NTPDase Inhibitor

ARL67156 (FPL 67156) trisodium is a selective small molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 trisodium is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with K_is of 11, 18 and 12?μM, respectively. ARL67156 trisodium can be used in the research of calcific aortic valve disease, asthma.

Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively.

Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively.

ARL67156 (FPL 67156) trisodium hydrate is a selective small is a selective samll molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 trisodium hydrate is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with K_is of 11, 18 and 12 μM, respectively. ARL67156 trisodium hydrate can be used in the research of disease like calcific aortic valve disease, asthma.

Afivastobart (AB598) is a human ENTPD1 (CD39)-targeting monoclonal antibody with antineoplastic activity.Afivastobart binds as a monoclonal antibody to modulate Homo sapiens ENTPD1 activity.Afivastobart constitutes a glycoform alfa immunoglobulin G1-kappa monoclonal antibody.

PSB-24379 is a CD39 inhibitor that potently inhibits human membrane-bound CD39 (K_i = 77.4 nM) and truncated soluble human CD39 (K_i = 23.1 nM). PSB-24379 reduces the level of ATP hydrolysis in melanoma and breast cancer cell membranes. PSB-24379 partially reverses ATP-mediated suppression of T cell activation and proliferation in a high-ATP environment. PSB-24379 can be used in research related to melanoma and breast cancer.

PUR001 is a monoclonal antibody targeting NTPDase 1 (CD39). PUR001 blocks the hydrolysis of extracellular ATP and ADP into AMP by inhibiting CD39, reduces the production of immunosuppressive adenosine, and increases extracellular ATP concentration to activate anti-tumor immune responses. PUR001 can be used in studies related to solid tumors.

NF279 is a selective P2X1 receptor antagonist and NTPDase inhibitor, with a P2X1 IC₅₀ value of 19 nM. NF279 suppresses GABA-evoked currents, reduces ATP-excited respiratory activity, alters hypoglossal nerve burst parameters, and blocks CXCR4, CCR5, CXCR3, and CXCR7-mediated calcium responses. NF279 arrests HIV-1 fusion downstream of CD4 binding, inhibits R5- and X4-tropic HIV-1 strains. NF279 can be used for the research of HIV-1 infection.

ARL67156 (FPL 67156) triethylamine is a selective small is a selective samll molecular inhibitor, targeting to ecto-ATPase, CD39, and CD73. ARL67156 triethylamine is also a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with K_is of 11, 18 and 12 μM, respectively. ARL67156 triethylamine can be used in the research of disease like calcific aortic valve disease, asthma.

Perenostobart (SRF617) is a human IgG4 antibody with inhibitory activity against CD39 ATPase. Perenostobart inhibits CD39-mediated hydrolysis of extracellular ATP to AMP, with IC₅₀ values of 1.9 nM (HEK293 OE cells), 0.7 nM (MOLP-8 cells), and 1.2 nM (RBC-lysed whole blood). Perenostobart enhances CD4⁺ T-cell proliferation, promotes dendritic cell maturation, and boosts inflammasome activation in macrophages in the presence of ATP. Perenostobart demonstrates significant single-agent anti-tumor efficacy in MOLP-8 and H520 xenograft models. Perenostobart can be used for the study of cancer.

PSB-16131 is a potent inhibitor of human NTPDase2, showing non-competitive inhibition with an IC₅₀ of 539 nM. PSB-16131 can be used in the study of inflammation, neurodegenerative diseases and cancer.

PSB-06126 is a selective nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitor, with the K_i values of 0.33 μM for rat NTPDase 1, 19.1 μM for NTPDase 2 and 2.22 μM for NTPDase 3, respectively. PSB-06126 acts on human NTPDase 3 with an IC₅₀ value of 7.76 μM and a K_i value of 4.39 μM.

IPH5201 is a selective CD39 inhibitor and a humanized IgG1 monoclonal antibody. IPH5201 selectively binds to and inhibits the enzymatic activity of both membrane-bound and soluble CD39, blocking ATP hydrolysis. IPH5201 enhances the phenotypic maturation and activation of dendritic cells and macrophages. IPH5201 potentiates the anti-tumor effect of Oxaliplatin (HY-17371). IPH5201 shows preliminary evidence of disease stabilization in advanced solid tumor models when used as a single agent or in combination with Durvalumab (HY-P9919). IPH5201 can be used for the research of advanced solid tumors.

Ticlopidine (Standard) is the analytical standard of Ticlopidine. This product is intended for research and analytical applications. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively.

PSB069 bearing a p-chlorophenylamino residue is a potent, well-tolerated and nonselective NTPDases1, 2, 3 inhibitor(K_i=16~18 μM).

8-BuS-AMP is a NTPDase1 inhibitor and a CD73/CD39 inhibitor, with an IC₅₀ of 35 μM and a K_i value of 0.292 μM against human NTPDase1; its K_i values against human CD73 and CD39 are 1.19 μM and 0.847 μM, respectively. 8-BuS-AMP binds to the substrate-binding pockets of NTPDase1 and CD73 to effectively block the conversion of ATP and AMP to adenosine, thereby enhancing the activation and proliferation of human peripheral T lymphocytes. 8-BuS-AMP possesses excellent enzymatic hydrolysis resistance and metabolic stability, resists hydrolysis by multiple NTPDase subtypes, and shows no activity against P2Y1 and P2Y12 receptors. 8-BuS-AMP can be used in purinergic signaling pathway and cancer-related studies.

Ticlopidine-d₄ is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively.

NTPDase2-IN-1 is a non-competitive, selective NTPDase2 inhibitor, with an IC₅₀ of 0.04 μM against h-NTPDase2 and an IC₅₀ of 2.27 μM against h-NTPDase8. NTPDase2-IN-1 is applicable for cancer-related research.

h-NTPDase-IN-5 (compound 3b) is a pan-inhibitor of NTPDase with IC50s of 1.10 μM (h-NTPDase1), 44.73 μM (h-NTPDase2), 26.14 μM (h-NTPDase3), 0.32 μM (h- NTPDase8).

Mebarase alfa is a human monoclonal antibody targeting ENTPD1/CD39 for the study of sepsis-associated renal injury.