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X4

" in MedChemExpress (MCE) Product Catalog:

37

Inhibitors & Agonists

1

Fluorescent Dye

4

Peptides

1

Inhibitory Antibodies

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-145997

    Mas-related G-protein-coupled Receptor (MRGPR) Inflammation/Immunology
    MRGPRX4 modulator-1 (compound 31-2) is a potent mas-related g-protein receptor X4 (MRGPR X4) modulator, with antagonist activity of IC50 < 100 nM for MRGPR4. MRGPRX4 modulator-1 can be used for researching MRGPR X4 dependent diseases such as itch, pain, and autoimmune disorders .
    MRGPRX4 modulator-1
  • HY-147051

    Mas-related G-protein-coupled Receptor (MRGPR) Inflammation/Immunology
    MRGPRX4 modulator-2 (compound 1-55) is a potent MRGPR X4 modulator, possessing antagonist activity against MRGPR X4 with an IC50 < 100 nM. MRGPRX4 modulator-2 can be used for researching autoimmune diseases such as psoriasis, multiple sclerosis, Steven Johnson’s Syndrome, and other chronic itch conditions .
    MRGPRX4 modulator-2
  • HY-P7061A
    ALX 40-4C Trifluoroacetate
    1 Publications Verification

    Apelin Receptor (APJ) CXCR Infection Endocrinology
    ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
    ALX 40-4C Trifluoroacetate
  • HY-15971A
    AMD 3465
    4 Publications Verification

    GENZ-644494

    CXCR HIV Infection Endocrinology
    AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
    AMD 3465
  • HY-15971
    AMD 3465 hexahydrobromide
    4 Publications Verification

    GENZ-644494 hexahydrobromide

    CXCR HIV Infection Endocrinology
    AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
    AMD 3465 hexahydrobromide
  • HY-P10415

    hSA(408–423) peptide

    CXCR Infection Inflammation/Immunology Cancer
    EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM .
    EPI-X4
  • HY-122058A

    CXCR HIV Infection Inflammation/Immunology
    KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM .
    KRH-3955 hydrochloride
  • HY-122058

    HIV Infection
    KRH-3955 is a CXCR4 antagonist with good bioavailability and potent anti-HIV-1 activity. KRH-3955 can effectively inhibit the replication of X4 HIV-1, including clinical isolates from different donors. KRH-3955 also shows activity against recombinant X4 HIV-1 containing reverse transcriptase, protease and tyrosinase resistance mutations. KRH-3955 can inhibit the binding of SDF-1alpha to CXCR4 and calcium ion signaling through this receptor. KRH-3955 inhibits the binding of an antibody against CXCR4 to CXCR4, showing a potent antagonistic effect on CXCR4. KRH-3955 shows an oral bioavailability of 25.6% in rats and can inhibit the replication of X4 HIV-1 in vivo .
    KRH-3955
  • HY-167945

    Others Infection
    AMD-3329 is a potent and selective anti-HIV-1 and HIV-2 agent, exhibiting activity by inhibiting virus replication through binding to the chemokine receptor CXCR4, which serves as a co-receptor for the entry of X4 viruses.
    AMD-3329
  • HY-P7061

    CXCR Apelin Receptor (APJ) Infection Endocrinology
    ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
    ALX 40-4C
  • HY-12108

    HIV Integrase HIV Infection
    S 1360 is a potent and selective inhibitor of HIV-1 integrase. S 1360 inhibits the catalytic activity of purified integrase ( IC50: 20 nM). The EC50, and CC50 of S 1360 in MTT assay (MT-4 cells infected with HIV-1 IIIB) are 200 nM and 12 μM, respectively. S 1360 has antiviral activity against both X4 tropic and R5 tropic strains, as well as NRTI, NNRTI and PI drug-resistant variants .
    S 1360
  • HY-134851
    HIV-1 inhibitor-6
    1 Publications Verification

    HIV Infection
    HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to agents targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM .
    HIV-1 inhibitor-6
  • HY-160677

    P2X Receptor Neurological Disease
    P2X4 antagonist-2 is an antagonist for P2X4 with an IC50 of 24 nM .
    P2X4 antagonist-2
  • HY-160645

    P2X Receptor Inflammation/Immunology
    P2X4 antagonist-1 (Compound 24) is an antagonist for P2X4 with IC50 of 15 nM .
    P2X4 antagonist-1
  • HY-139090

    28-O-Acetyl-3-Oxobetulin; 3-oxo-28-O-Acetylbetulin

    Others Infection
    3-Oxobetulin acetate is a derivative of the cholesterol biosynthesis inhibitor Betulin (HY-N0083). It inhibits the growth of P388 murine lymphocytic leukemia cells (EC50=0.12 μg/mL), as well as human MCF-7 breast, SF-268 CNS, H460 lung, and KM20L2 colon cancer cells (GI50s=8, 10.6, 5.2, and 12.7 μg/mL, respectively), but not BxPC-3 pancreas or DU145 prostate cancer cells (GI50s=>10 μg/mL for both).2 3-Oxobetulin acetate inhibits replication of X4 tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblastoid cells (IC50=13.4 μM). It is also active against L. donovani amastigotes when used at a concentration of 50 μM.
    3-Oxobetulin acetate
  • HY-D2155

    Fluorescent Dye Others
    Texas red-X 4-succinimidyl ester is a derivative of Texas Red (HY-101878), an amphoteric rhodamine red fluorescent dye. Texas Red is widely used to study neuronal morphology and as a cell type-selective fluorescent marker for astrocytes, both in vivo and in slice preparations.
    Texas red-X 4-succinimidyl ester
  • HY-101910

    N-(p-Methylphenylsulfonyl)phenoxazine

    P2X Receptor Neurological Disease
    PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4.
    PSB-12062
  • HY-101911
    5-BDBD
    2 Publications Verification

    P2X Receptor Neurological Disease
    5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG) .
    5-BDBD
  • HY-131502

    P2X Receptor Inflammation/Immunology
    Taspine is a natural product with anti-inflammatory activity. Taspine suppresses P2X4 receptor activity via PI3K inhibition. Taspine inhibits pro-inflammatory signalling via inhibition of P2X4 receptors in macrophage .
    Taspine
  • HY-151546

    P2X Receptor Neurological Disease
    MRS4596 is a potent and selective P2X4 receptor antagonist with an IC50 value of 1.38 μM for human P2X4 receptor. MRS4596 has neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4596 can be used in research of ischemic stroke .
    MRS4596
  • HY-130605
    BAY-1797
    2 Publications Verification

    P2X Receptor Neurological Disease
    BAY-1797 is a potent, orally active, and selective P2X4 antagonist, with an IC50 of 211 nM against human P2X4. BAY-1797 displays no or very weak activity on the other P2X ion channels. BAY-1797 shows anti-nociceptive and anti-inflammatory effects .
    BAY-1797
  • HY-108676

    P2X Receptor Neurological Disease
    NF023 hexasodium is a selective and competitive P2X1 receptor antagonist, with IC50 values of 0.21 μM, 28.9 μM, > 50 μM and > 100 μM for human P2X1, P2X3, P2X2, and P2X4-mediated responses respectively [4].
    NF023 hexasodium
  • HY-151547

    P2X Receptor Neurological Disease
    MRS4719 is a potent P2X4 receptor antagonist with an IC50 value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca 2+]i influx in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke .
    MRS4719
  • HY-144285

    CXCR HIV Inflammation/Immunology
    CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM) .
    CXCR4 antagonist 4
  • HY-P99572

    BNT-312; DuoBody-CD40x-4-1BB; GEN1042

    TNF Receptor Inflammation/Immunology Cancer
    Tecaginlimab (BNT-312) is a Fc-inert bispecific antibody for dual targeting and conditional stimulation of CD40 and 4-1BB. Tecaginlimab can enhance priming and reactivation of tumor-specific immunity .
    Tecaginlimab
  • 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-113700

    Antibiotic Cancer
    PD 116779 is an Antibiotic with anticancer activity. PD 116779 demonstrates moderate cytotoxicity against L1210 lymphocytic leukemia and HCT-8 human colon adenocarcinoma cell lines with IC50 values of 3.55x10 -7 and 4.08x10 -7 M, respectively .
    PD 116779
  • HY-150270

    P2X Receptor Neurological Disease Inflammation/Immunology
    NP-1815-PX is a potent and selective P2X4R antagonist. NP-1815-PX has anti-inflammatory activity, and can relieve pain in chronic pain models. NP-1815-PX also inhibits guinea pig tracheal/bronchial smooth muscle (TSM and BSM) contractions .
    NP-1815-PX
  • HY-150270A

    P2X Receptor Neurological Disease Inflammation/Immunology
    NP-1815-PX sodium is a potent and selective P2X4R antagonist. NP-1815-PX sodium has anti-inflammatory activity, and can relieve pain in chronic pain models. NP-1815-PX sodium also inhibits guinea pig tracheal/bronchial smooth muscle (TSM and BSM) contractions .
    NP-1815-PX sodium
  • HY-D0976

    P2X Receptor HIV Infection
    NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env .
    NF279
  • HY-101308

    P2Y Receptor Cardiovascular Disease
    MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors . MRS2179 tetrasodium inhibits platelet aggregation .
    MRS2179 tetrasodium
  • HY-101308A
    MRS2179 tetrasodium hydrate
    1 Publications Verification

    P2Y Receptor Cardiovascular Disease
    MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium hydrate is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors . MRS2179 tetrasodium hydrate inhibits platelet aggregation .
    MRS2179 tetrasodium hydrate
  • HY-136254
    BzATP triethylammonium salt
    4 Publications Verification

    P2X Receptor Inflammation/Immunology Cancer
    BzATP triethylammonium salt acts as a P2X receptor agonist with pEC50s of 8.74, 5.26, 7.10, 7.50, 6.19, 6.31, 5.33 for P2X1, P2X2, P2X3, P2X2/3, P2X4 and P2X7, respectively . BzATP triethylammonium salt is potent at P2X7 receptors with EC50s of 3.6 μM and 285 μM for rat P2X7 and mouse P2X7, respectively .
    BzATP triethylammonium salt
  • HY-18745

    Benzoylbenzoyl-ATP triethylammonium

    P2X Receptor Inflammation/Immunology Cancer
    BzATP triethylammonium acts as a P2X receptor agonist with pEC50s of 8.74, 5.26, 7.10, 7.50, 6.19, 6.31, 5.33 for P2X1, P2X2, P2X3, P2X2/3, P2X4 and P2X7, respectively . BzATP triethylammonium is potent at P2X7 receptors with EC50s of 3.6 μM and 285 μM for rat P2X7 and mouse P2X7, respectively .
    BzATP triethylammonium
  • HY-15310
    Ivermectin
    Maximum Cited Publications
    25 Publications Verification

    MK-933; CD-5024; K-237

    Flavivirus Dengue virus Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Bacterial Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import [4]. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
    Ivermectin
  • HY-15310R

    Dengue virus Flavivirus Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Bacterial Infection Cancer
    Ivermectin (Standard) is the analytical standard of Ivermectin. This product is intended for research and analytical applications. Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import [4]. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
    Ivermectin (Standard)
  • HY-134807

    P2X Receptor 5-HT Receptor Autophagy Cancer
    Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7 .
    Indophagolin

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