Belatacept
Based on 1 Customer Validation
Belatacept (BMS 224818) is a selective T-cell costimulation blocker and a costimulator of the CD28-CD80/86 pathway. Belatacept binds to the CD 80/86 ligand and inhibits CD-28-mediated T cell costimulation and IFN-γ production. Belatacept can be used in studies of immunosuppression in organ transplantation. The component ratio of this product is Active ingredient : Excipients = 1:2.4.
For research use only. We do not sell to patients.
- Purity: 99.45%
- CAS No.: 706808-37-9
- Molecular Weight:90 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Fusion-CTLA4-IGHG1 Fc
Human
CD80/86[1]
Belatacept (0-5 mg/mL, 1 h) inhibits T-cell proliferation in a dose-dependent manner[2].
Belatacept (500 ng/mL, 7 days) enhances predominance of effector-memory T-cells after allogeneic stimulation[2].
Belatacept (100, 500 ng/mL, 7 days) has no effect on differentiation and allogeneic IFNγ production of isolated effector-memory T cells[2].
Belatacept (10 μg/mL, 1 h) does not inhibit follicular T Cell-dependent B-Cell differentiation[4].
Belatacept (40 μg/mL, 10 days) reduces plasmablast differentiation, Ig production, and the major transcription factor Blimp-1 in a T cell-independent manner[5].
Belatacept (40 μg/mL, 30 min) induces activation of the STAT3 transcription factor in stimulated B cells and reduced the expression of CD86[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PBMCs from healthy volunteers
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Concentration:0-5 mg/mL
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Incubation Time:1 h
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Result:Inhibited T-cell proliferation l with IC50 values of 215 ng/mL, and residual T-cell proliferation (±30%) was still present at high doses.
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Cell Line:CD40L and IL-21 stimulated B cells
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Concentration:40 μg/mL
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Incubation Time:15, 30 min
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Result:Increased in STAT signaling determined by increased STAT3 phosphorylation.
Belatacept (intravenous injection, 20 mg/kg) displays immunosuppressive activities in monkeys immunized with sheep red blood cell[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute rejection model of orthotopic kidney transplantation in rats[3]
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Dosage:60 mg/kg
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Administration:Intraperitoneal injection, at postoperative and 4 days after transplantation.
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Result:Inhibited creatinine increase after kidney transplantation (combined with BTLA overexpression therapy).
Reduced C4d in graft IF staining, and reduced CD138 infiltration and DSA production.
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Animal Model:Rhesus monkeys immunized with sheep red blood cell[6]
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Dosage:Intra-operatively 10 mg/kg, on day 4 (15 mg/kg) and on post-operative days 14, 28, 42, 56, 70 (20 mg/kg).
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Administration:intravenous injection
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Result:Caused a 50% reduction in the peak anti-SRBC response.
Prolonged renal allograft survival and synergies with conventional immunosuppression.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Fusion - [CTLA4 (cytotoxic T-lymphocyte-associated protein 4, CD152)]2 - IGHG1 Fc (Fragment constant)
Chemical Information
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CAS No. 706808-37-9
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Appearance Solid
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Molecular Weight 90 kDa
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Color White to off-white
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SMILES
[Belatacept]
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Synonyms
BMS 224818; LEA 29Y
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (264 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)
References
[1]. George Melvin, et al. Belatacept: A worthy alternative to cyclosporine?. J Pharmacol Pharmacother. 2012 Jan-Mar; 3(1): 90–92. [Content Brief]
[2]. Gretchen N de Graav, et al. Down-Regulation of Surface CD28 under Belatacept Treatment: An Escape Mechanism for Antigen-Reactive T-Cells. PLoS One. 2016 Feb 26;11(2):e0148604. [Content Brief]
[3]. Hengcheng Zhang, et al. Combined Immunotherapy With Belatacept and BTLA Overexpression Attenuates Acute Rejection Following Kidney Transplantation. Front Immunol. 2021 Feb 24;12:618737. [Content Brief]
[4]. Gretchen N de Graav, et al. Belatacept Does Not Inhibit Follicular T Cell-Dependent B-Cell Differentiation in Kidney Transplantation. Front Immunol. 2017 May 31;8:641. [Content Brief]
[5]. laire Leibler, et al. Control of Humoral Response in Renal Transplantation by Belatacept Depends on a Direct Effect on B Cells and Impaired T Follicular Helper-B Cell Crosstalk. J Am Soc Nephrol. 2018 Mar;29(3):1049-1062. [Content Brief]
[6]. Christian P Larsen, et al. Rational development of LEA29Y (belatacept), a high-affinity variant of CTLA4-Ig with potent immunosuppressive properties. Am J Transplant. 2005 Mar;5(3):443-53. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)