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intracranial

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29

Inhibitors & Agonists

1

Fluorescent Dyes

8

Peptides

1

Inhibitory Antibodies

1

Natural
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3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B1060
    Methylprednisolone succinate sodium
    2 Publications Verification

    Methylprednisolone hydrogen succinate sodium

    		 Glucocorticoid Receptor Infection Neurological Disease Inflammation/Immunology Cancer
    Methylprednisolone succinate (Methylprednisolone hydrogen succinate) sodium is a prodrug of Methylprednisolone (HY-B0260) and glucocorticoid with immunosuppressant and anti-inflammatory activity. Methylprednisolone succinate sodium binds cytosolic glucocorticoid receptors, translocates to nuclei, and modulates target gene transcription. Methylprednisolone succinate sodium alters Bax, Bcl-2, occludin, and ZO-1 expression; attenuates TLR4/NF-κB signaling; suppresses proinflammatory cytokine production and immune cell activation. Methylprednisolone succinate sodium can be used for the research of intracranial haemorrhage, rheumatoid arthritis, multiple sclerosis, preterminal cancer, inflammatory conditions, shock, immediate-type hypersensitivity, acute myocardial ischemia, hypoxic heart muscle damage, and traumatic spinal cord injury .
    Methylprednisolone succinate sodium
  • HY-173629
    RMC-5127

    		Ras Apoptosis Cancer
    RMC-5127 is a small molecule inhibitor that binds to GTP-targeted KRAS G12V, with oral bioavailability and blood-brain barrier permeability. RMC-5127 inhibits the activities of the RAS and MAPK pathways, suppresses the proliferation of KRAS G12V-mutant cancer cells and induces their apoptosis. RMC-5127 can be used for the research of KRAS G12V-mutant non-small cell lung cancer, pancreatic ductal adenocarcinoma, colorectal cancer and intracranial KRAS G12V tumors .
    RMC-5127
  • HY-B1900
    Methylprednisolone succinate
    2 Publications Verification

    Methylprednisolone hydrogen succinate

    		 Glucocorticoid Receptor Bacterial Toll-like Receptor (TLR) NF-κB Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Methylprednisolone succinate (Methylprednisolone hydrogen succinate) is a prodrug of Methylprednisolone (HY-B0260) and glucocorticoid with immunosuppressant and anti-inflammatory activity. Methylprednisolone succinate binds cytosolic glucocorticoid receptors, translocates to nuclei, and modulates target gene transcription. Methylprednisolone succinate alters Bax, Bcl-2, occludin, and ZO-1 expression; attenuates TLR4/NF-κB signaling; suppresses proinflammatory cytokine production and immune cell activation. Methylprednisolone succinate can be used for the research of intracranial haemorrhage, rheumatoid arthritis, multiple sclerosis, preterminal cancer, inflammatory conditions, shock, immediate-type hypersensitivity, acute myocardial ischemia, hypoxic heart muscle damage, and traumatic spinal cord injury .
    Methylprednisolone succinate
  • HY-117656
    ESI-05
    4 Publications Verification

    NSC 116966

    		 Acyltransferase Neurological Disease Metabolic Disease
    ESI-05 is a specific exchange proteins directly activated by cAMP 2 (EPAC2) inhibitor. ESI-05 inhibits cAMP-mediated EPAC2 GEF activity with an IC50 of 0.43 μM. ESI-05 can be used for the research of diabetes, insulin secretion and neurological disorders .
    ESI-05
  • HY-131904A
    Hex

    		Enolase Parasite Infection Cancer
    Hex is an enolase inhibitor and antimalarial agent with Ki values of 74.4 nM and 269.4 nM for ENO2 and ENO1, respectively. Hex is a NfENO and TbENO inhibitor with IC50s value of 0.14 μM and 2.1 μM, respectively. Hex has antimalarial activity against Plasmodium falciparum 3D7, Naegleria fowleri trophozoites and Plasmodium berghei ANKA strain. Hex has anti-tumor effects against intracranial tumors .
    Hex
  • HY-153268
    Silevertinib
    2 Publications Verification

    BDTX-1535; EGFR-IN-76

    		 EGFR Infection Neurological Disease Metabolic Disease Cancer
    Silevertinib (BDTX-1535) is an irreversible, brain-penetrant, selective and orally active EGFR inhibitor with wild-type EGFR-sparing. Silevertinib targets key EGFR resistance mutations, including the kinase domain (C797S, L718Q, G724S, S768I), extracellular domain (EGFRvIII, A289X), and EGFR amplification. Silevertinib exerts anti-tumor activity with well tolerated in vivo. Silevertinib can be used for non-small cell lung cancer (NSCLC) and glioblastoma (GBM) research .
    Silevertinib
  • HY-B0383
    Almotriptan malate

    PNU180638

    		 5-HT Receptor Neurological Disease
    Almotriptan malate (PNU180638) is an orally active, highly selective agonist of the 5-HT1B/1D receptor (5-HT1B/1D receptor), with EC50 values of 1.6 nM and 3.1 nM, respectively. Almotriptan malate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan malate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan malate can be used in research related to migraine .
    Almotriptan malate
  • HY-N6784
    Oligomycin B

    		ATP Synthase Bacterial Apoptosis Antibiotic Infection Neurological Disease
    Oligomycin B is an antibiotic that acts as a non-selective inhibitor of ATP Synthase. Oligomycin B increases mitochondrial membrane potential. Oligomycin B induces apoptosis and necrosis. Oligomycin B impairs the motility of Plasmopara viticola zoospores and induces their lysis. Oligomycin B inhibits Magnaporthe oryzae (wheat blast fungus) and suppresses the development of wheat blast. Oligomycin B reduces hyphal growth and spore germination of Botrytis cinerea, and protects Arabidopsis thaliana against Botrytis cinerea infection. Oligomycin B exacerbates cytotoxic brain edema in rats with cerebral cortical contusion, increases intracranial pressure and brain water content, and aggravates mitochondrial damage in these rats. Oligomycin B is used in studies related to grape downy mildew, traumatic brain injury, wheat blast, and gray mold .
    Oligomycin B
  • HY-P11303
    PADRE peptide

    		CD74 MHC Neurological Disease Cancer
    PADRE peptide is a pan-HLA-DR binding epitope and immunostimulant. PADRE peptide binds to the peptide-binding groove of MHC class II molecules for presentation to CD4 + T cells, thereby effectively stimulating specific immune responses. PADRE peptide not only enhances anti-tumor immune responses, inhibits tumor growth and prolongs survival; it also significantly increases the frequency of E7-specific CD8 + T cells and improves therapeutic efficacy against TC-1 tumors when used in combination with E7 peptide-based vaccines and poly (I:C). The intensity of the immune response induced by PADRE peptide is lower than that of the Ii-PADRE DNA vaccine, and it fails to enhance the immune effect of CRT-E7 DNA. PADRE peptide is widely applicable to research on related tumors such as melanoma, glioblastoma and cervical cancer .
    PADRE peptide
  • HY-124813
    PDZ1i

    113B7

    		 FAK EGFR MMP NF-κB SDCBP Cancer
    PDZ1i (113B7) is a inhibitor of MDA-9/Syntenin, with selective binding to the PDZ1 domain. PDZ1i inhibits radiation-induced invasion of glioblastoma (GBM) cells, radiosensitizes GBM cells, and impairs GBM-related signaling pathways (including Src/EphA2, EGFRvIII/FAK, and NF-κB). PDZ1i reduces radiation-induced secretion of invasion-related proteases (MMP-2, MMP-9, ADAM9). PDZ1i shows anti-tumor effects in nude mice bearing intracranial U1242-luc xenografts or GBM xenografts. PDZ1i can be used for the study of glioblastoma (GBM), breast cancer and prostate cancer .
    PDZ1i
  • HY-B0383A
    Almotriptan

    PNU180638 free base

    		 5-HT Receptor Neurological Disease
    Almotriptan (PNU180638 free base) is an orally active, highly selective agonist of the 5-HT1B/1D receptor (5-HT1B/1D receptor), with EC50 values of 1.6 nM and 3.1 nM, respectively. Almotriptan shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan can be used in research related to migraine .
    Almotriptan
  • HY-161275
    BI-4732

    		EGFR Akt ERK Ribosomal S6 Kinase (RSK) Cancer
    BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) .
    BI-4732
  • HY-P10427
    DV1

    		CXCR Dengue Virus Neurological Disease Inflammation/Immunology Cancer
    DV1 is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases .
    DV1
  • HY-B1900R
    Methylprednisolone succinate (Standard)
    1 Publications Verification

    Methylprednisolone hydrogen succinate (Standard)

    		 Reference Standards Glucocorticoid Receptor Bacterial Toll-like Receptor (TLR) NF-κB Metabolic Disease Inflammation/Immunology Cancer
    Methylprednisolone succinate (Standard) is the analytical standard of Methylprednisolone succinate (HY-B1900). This product is intended for research and analytical applications. Methylprednisolone succinate (Methylprednisolone hydrogen succinate) is a prodrug of Methylprednisolone (HY-B0260) and glucocorticoid with immunosuppressant and anti-inflammatory activity. Methylprednisolone succinate binds cytosolic glucocorticoid receptors, translocates to nuclei, and modulates target gene transcription. Methylprednisolone succinate alters Bax, Bcl-2, occludin, and ZO-1 expression; attenuates TLR4/NF-κB signaling; suppresses proinflammatory cytokine production and immune cell activation. Methylprednisolone succinate can be used for the research of intracranial haemorrhage, rheumatoid arthritis, multiple sclerosis, preterminal cancer, inflammatory conditions, shock, immediate-type hypersensitivity, acute myocardial ischemia, hypoxic heart muscle damage, and traumatic spinal cord injury .
    Methylprednisolone succinate (Standard)
  • HY-117902
    SRI-31142

    		Dopamine Transporter Neurological Disease
    SRI-31142 is a putative, brain-penetrant allosteric inhibitor of the dopamine transporter (DAT). In behavioral studies using intracranial self-stimulation (ICSS), SRI-31142 did not produce the abuse-related effects seen with cocaine and GBR-12935, but instead reduced ICSS responses and dopamine levels in the nucleus accumbens (NAc) at effective doses. SRI-31142 also blocked cocaine-induced increases in ICSS and NAc dopamine .
    SRI-31142
  • HY-P10427A
    DV1 TFA

    		CXCR Dengue Virus Infection
    DV1 TFA is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 TFA inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 TFA not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 TFA induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 TFA has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases .
    DV1 TFA
  • HY-178061
    APS03118

    		ERK RET Cancer
    APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research .
    APS03118
  • HY-150639
    Everafenib

    		Raf Cancer
    Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma .
    Everafenib
  • HY-175599
    Z6466608628

    		Molecular Glues Cardiovascular Disease Neurological Disease
    Z6466608628 is a selective PPIL4 molecular glue degrader with human PPIL4 EC50 values of 0.34 µM. Z6466608628 functionally recruits PPIL4 to CRBN, induces CRL4 CRBN-mediated ubiquitylation and degradation of PPIL4. Z6466608628 can be used for the research of intracranial aneurysms .
    Z6466608628
  • HY-178391
    SMU-037

    		ROS Kinase p38 MAPK ERK Apoptosis Cancer
    SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC₅₀ = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research .
    SMU-037
  • HY-W018475
    Rizatriptan

    MK 462 free base

    		 5-HT Receptor Neurological Disease
    Rizatriptan (MK 462 free base) is an orally active 5-HT1B/5-HT1D receptor agonist, with BBB permeability. Rizatriptan exerts significant anti-migraine effects by constricting intracranial and extracranial blood vessels and inhibiting neuropeptide release. Rizatriptan exhibits species- and tissue-specific metabolic characteristics; for example, it undergoes oxidative deamination mainly by MAO-A in the liver of brown rats, so co-administration with MAO-A inhibitors is prohibited. Rizatriptan may also exacerbate nitroglycerin-induced cutaneous allodynia, prolong the duration of central sensitization, and increase anxiety-like behavior and active drug-seeking behavior in mice. Rizatriptan has been widely used in studies related to migraine and medication-overuse headache .
    Rizatriptan
  • HY-19248
    ME-3277

    		Integrin Cardiovascular Disease Neurological Disease
    ME-3277 is a potent GPIIb/IIIa antagonist. ME-3277 reduces cerebral infarction without enhancing intracranial hemorrhage in photothrombotic occlusion of rabbit middle cerebral artery (MCA). ME-3277 can be used for the acute cerebral infarction research .
    ME-3277
  • HY-149696
    IR-Crizotinib

    		NF-κB Cancer
    IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC50=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research .
    IR-Crizotinib
  • HY-W335976
    Almotriptan hydrochloride

    		5-HT Receptor Neurological Disease
    Almotriptan (PNU180638) hydrochloride is an orally active, highly selective agonist of the 5-HT1B/1D receptor (5-HT1B/1D receptor), with EC50 values of 1.6 nM and 3.1 nM, respectively. Almotriptan hydrochloride shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan hydrochloride induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan hydrochloride can be used in research related to migraine.
    Almotriptan hydrochloride
  • HY-B0383AS
    Almotriptan hydrochloride-d6

    PNU180638 hydrochloride-d6

    		 Isotope-Labeled Compounds 5-HT Receptor Neurological Disease
    Almotriptan-d6 (PNU180638-d6) hydrochloride is the deuterium labeled Almotriptan hydrochloride. Almotriptan hydrochloride is an orally active, highly selective agonist of the 5-HT1B/1D receptor (5-HT1B/1D receptor), with EC50 values of 1.6 nM and 3.1 nM, respectively. Almotriptan hydrochloride shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan hydrochloride induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan hydrochloride can be used in research related to migraine.
    Almotriptan hydrochloride-d6
  • HY-B0383AS2
    Almotriptan-d3 benzoate

    PNU180638 free base-d3 benzoate

    		 Isotope-Labeled Compounds 5-HT Receptor Neurological Disease
    Almotriptan-d3 benzoate (PNU180638 free base-d3) is deuterated labeled Almotriptan benzoate. Almotriptan benzoate is an orally active, highly selective agonist of the 5-HT1B/1D receptor (5-HT1B/1D receptor), with EC50 values of 1.6 nM and 3.1 nM, respectively. Almotriptan benzoate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan benzoate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan benzoate can be used in research related to migraine.
    Almotriptan-d3 benzoate
  • HY-143797S
    Almotriptan-d6 maleate

    		Isotope-Labeled Compounds 5-HT Receptor Neurological Disease
    Almotriptan-d6 (PNU180638-d6) maleate is the deuterium labeled Almotriptan maleate. Almotriptan malate is an orally active, highly selective agonist of the 5-HT1B/1D receptor (5-HT1B/1D receptor), with EC50 values of 1.6 nM and 3.1 nM, respectively. Almotriptan malate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan malate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan malate can be used in research related to migraine.
    Almotriptan-d6 maleate
  • HY-175599A
    Z6466608628 hydrochloride

    		Molecular Glues Cardiovascular Disease Neurological Disease
    Z6466608628 hydrochloride is a selective PPIL4 molecular glue degrader with human PPIL4 EC50 values of 0.34 µM. Z6466608628 hydrochloride functionally recruits PPIL4 to CRBN, induces CRL4 CRBN-mediated ubiquitylation and degradation of PPIL4. Z6466608628 hydrochloride can be used for the research of intracranial aneurysms[1].
    Z6466608628 hydrochloride
  • HY-P99658A
    Imaprelimab (powder)

    		Transmembrane Glycoprotein Cardiovascular Disease Neurological Disease Cancer
    Imaprelimab (powder) is a humanized IgG1κ anti-CD146 antibody. Imaprelimab (powder) exerts anti-angiogenic effects on brain metastasis of lung cancer in animal models. Imaprelimab (powder) can be used in studies related to brain metastasis of non-small cell lung cancer .
    Imaprelimab (powder)

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