor activity .
    β-Glucuronide-dPBD-PEG5-NH2 TFA
  • HY-17509
    Deracoxib
    1 Publications Verification

    SC 046; SC 46; SC 59046

    COX Apoptosis Neurological Disease Inflammation/Immunology Cancer
    Deracoxib (SC 046; SC 59046), an orally active COX-2 inhibitor, is a veterinary nonsteroidal anti-inflammatory agent used exclusively in dogs. Deracoxib inhibits the COX-2 enzyme to reduce the production of prostaglandins, effectively controlling pain and inflammation after canine soft tissue surgery. Deracoxib reduces the inhibition of COX-1 and lowers the risk of gastrointestinal side effects. Deracoxib induces tumor cell cycle arrest and apoptosis, and shows anti-tumor activity in canine osteosarcoma, breast tumors and bladder transitional cell carcinomas .
    Deracoxib
  • HY-B0527AS

    Isotope-Labeled Compounds Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline-d6 hydrochloride
  • HY-145736

    Drug-Linker Conjugates for ADC Apoptosis Cancer
    β-Glucuronide-dPBD-PEG5-NH2 is the β-glucuronide-linked pyrrolobenzodiazepine dimer, which binds to the prenylated antibody for synthesis of antibody-drug conjugate (ADC) cIRCR201-dPBD. β-glucuronide-linkage as a cleavable linker. β-Glucuronide-dPBD-PEG5-NH2, as a proagent of cIRCR201-dPBD, reduces side effects. β-Glucuronide-dPBD-PEG5-NH2 can induce apoptosis and arrest cell cycle. β-Glucuronide-dPBD-PEG5-NH2 has antitumor activity .
    β-Glucuronide-dPBD-PEG5-NH2
  • HY-17509S

    SC 046-d3; SC 46-d3; SC 59046-d3

    Isotope-Labeled Compounds COX Apoptosis Neurological Disease Inflammation/Immunology Cancer
    Deracoxib-d3 (SC 046-d3; SC 59046-d3) is the deuterium labeled Deracoxib (HY-17509). Deracoxib, an orally active COX-2 inhibitor, is a veterinary nonsteroidal anti-inflammatory agent used exclusively in dogs. Deracoxib inhibits the COX-2 enzyme to reduce the production of prostaglandins, effectively controlling pain and inflammation after canine soft tissue surgery. Deracoxib reduces the inhibition of COX-1 and lowers the risk of gastrointestinal side effects. Deracoxib induces tumor cell cycle arrest and apoptosis, and shows anti-tumor activity in canine osteosarcoma, breast tumors and bladder transitional cell carcinomas.
    Deracoxib-d3
  • HY-109747

    MMP Cancer
    RO-28-2653 is an orally active matrix metalloproteinase (MMP) inhibitor. RO-28-2653 exhibits highly selective inhibitory effects on MMP2, MMP9 and membrane-type 1-MMP, and may reduce side effects (such as musculoskeletal pain) compared to broad-spectrum MMP inhibitors. RO-28-2653 shows significant tumor growth inhibition in a rat prostate model. RO-28-2653 can be used in studies of hormone-sensitive tumors .
    RO-28-2653
  • HY-P1723A

    Neuropeptide Q TFA

    Neuropeptide Y Receptor Apoptosis Ferroptosis Autophagy Cardiovascular Disease Metabolic Disease
    Spexin (Neuropeptide Q) TFA is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin TFA can function through both central and peripheral actions. Spexin TFA upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin TFA improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin TFA can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
    Spexin TFA
  • HY-124406

    mGluR Neurological Disease
    A-794282 is a compound with analgesic activity and is a selective mGlu1 receptor antagonist that significantly reduces pain behaviors in a postoperative pain model, but motor side effects may occur at higher doses.
    A-794282
  • HY-118499

    RIV-2093

    Drug Derivative Endocrinology
    Alpiropride (RIV-2093) is a metoclopramide (HY-17382) analog that is effective in reducing the gastrointestinal side effects of cancer chemotherapy drugs. In animal studies, alpiropride showed a stronger antiemetic effect than metoclopramide .
    Alpiropride
  • HY-130587

    Piperazine sultosylate; A-585

    LDLR Apolipoprotein Metabolic Disease
    Sultosilic acid piperazine salt (Piperazine sultosylate; A-585) is a lipid-lowering agent. Sultosilic acid piperazine salt modifies the blood lipids levels, reduces platelet adhesiveness without promoting peroxisomal activity of hepatocytes or producing other adverse side-effects .
    Sultosilic acid piperazine salt
  • HY-119385

    Dopamine Receptor Neurological Disease
    Savoxepin mesylate is a D2 dopamine receptor (D2 Dopamine Receptor) antagonist with antipsychotic activity. Savoxepin mesylate selectively blocks dopamine D2 receptors in the hippocampus while having no significant effect on D2 receptors in the striatum. This selective blockade helps reduce the risk of extrapyramidal side effects (EPS) .
    Savoxepin mesylate
  • HY-159916

    Toll-like Receptor (TLR) Inflammation/Immunology
    AYK004 is a TLR7/8 agonist that enhances immune responses by activating the TLR signaling pathway. AYK004 is an adenine derivative with a favorable hydrophilic-lipophilic balance, which improves the loading capacity and stability in immunoadjuvant systems such as liposomes, while reducing the side effects of the immunoadjuvant system in systemic immunity .
    AYK004
  • HY-144036

    DNA-PK Cancer
    DNA-PK-IN-3 is a potent inhibitor of DNA-PK. DNA-PK-IN-3 synergistically enhances the effect of radiotherapy and chemotherapy and effectively inhibits tumor growth. DNA-PK-IN-3 also effectively reduces the damage to normal cells and reducing side effects. DNA-PK-IN-3 has the potential for the research of cancer disease (extracted from patent WO2021213460A1, compound 4) .
    DNA-PK-IN-3
  • HY-159923

    Opioid Receptor Neurological Disease
    BPRMU191 is a μ-opioid receptor (MOR) modulator that converts small-molecule morphinan antagonists into G protein-biased MOR agonists, thereby inducing MOR-dependent activation and analgesic effects. Co-administration of BPRMU191 with morphinan antagonists provides analgesia while reducing side effects such as gastrointestinal dysfunction, antinociceptive tolerance, and dependency-related adverse effects. BPRMU191, in combination with morphinan antagonists, offers a potential strategy for studying severe pain management and G protein-coupled receptor modulation .
    BPRMU191
  • HY-121974

    Opioid Receptor Neurological Disease
    SR14150 is a partial agonist of the NOP receptor with high affinity. The biological activity of SR14150 makes it potentially useful for the development of a new generation of multi-target opioids designed to simultaneously improve analgesia and reduce side effects. The activity of SR14150 and its interaction with other opioid receptors may provide new inhibitory options for the management of chronic pain .
    SR14150
  • HY-159169

    COX Epoxide Hydrolase Lipoxygenase Inflammation/Immunology
    5-LOX/sEH-IN-1 (Compound 8o) is a dual 5-LOX/sEH-IN-1 inhibitor with cardioprotective effects, exhibiting IC50 values of 3.05 μM and 2.20 nM respectively, and 5-LOX/sEH-IN-1 can also inhibit the activity of COX-2 (IC50=10.50 μM). 5-LOX/sEH-IN-1 has analgesic and anti-inflammatory effects, while reducing ulcer pathogenicity, and can be used to develop anti-inflammatory agents with fewer gastrointestinal and cardiovascular side effects .
    5-LOX/sEH-IN-1
  • HY-117649

    Estrogen Receptor/ERR Cancer
    RU-39411 is a steroidal anti-estrogen with mixed estrogenic/antiestrogen activity. RU-39411 has shown inhibitory effects on cell growth in the MCF-7 breast cancer model, with the effect being correlated with its binding affinity to the estrogen receptor. RU-39411 was able to downregulate the estrogen binding capacity of cells, but did not reduce estrogen receptor mRNA levels, indicating that the grafting of its side chain prevents the antagonistic effects usually associated with steroidal estrogens. The administration of RU-39411 can promote the synthesis of progesterone receptors, further supporting its activity as an estrogen .
    RU-39411
  • HY-17509R

    SC 046 (Standard); SC 46 (Standard); SC 59046 (Standard)

    Reference Standards COX Apoptosis Neurological Disease Inflammation/Immunology Cancer
    Deracoxib (SC 046; SC 59046) (Standard) is the analytical standard of Deracoxib (HY-17509). This product is intended for research and analytical applications. Deracoxib, an orally active COX-2 inhibitor, is a veterinary nonsteroidal anti-inflammatory agent used exclusively in dogs. Deracoxib inhibits the COX-2 enzyme to reduce the production of prostaglandins, effectively controlling pain and inflammation after canine soft tissue surgery. Deracoxib reduces the inhibition of COX-1 and lowers the risk of gastrointestinal side effects. Deracoxib induces tumor cell cycle arrest and apoptosis, and shows anti-tumor activity in canine osteosarcoma, breast tumors and bladder transitional cell carcinomas
    Deracoxib (Standard)
  • HY-W703540

    SC 046-d4; SC 46-d4; SC 59046-d4

    Isotope-Labeled Compounds Apoptosis COX Neurological Disease Inflammation/Immunology Cancer
    Deracoxib-d4 (SC 046-d4; SC 59046--d4) is deuterium labeled Deracoxib (HY-17509). Deracoxib, an orally active COX-2 inhibitor, is a veterinary nonsteroidal anti-inflammatory agent used exclusively in dogs. Deracoxib inhibits the COX-2 enzyme to reduce the production of prostaglandins, effectively controlling pain and inflammation after canine soft tissue surgery. Deracoxib reduces the inhibition of COX-1 and lowers the risk of gastrointestinal side effects. Deracoxib induces tumor cell cycle arrest and apoptosis, and shows anti-tumor activity in canine osteosarcoma, breast tumors and bladder transitional cell carcinomas.
    Deracoxib-d4
  • HY-W328882

    Endogenous Metabolite Cardiovascular Disease
    3-(2-Aminopropyl)phenol is a biologically active compound with significant blood pressure-raising activity. 3-(2-Aminopropyl)phenol can effectively improve the symptoms of orthostatic hypotension in patients. 3-(2-Aminopropyl)phenol can significantly increase blood pressure at rest and when standing after oral administration. 3-(2-Aminopropyl)phenol can help reduce pathological orthostatic adjustment disorders. 3-(2-Aminopropyl)phenol has a relatively small effect on heart rate, and no significant side effects have been observed .
    3-(2-Aminopropyl)phenol
  • HY-175486

    Opioid Receptor Neurological Disease
    KOR agonist 6 is a KOR agonist (Ki = 0.25 pM). KOR agonist 6 shows agonistic activity at MOR and DOR in CHO cells and inhibits Forskolin (HY-15371)-stimulated cAMP accumulation. KOR agonist 6 stimulates KOR-mediated [ 35S]GTPγS binding and inhibits cAMP accumulation in KOR-expressing HEK293 cells with potent agonistic activity, while showing lower β-arrestin recruitment potency. KOR agonist 6 demonstrates anti-nociceptive efficacy in mice. KOR agonist 6 can be used for the study of analgesics with reduced central nervous system (CNS) side effects .
    KOR agonist 6
  • HY-16778

    Drug Derivative Neurological Disease Metabolic Disease Endocrinology
    Etiguanfacine is a derivative of Guanfacine (HY-17416A). Etiguanfacine can be used for research to reduce the gastrointestinal side effects of Guanfacine .
    Etiguanfacine
  • HY-180382

    Cholinesterase (ChE) Cardiovascular Disease
    Trimethidinium methosulfate is an orally active ganglionic blocker with central antihypertensive activity. Trimethidinium methosulfate inhibits the conduction of sympathetic ganglia and reduces vascular contraction. Trimethidinium methosulfate acts on the cerebrovascular motor center and lowers peripheral vascular resistance. Trimethidinium methosulfate has cholinergic nerve inhibitory side effects, but they are relatively mild. Trimethidinium methosulfate can be used in hypertension research .
    Trimethidinium methosulfate
  • HY-183489

    Trace Amine-associated Receptor (TAAR) Neurological Disease Metabolic Disease
    TAAR1-agonist-4 is a TAAR1 agonist and oral hypoglycemic agent with an EC50 of 0.0046 μM for TAAR1. TAAR1-agonist-4 alleviates antipsychotic-related metabolic side effects, improves negative and cognitive symptoms, and reduces drug abuse behaviors. TAAR1-agonist-4 is applicable to research on schizophrenia, acute manic episodes associated with bipolar disorder, and glucose intolerance .
    TAAR1-agonist-4
  • HY-180822

    COX TNF Receptor Interleukin Related Inflammation/Immunology
    COX-2-IN-63 (Compound 6k) is an orally active COX-2 inhibitor with an IC50 of 0.89 μM. COX-2-IN-63 reduces the levels of inflammatory mediators PGE2, TNF-α, and IL-6. COX-2-IN-63 can effectively alleviate acute inflammation in a rat paw edema model and has a lower risk of gastrointestinal side effects. COX-2-IN-63 can be used in anti-inflammatory research .
    COX-2-IN-63
  • HY-181546

    Btk PERK Syk HMG Family Cancer
    Ibt-DOX is a BTK inhibitor with an IC50 of 2.89 nM. Ibt-DOX is also a targeted covalent activated chemotherapeutic agent composed of the targeting ligand Ibrutinib (HY-10997), Doxorubicin (DOX) (HY-15142A), α-MAA (HY-W017180), and a linker (HY-Y0892). Ibt-DOX specifically binds to BTK and releases DOX, synergistically achieving BTK inhibition and chemotherapeutic killing, significantly enhancing toxicity against B-cell lymphoma cells and greatly reducing the toxic side effects of DOX on BTK-negative cells. Ibt-DOX can be used in lymphoma-related research .
    Ibt-DOX
  • HY-182517

    TRP Channel Inflammation/Immunology
    AG1529 is a TRPV1 inhibitor and capsaicinoid-based soft agent with a human TRPV1 IC50 of 0.9-0.93 μM. AG1529 reversibly blocks capsaicin-evoked TRPV1 activation, binds to the TRPV1 capsaicin binding site, moderately affects pH-induced TRPV1 gating, and does not alter voltage- or heat-mediated TRPV1 responses. AG1529 suppresses TRPV1-mediated neuronal excitability, reduces capsaicin- and pH-evoked neuronal firing, abolishes histaminergic and inflammation-mediated TRPV1 sensitization. AG1529 exhibits anti-nociceptive and antipruritic effects, attenuates in vivo hyperalgesia and pruritus, dose-dependently reduces acute histaminergic itch in rodents, and mildly blocks hTRPA1 and hTRPM8 channel activity. AG1529 undergoes hydrolysis and dermal deactivation, minimizes TRPV1-associated side reactions, does not evoke capsaicin-like burning sensation, and does not disrupt physiological thermal regulation. AG1529 can be used for the research of inflammatory cutaneous nociception and acute histaminergic pruritus .
    AG1529

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