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Purity: ≥98%
CTLA-4 inhibitor (B7/CD28 interaction inhibitor 1) is a novel and potent inhibitor of CTLA4 or CTLA-4 (cytotoxic T-lymphocyte-associated protein 4). CTLA4 is also known as CD152 (cluster of differentiation 152) and is a protein receptor that, functioning as an immune checkpoint, downregulates immune responses. CTLA4 is constitutively expressed in Tregs but only upregulated in conventional T cells after activation. It acts as an 'off' switch when bound to CD80 or CD86 on the surface of antigen-presenting cells. Polymorphisms of the CTLA-4 gene are associated with autoimmune diseases such as autoimmune thyroid disease and multiple sclerosis, though this association is often weak. In Systemic Lupus Erythematosus (SLE), the splice variant sCTLA-4 is found to be aberrantly produced and found in the serum of patients with active SLE.
| ln Vitro |
To create an exceptionally stable signaling complex, the divalent B7.1 homodimer is bridged by the divalent CTLA4 homodimer. Immunosuppression and improved allograft survival are the outcomes of blocking B7/CD28 interaction with soluble receptors or monoclonal antibodies, while B7/CTLA-4 blockage strengthens anticancer immune responses. An essential part of naive T cell activation involves the interaction between B7 molecules on antigen-presenting cells and costimulatory molecules on T cells. Drugs that interfere with these interactions might therefore be helpful in the management of autoimmune disorders and transplant rejection [1].
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| References |
[1]. Green NJ, et al. Structure-activity studies of a series of dipyrazolo[3,4-b:3',4'-d]pyridin-3-ones binding to the immune regulatory protein B7.1. Bioorg Med Chem. 2003 Jul 3;11(13):2991-3013.
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| Molecular Formula |
C21H13F4N5O
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| Molecular Weight |
427.36
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| CAS # |
635324-72-0
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| SMILES |
O=C1N(C2=CC=C(F)C=C2)NC3=C4C=NN(C)C4=NC(C5=CC=CC(C(F)(F)F)=C5)=C13
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.87 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3399 mL | 11.6997 mL | 23.3995 mL | |
| 5 mM | 0.4680 mL | 2.3399 mL | 4.6799 mL | |
| 10 mM | 0.2340 mL | 1.1700 mL | 2.3399 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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