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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2628092-47-5
- Molecular Weight:145.56 kDa
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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CD40L |
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.
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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 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. Nr. 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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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Tegoprubart (powder) Related Classifications
HY-P990083A Related Classifications
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