Povetacicept
Based on 1 Customer Validation
Povetacicept (ALPN-303) is an engineered Fc fusion protein containing the TACI domain, and acts as a dual APRIL/BAFF antagonist. The Kd value of Povetacicept for human BAFF is 59.3 pM, while its Kd value for human APRIL is 1.00 pM. Povetacicept reduces the activation, proliferation, differentiation and survival of B cells, and inhibits the production of immunoglobulins and autoantibodies. Povetacicept can be used in research related to autoimmune hemolytic anemia, immune thrombocytopenia, systemic lupus erythematosus, lupus nephritis and myasthenia gravis.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.9%
- CAS. Nr.: 2490217-42-8
- Molecular Weight:62.61 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
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Help & FAQs
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Biologische Aktivität
Human
TNFSF13B
Povetacicept (0.137-33.3 nM; 240-1800 s) binds to recombinant human APRIL with a Kd value of 1.00 pM, and also binds to recombinant human BAFF with a Kd value of 59.3 pM, exhibiting high-affinity dual binding activity toward these two cytokines[2].
Povetacicept (2.5 pM-200 nM; 5 h) potently inhibits the signaling pathways of APRIL, BAFF, BAFF 60-mer and BAFF/APRIL heterotrimer in TACI/Jurkat/NF-κB reporter cells[2].
Povetacicept (7 d) potently inhibits the proliferation of primary human B cells, the differentiation of class-switched memory B cells into plasma cells, and the secretion of immunoglobulins[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | AUC |
|---|---|---|---|---|
| Cynomolgus Monkey[2] | 9 mg/kg | i.v. | 27 μg/mL | 1167 μg·h/mL |
Povetacicept (15 mg/kg; i.p.; 2 doses (days 4 and 11)) potently reduces splenic immune cell subsets and inhibits T cell-dependent antibody formation more effectively than WT TACI-Fc comparators in KLH-immunized mice[2].
Povetacicept (10 mg/kg; i.p.; 2 doses (days 1 and 6)) exhibits superior immunosuppressive activity over single-target inhibitors, combination therapy, telitacicept, and anti-CD20 in SRBC-immunized mice, leading to greater suppression of T cell-dependent antibody responses[2].
Povetacicept (17 mg/kg; i.p.; twice weekly; 20 weeks) significantly suppresses lupus disease activity, improves survival, and reduces renal and glandular pathology in the spontaneous NZB/NZW F1 lupus mouse model[2].
Povetacicept (10 mg/kg; i.p.; twice weekly; day 5 to day 88) significantly suppresses renal immune deposition and reduces pathogenic splenic immune cell subsets in the inducible bm12 lupus mouse model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HOD+OTII+ transgenic mice (1.5 to 3.5 months old; AIHA model via intraperitoneal anti-CTLA-4/IL-10R/LAG-3/PD-1 antibodies for 2.5 weeks)[1]
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Dosage:10 mg/kg
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Administration:i.p.; twice weekly; 3.5 weeks
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Result:Significantly reduced numbers of antibody-secreting cells (ASCs) in bone marrow.
Suppressed autoantibody generation.
Increased hematocrit compared to controls.
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Animal Model:C57BL/6NJ (male, 10-week-old, KLH-immunized antibody-mediated immune response model)[2]
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Dosage:15 mg/kg
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Administration:i.p.; 2 doses (days 4 and 11)
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Result:Significantly reduced total spleen cellularity compared to Fc control, WT TACI 30-110-Fc, or WT TACI 13-118-Fc.
Significantly reduced splenic transitional type 2, follicular, marginal zone, germinal center, and plasma cell subsets (excluding transitional type 1 B cells) beyond the activity of WT TACI-Fc.
Mediated the greatest reduction in total number of CD4+ follicular helper T cells per spleen compared to other treatment groups.
Significantly reduced serum anti-KLH IgM and IgG1 antibody titers, with reductions greater than those observed with WT TACI-Fc treatment.
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Animal Model:C57BL/6NJ (female, 8-9-week-old, inducible bm12 lupus model); bm12 (female, 8-11-week-old, splenocyte donor)[2]
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Dosage:10 mg/kg
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Administration:i.p.; twice weekly; day 5 to day 88
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Result:Significantly reduced renal IgG deposit scores compared to Fc control.
Significantly lower total number of splenic plasma cells, germinal center B cells, and follicular helper T cells compared to Fc control.
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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FPIA_[PROTEIN_1REPEAT]2-FC
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Immobilized APRIL/TNFSF13 Trimer Protein, Human (HEK293, His-Flag, HY-P70733A) can bind Povetacicept. The EC50 for this effect is 2.624 ng/mL.
Chemical Information
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CAS. Nr. 2490217-42-8
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Appearance Liquid
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Molecular Weight 62.61 kDa
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Color Colorless to light yellow
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Synonyms
ALPN-303
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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 (263 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
[2]. Evans LS, et al. Povetacicept, an Enhanced Dual APRIL/BAFF Antagonist That Modulates B Lymphocytes and Pathogenic Autoantibodies for the Treatment of Lupus and Other B Cell-Related Autoimmune Diseases. Arthritis Rheumatol. 2023;75(7):1187-1202. [Content Brief]
[3]. Rinaldi E, et al. Povetacicept (ALPN-303; TACI vTD-Fc), an enhanced, potent dual inhibitor of BAFF and APRIL, ameliorates experimental autoimmune myasthenia gravis in C57BL/6N mice. Front Immunol. 2025;16:1533093. Published 2025 Jun 6. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Povetacicept Related Classifications
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