Tegoprubart
Based on 1 Customer Validation
Tegoprubart (AT-1501) 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 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 preserves renal function when combined with Mycophenolate (HY-B0421) and Corticosteroids, and maintains graft function in preclinical studies. Tegoprubart is applicable to research related to kidney transplantation and kidney transplant rejection.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.86%
- 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.
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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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
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Help & FAQs
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Biologische Aktivität
Human IgG1 kappa
Human
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CD40L |
The immune complex formed by Tegoprubart (600 nM; in vitro platelet activation assay) 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) 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), 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.
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Human IgG1 kappa
ELISA, FACS, Functional assay
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Immobilized CD40L/CD154/TRAP Protein, Human (His, HY-P72907) can bind Tegoprubart. The EC50 for this effect is 4.211 ng/mL. -
Flow cytometric analysis of 1X106 500 ng/mL anti-CD3 stimulated Jurkat cells(24h) with Tegoprubart (HY-P990083, red). Cells were fixed with 4% paraformaldehyde. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. Alexa Fluor 488-conjugated AffiniPure Goat Anti-Human IgG H&L (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG1 kappa Isotype Control (HY-P99001, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black). -
Loaded Tegoprubart on ProA biosensor, can bind CD40L/CD154/TRAP Protein, Human (HY-P7144) with an affinity constant of 4.923E-10 M as determined in BLI assay.
Chemical Information
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CAS. Nr. 2628092-47-5
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Appearance Liquid
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Molecular Weight 145.56 kDa
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Color Colorless to light yellow
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SMILES
[Tegoprubart]
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Synonyms
AT-1501
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Versand
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
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Data Sheet (262 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Tegoprubart Related Classifications
HY-P990083 Related Classifications
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