Tegoprubart (powder)
Tegoprubart (powder) (AT-1501 (powder)) is a CD40 ligand inhibitor (EC50=100 ng/mL) and immunosuppressant that selectively inhibits the CD40 ligand, a co-stimulatory molecule involved in T cell activation. Tegoprubart (powder) suppresses immune rejection, prevents rejection in animal transplantation models, and reduces cell-mediated and antibody-mediated immune responses to create a more immunotolerant environment. Tegoprubart (powder) preserves renal function when combined with Mycophenolate (HY-B0421) and Corticosteroids, and maintains graft function in preclinical studies. Tegoprubart (powder) is applicable to research related to kidney transplantation and kidney transplant rejection.
For research use only. We do not sell to patients.
- CAS No.: 2628092-47-5
- Molecular Weight:145.56 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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CD40L |
In Vitro
The immune complex formed by Tegoprubart (600 nM; in vitro platelet activation assay) (powder) and soluble CD40L fails to induce PAC-1 expression on the surface of platelets from healthy individuals, does not trigger platelet aggregation, and exerts no platelet-activating effect; in contrast, the immune complex formed by Hu5C8 (HY-P99315) and soluble CD40L significantly induces platelet aggregation[1].
Tegoprubart (2 μg/mL; 1 h; CD40L binding assay) (powder) exhibits binding affinity to recombinant human CD40L comparable to that of Hu5C8, with both antibodies having an EC50 value of 100 ng/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:No specific cell line (in vitro protein binding system with recombinant human CD40L)
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Concentration:2 μg/mL
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Incubation Time:Overnight coating at 4°C, 1 hour of incubation
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Result:Exhibited a binding affinity to recombinant human CD40L that was comparable to that of Hu5C8, with an EC50 value of 100 ng/mL for both antibodies.
Abatacept (HY-108829) was used as a negative control and showed no binding to CD40L.
In Vivo
In the cynomolgus monkey intrahepatic islet allotransplantation model, Tegoprubart (25 mg/kg; intravenous injection; once on days -2, -1, 0, 1, 3, 7, 10, 18, 23, and 28 post-operation, then once every 14 days thereafter; for 182 days) (powder), when combined with thymoglobulin (5 mg/kg, intravenous injection on days -2, -1, 0, 1, and 2 post-operation), rapamycin, and anti-TNF-α, maintains islet graft function, enables insulin independence in some animals, and causes no severe cytomegalovirus (CMV) reactivation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cynomolgus Monkey Intrahepatic Islet Allotransplantation Model (MHC-disparate intrahepatic islet allotransplantation model, induced with 100 mg/kg IV streptozotocin to establish diabetes)[1]
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Dosage:25 mg/kg,
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Administration:Intravenous injection; administered on POD#−1, 0, 3, 10, 18, 23, 28, then biweekly for 182 days
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Result:One recipient remained insulin-free until POD#182 with improved %A1C and fasting C-peptide > 1.0 ng/mL, accompanied by increased CD4+ regulatory T cell (Treg) frequencies; the other recipient rejected the first graft within 2 weeks but achieved partial graft function after a second transplant on POD#98, maintaining C-peptide > 1.0 ng/mL until POD#182; no thromboembolic events were observed throughout the study.
Chemical Information
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CAS No. 2628092-47-5
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Molecular Weight 145.56 kDa
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SMILES
[Tegoprubart (powder)]
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Synonyms
AT-1501 (powder)
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Research Protocol for Cancer Immunology
Cancer immunology studies how the immune system recognizes, suppresses, edits, or fails to eliminate malignant cells through tumor antigen release, antigen presentation, T-cell priming, immune trafficking, tumor-cell killing, and feedback inhibition in the tumor microenvironment. The cancer-immunity cycle links tumor antigenicity, dendritic-cell priming, CD8+ T-cell infiltration, cytotoxic function, and immune-checkpoint regulation to tumor rejection or immune escape. Immune-checkpoint pathways such as PD-1/PD-L1 and CTLA-4 suppress antitumor T-cell activity and can be therapeutically blocked, but many tumors remain resistant because of poor antigen presentation, weak T-cell infiltration, suppressive myeloid cells, regulatory T cells, and tumor-intrinsic immune-exclusion programs. Unresolved questions include which immune-cell states predict response, how tumor-intrinsic pathways exclude immune cells, how myeloid suppression limits checkpoint blockade, and which combination strategies
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tegoprubart (powder) Related Classifications
HY-P990083A Related Classifications
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