Physicochemical Properties
| Molecular Formula | 0 |
| Molecular Weight | 0 |
| CAS # | 706808-37-9 |
| Appearance | White to off-white solid powder |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| ln Vitro | In a dose-dependent manner, belatacept (0–5 mg/mL, 1 hour) inhibits T cell proliferation [2]. After allogeneic stimulation, belatacept (500 ng/mL, 7 days) increases effector memory T cell dominance [2]. Isolated effector memory T cell differentiation and allogeneic IFNγ production were unaffected by belatacept (100, 500 ng/mL, 7 days) [2]. The differentiation of B cells dependent on follicular T cells is not inhibited by belatacept (10 μg/mL, 1 hour) [4]. T cell-independent reductions in plasmablast differentiation, Ig production, and the major transcription factor Blimp-1 are observed with belatacept (40 μg/mL, 10 days) [5]. When administered at a dose of 40 μg/mL for 30 minutes, belatacept decreases the expression of CD86 and activates the STAT3 transcription factor in stimulated B cells [5]. |
| ln Vivo | Belatacept (ip, 60 mg/kg) suppresses antibody-mediated rejection (ABMR) and, when paired with BTLA (B and T lymphocyte attenuator) overexpression treatment, can suppress acute rejection [3]. In monkeys given sheep red blood cells as an immunization, belatacept (20 mg/kg administered intravenously) exhibited immunosuppressive effects [6]. |
| Cell Assay |
Cell viability assay [2] Cell Types: PBMC from healthy volunteers Tested Concentrations: 0-5 mg/mL Incubation Duration: 1 hour Experimental Results: Inhibited T cell proliferation with an IC50 value of 215 ng/mL, and residual T cell proliferation (± 30%) persisted at high doses. Western Blot Analysis [5] Cell Types: CD40L and IL-21 stimulated B cells Tested Concentrations: 40 μg/mL Incubation Duration: 15, 30 min Experimental Results: Increased STAT signaling as determined by increased STAT3 phosphorylation. |
| Animal Protocol |
Animal/Disease Models: Rat orthotopic renal transplantation acute rejection model [3] Doses: 60 mg/kg Route of Administration: intraperitoneal (ip) injection, after transplantation and 4 days after transplantation. Experimental Results: Inhibition of creatinine increase after renal transplantation (combined with BTLA overexpression treatment). There was diminished C4d in graft IF staining, CD138 infiltration, and DSA production. Animal/Disease Models: immunize rhesus monkeys with sheep red blood cells [6] Doses: 10 mg/kg intraoperatively, day 4 (15 mg/kg) and postoperative days 14, 28, 42, 56, and 70 (20 mg/kg ). Route of Administration: intravenous (iv) (iv)injection Experimental Results: resulted in a 50% reduction in the peak anti-SRBC response. Prolonged renal allograft survival and synergy with conventional immunosuppression. |
| References |
[1]. Belatacept: A worthy alternative to cyclosporine?. J Pharmacol Pharmacother. 2012 Jan-Mar; 3(1): 90–92. [2]. Down-Regulation of Surface CD28 under Belatacept Treatment: An Escape Mechanism for Antigen-Reactive T-Cells. PLoS One. 2016 Feb 26;11(2):e0148604. [3]. Combined Immunotherapy With Belatacept and BTLA Overexpression Attenuates Acute Rejection Following Kidney Transplantation. Front Immunol. 2021 Feb 24;12:618737. [4]. Belatacept Does Not Inhibit Follicular T Cell-Dependent B-Cell Differentiation in Kidney Transplantation. Front Immunol. 2017 May 31;8:641. [5]. 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. [6]. 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. |
Solubility Data
| Solubility (In Vitro) | H2O : ~50 mg/mL |
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |