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bioavailability modulator

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45

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2

Biochemical Assay Reagents

4

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Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N1445
    Isoquercitrin
    Maximum Cited Publications
    7 Publications Verification

    Isoquercetin; Quercetin 3-glucoside

    		 NF-κB NO Synthase Inflammation/Immunology Cancer
    Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway . Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies .
    Isoquercitrin
  • HY-W004260
    Arachidic acid
    3 Publications Verification

    Eicosanoic acid

    		 Endogenous Metabolite Neurological Disease
    Arachidic acid is an orally bioavailable membrane fluidity modulator and receptor/ion channel effector. Arachidic acid does not activate arachidonic acid-sensitive K + channels in rat midbrain and hypothalamic neurons. Arachidic acid alleviates age-related spatial cognitive impairment. Arachidic acid is applicable for research related to age-related spatial cognitive impairment .
    Arachidic acid
  • HY-Y0669
    Pipecolic acid
    2 Publications Verification

    		 Endogenous Metabolite YAP Glutathione Peroxidase Ferroptosis Neurological Disease Metabolic Disease Inflammation/Immunology
    Pipecolic acid is an orally bioavailable, blood-brain barrier-permeable metabolite of lysine with antioxidant, inhibitor, and inducer activity. Pipecolic acid modulates the YAP-GPX4 signaling pathway, reduces retinal vascular tube formation, and mitigates ferroptosis. Pipecolic acid potentiates voltage-sensitive Ca 2+ channel currents and induces neuronal apoptosis. Pipecolic acid can be used for the research of diabetic retinopathy .
    Pipecolic acid
  • HY-111498A
    RGX-104
    3 Publications Verification

    Abequolixron

    		 LXR Inflammation/Immunology Cancer
    RGX-104 is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
    RGX-104
  • HY-105296
    Blarcamesine
    3 Publications Verification

    		 Sigma Receptor mAChR Cancer
    Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome .
    Blarcamesine
  • HY-114530
    LY2452473
    5+ Cited Publications

    		 Androgen Receptor Metabolic Disease Cancer
    LY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
    LY2452473
  • HY-124634
    PZ-2891
    4 Publications Verification

    		 PANK Neurological Disease
    PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively .
    PZ-2891
  • HY-N0712
    Typhaneoside
    3 Publications Verification

    		 Autophagy mTOR Akt FXR Cardiovascular Disease Neurological Disease Metabolic Disease Cancer
    Typhaneoside is an orally bioavailable signal modulator and cellular regulator. Typhaneoside regulates the PI3K/Akt/mTOR autophagy transduction pathway. Typhaneoside promotes the activation of AMP-activated protein kinase and Caspase-3, induces apoptosis, ferroptosis, autophagy, ROS accumulation, and cell cycle arrest at the G2/M phase, and reduces cancer cell viability. Typhaneoside activates the farnesoid X receptor signaling pathway, improves glucose and lipid metabolism, alleviates inflammatory responses, oxidative stress and hepatic lipid accumulation, and exerts hepatoprotective effects. Typhaneoside is applicable to research related to post-myocardial infarction heart failure, acute myeloid leukemia, non-alcoholic fatty liver disease, and neurological disorders .
    Typhaneoside
  • HY-104037
    Cintirorgon
    Maximum Cited Publications
    8 Publications Verification

    LYC-55716

    		 ROR Cancer
    Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival .
    Cintirorgon
  • HY-118424
    JNJ-55511118

    		iGluR Neurological Disease Metabolic Disease
    JNJ-55511118 is a selective TARP γ-8 binding AMPA receptor modulator with oral bioavailability and blood-brain barrier permeability, with a Ki of 26 nM. JNJ-55511118 reduces voluntary intake of sweetened alcohol in male mice. In rodent models, JNJ-55511118 inhibits hippocampal neurotransmission, reduces specific electroencephalogram frequency bands, induces transient hyperlocomotion, impairs learning and memory abilities, and exerts anticonvulsant effects. JNJ-55511118 is applicable to research related to alcohol use disorder and seizures .
    JNJ-55511118
  • HY-124600
    NVR 3-778
    3 Publications Verification

    		 HBV Infection
    NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity .
    NVR 3-778
  • HY-B2235C
    L-α-Lecithin (soybean)

    		Biochemical Assay Reagents Glutathione Peroxidase Metabolic Disease
    L-α-Lecithin (soybean) is an orally active phospholipid. L-α-Lecithin (soybean) increases the bioavailability of Lutein in plasma and eyes of Rattus norvegicus, enhances plasma Glutathione peroxidase activity, and regulates fatty acids in plasma and tissues .
    L-α-Lecithin (soybean)
  • HY-107457
    AZD-8529
    1 Publications Verification

    		 mGluR Neurological Disease
    AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
    AZD-8529
  • HY-135891
    AZD2423

    		CCR Neurological Disease
    AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux .
    AZD2423
  • HY-170419
    APJ receptor agonist 10

    		Apelin Receptor (APJ) Cardiovascular Disease
    APJ receptor agonist 10 (Compound I choline salt) modulates the activity of APJ receptor and can be used in research about pulmonary arterial hypertension. APJ receptor agonist 10 exhibits good bioavailability other than its free base form .
    APJ receptor agonist 10
  • HY-122559
    BMS-984923

    		mGluR Neurological Disease
    BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling .
    BMS-984923
  • HY-147403S
    Tebideutorexant

    JNJ-61393215

    		 Orexin Receptor (OX Receptor) Isotope-Labeled Compounds Neurological Disease
    Tebideutorexant is an OX1R-selective inhibitor with oral bioavailability and blood-brain barrier permeability, with human OX1R pKi 8.17 and rat OX1R pKi 8.13.Tebideutorexant selectively modulates OX1R, with no significant functional effect on OX2R. Tebideutorexant can be used for the research of panic and anxiety disorders .
    Tebideutorexant
  • HY-117482
    BPN-15606

    		γ-secretase Neurological Disease
    BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance .
    BPN-15606
  • HY-N1445R
    Isoquercitrin (Standard)
    1 Publications Verification

    Isoquercetin (Standard); Quercetin 3-glucoside (Standard)

    		 Reference Standards NF-κB NO Synthase Inflammation/Immunology Cancer
    Isoquercetin (Standard) is the analytical standard of Isoquercetin. This product is intended for research and analytical applications. Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway . Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies .
    Isoquercitrin (Standard)
  • HY-107987
    CXCR7 modulator 1

    		CXCR Endocrinology
    CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM .
    CXCR7 modulator 1
  • HY-114403
    VU6012962

    		mGluR Neurological Disease
    VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM .
    VU6012962
  • HY-153715
    NV-354

    Mitochondria modulator-1

    		 Biochemical Assay Reagents Metabolic Disease
    NV-354 (Mitochondria modulator-1) (compound 1) is a mitochondrial regulator that stimulates mitochondrial ATP production. NV-354 has good oral bioavailability, blood-brain barrier permeability, and good plasma stability. NV-354 has the potential to study mitochondrial diseases .
    NV-354
  • HY-155088
    MK-8768

    		mGluR Metabolic Disease
    MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
    MK-8768
  • HY-107457A
    AZD-8529 mesylate
    1 Publications Verification

    		 mGluR Neurological Disease
    AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes .
    AZD-8529 mesylate
  • HY-14419
    TCN238

    		mGluR Neurological Disease
    TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM .
    TCN238
  • HY-133555
    mGluR2 antagonist 1

    		mGluR Neurological Disease
    mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability .
    mGluR2 antagonist 1
  • HY-120004
    PF-06827443

    		mAChR Infection
    PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion .
    PF-06827443
  • HY-145559
    Cemdomespib

    KU-596

    		 HSP Metabolic Disease
    Cemdomespib (KU-596) is a highly bioavailable second-generation Hsp90 modulator. Cemdomespib has shown efficacy in improving sensory deficits in models of diabetic peripheral neuropathy. Cemdomespib induces Hsp70 levels and manifest neuroprotective activity through induction of the heat shock response .
    Cemdomespib
  • HY-141431
    Cbl-b-IN-2

    		E1/E2/E3 Enzyme Inflammation/Immunology Cancer
    Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent .
    Cbl-b-IN-2
  • HY-124372
    JNJ-46356479

    		mGluR Neurological Disease
    JNJ-46356479 is a selective and orally bioavailable mGlu2 receptor positive allosteric modulator (PAM), with the EC50 of 78 nM. JNJ-46356479 shows active in vivo .
    JNJ-46356479
  • HY-143880
    MRGPRX1 agonist 4

    		Mas-related G-protein-coupled Receptor (MRGPR) Neurological Disease
    MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain .
    MRGPRX1 agonist 4
  • HY-16622A
    GSK 1842799 TFA

    		LPL Receptor Others
    GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .
    GSK 1842799 TFA
  • HY-120184
    VU0467485

    AZ13713945

    		 mAChR Neurological Disease
    VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
    VU0467485
  • HY-147528
    mGluR2 modulator 2

    		mGluR Neurological Disease
    mGluR2 modulator 2 (compound 2) is a potent, selective and orally bioavailable mGluR2 positive allosteric modulator with an EC50 value of 0.13 μM. mGluR2 modulator 2 can be used for researching antipsychotic .
    mGluR2 modulator 2
  • HY-176420
    VU6031545

    		mGluR Neurological Disease
    VU6031545 is a potent mGlu 5 negative allosteric modulator with an IC50 of 15 nM. VU6031545 has excellent brain penetrant and oral bioavailability in rats .
    VU6031545
  • HY-124600R
    NVR 3-778 (Standard)

    		HBV Infection
    NVR 3-778 (Standard) is the analytical standard of NVR 3-778. This product is intended for research and analytical applications. NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity .
    NVR 3-778 (Standard)
  • HY-104037A
    Cintirorgon sodium

    LYC-55716 sodium

    		 ROR Cancer
    Cintirorgon sodium is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon sodium (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival .
    Cintirorgon sodium
  • HY-173032
    VU6033685

    		mGluR Neurological Disease
    VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8% .
    VU6033685
  • HY-117482A
    BPN-15606 besylate

    		γ-secretase Neurological Disease
    BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance .
    BPN-15606 besylate
  • HY-118285
    Ro4491533

    		mGluR Neurological Disease
    Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.
    Ro4491533
  • HY-107987R
    CXCR7 modulator 1 (Standard)

    		Reference Standards CXCR Endocrinology
    CXCR7 modulator 1 (Standard) is the analytical standard of CXCR7 modulator 1 (HY-107987). This product is intended for research and analytical applications. CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM .
    CXCR7 modulator 1 (Standard)
  • HY-107457AR
    AZD-8529 mesylate (Standard)

    		Reference Standards mGluR Neurological Disease
    AZD-8529 mesylate (Standard) is the analytical standard of AZD-8529 (mesylate) (HY-107457A). This product is intended for research and analytical applications. AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes .
    AZD-8529 mesylate (Standard)
  • HY-105296R
    Blarcamesine (Standard)

    		Reference Standards Sigma Receptor mAChR Cancer
    Blarcamesine (Standard) is the analytical standard of Blarcamesine (HY-105296). This product is intended for research and analytical applications. Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome .
    Blarcamesine (Standard)
  • HY-104037R
    Cintirorgon (Standard)

    LYC-55716 (Standard)

    		 Reference Standards ROR Cancer
    Cintirorgon (Standard) is the analytical standard of Cintirorgon (HY-104037). This product is intended for research and analytical applications. Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival .
    Cintirorgon (Standard)
  • HY-16265A
    JI-101 hydrochloride

    		Ephrin Receptor PDGFR VEGFR Cancer
    JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity .JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis .JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes .JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route .JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors .
    JI-101 hydrochloride

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