Abatacept (Synonyms: CTLA4lg; BMS-188667) |
| カタログ番号GC38130 |
アバタセプト（CTLA4lg）は、人間のCTLA4の細胞外ドメインと、ヒトIgG1のFc部分（ヒンジおよびCH2および3ドメインのフラグメント）から構成される可溶性融合タンパク質です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 332348-12-6
Sample solution is provided at 25 µL, 10mM.
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Abatacept (CTLA4Ig) is a soluble fusion protein composed of the extracellular domain of human cytotoxic T lymphocyte-associated protein 4 (CTLA4) and a fragment of the human IgG1 Fc portion (hinge, CH2 and 3 domains)[1]. Abatacept is a selective T cell co-stimulatory modulator and a protein drug used to treat autoimmune diseases[2]. CTLA4 is structurally similar to CD28, but binds to CD80 and CD86 with higher affinity, thereby inhibiting T cell activation[3]. Abatacept can be used to treat moderate to severe rheumatoid arthritis (RA), and is also used to treat psoriatic arthritis and juvenile idiopathic arthritis[4].
In vitro, Abatacept (0.5, 5, 50μM) treatment of human Burkitt lymphoma B (BJAB) wild-type, CD80 KO, and CD86 KO cells for 2h reduced the expression of CD86 and CD80 on the cell surface[5].
In vivo, subcutaneous administration of Abatacept (10mg/kg, once every 2 days) to DO11.10 RAG-2–/– mice inhibited T cell activation in the draining lymph nodes of mice, but did not induce T cell anergy or the generation of Treg cells[6]. Subcutaneous administration of Abatacept (20mg/kg) to rats with collagen-induced arthritis (CIA) significantly reduced paw edema[7].
References:
[1] Douthwaite J, Moisan J, Privezentzev C, et al. A CD80-biased CTLA4-Ig fusion protein with superior in vivo efficacy by simultaneous engineering of affinity, selectivity, stability, and FcRn binding[J]. The Journal of Immunology, 2017, 198(1): 528-537.
[2] Chitale S, Moots R. Abatacept: the first T lymphocyte co-stimulation modulator, for the treatment of rheumatoid arthritis[J]. Expert opinion on biological therapy, 2008, 8(1): 115-122.
[3] da Rosa L C, Scales H E, Benson R A, et al. The effect of abatacept on T-cell activation is not long-lived in vivo[J]. Discovery Immunology, 2024, 3(1): kyad029.
[4] Brunner H I, Wong R, Nys M, et al. Abatacept: a review of the treatment of polyarticular-course juvenile idiopathic arthritis[J]. Pediatric Drugs, 2020, 22: 653-672.
[5] Lorenzetti R, Janowska I, Smulski C R, et al. Abatacept modulates CD80 and CD86 expression and memory formation in human B-cells[J]. Journal of Autoimmunity, 2019, 101: 145-152.
[6] Patakas A, Ji R R, Weir W, et al. Abatacept inhibition of T cell priming in mice by induction of a unique transcriptional profile that reduces their ability to activate antigen‐presenting cells[J]. Arthritis & rheumatology, 2016, 68(3): 627-638.
[7] Lon H K, Liu D, DuBois D C, et al. Modeling pharmacokinetics/pharmacodynamics of abatacept and disease progression in collagen-induced arthritic rats: a population approach[J]. Journal of pharmacokinetics and pharmacodynamics, 2013, 40: 701-712.
| Cell experiment [1]: | |
Cell lines | Human Burkitt lymphoma B (BJAB) wild type (WT)、CD80 KO、CD86 KO cells |
Preparation Method | BJAB wild type (WT), CD80 KO and CD86 KO cells were treated with Abatacept (10μg/mL) for 2h and CD86 and CD80 expression as sessed by flow cytometry prior removal of bound abatacept by acidic elution. |
Reaction Conditions | 10μg/mL; 2h |
Applications | Reduction in surface expression of CD86 and CD80 on human B-cells in the presence of Abatacept. |
| Animal experiment [2]: | |
Animal models | DO11.10 RAG-2–/– mice |
Preparation Method | To prime CD41 T cells, DO11.10 RAG-2–/– mice were injected subcutaneously in the scruff of the neck with 100 mg of OVA in Freund’s complete adjuvant. Mice were treated with 10mg/kg of Abatacept or control IgG beginning 2 days before priming and continuing every 2 days thereafter. |
Dosage form | 10mg/kg; s.c. |
Applications | Abatacept reduced the proportion of activated T cells (CD44highCD62L–) and inhibited the upregulation of ICOS and CD71. Cells primed in the presence of Abatacept produced substan tial amounts of IL-2, similar to the naive T cells, where as cells from orally tolerized mice produced very low levels of the cytokine, confirming their anergic state. |
References: | |
| Cas No. | 332348-12-6 | SDF | |
| 同義語 | CTLA4lg; BMS-188667 | ||
| Canonical SMILES | [Abatacept] | ||
| Formula | M.Wt | ||
| 溶解度 | Soluble in water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
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