Apilimod mesylate (Synonyms: STA 5326 mesylate) |
カタログ番号GC35374
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アピリモド (STA 5326) メシレートは強力な IL-12/IL-23 阻害剤であり、IFN-γ/SAC 刺激ヒト PBMC および SAC 処理サル PBMC において、1 nM および 2 nM の IC50 で IL-12 を強力に阻害します。それぞれ。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 870087-36-8
Sample solution is provided at 25 µL, 10mM.
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Apilimod(STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, IL-12 production in cultures of IFN-γ/LPS-stimulated human PBMCs is strongly inhibited by STA-5326 with an IC50 of 10 nM. IC50 value: 10 nM (IFN-γ/LPS-stimulated human PBMCs) [1]IL-12/IL-23
in vitro: STA-5326 not only inhibited IL-12, but it also potently inhibited IL-23 and total p40 products in various forms as monomer, homodimer, and heterodimerin IFN-γ/SAC-stimulated human PBMCs [1]. STA-5326 inhibited IFN-γ production induced by either IFN-γ/SAC or SAC in human PBMCs, with an IC50 of approximately 20 nM, while the compound had no significant effect on the production when T cells were stimulated using anti-CD3 and anti-CD28 antibodies, suggesting that the T-cell-receptor-dependent production of IFN-γ that occurs independently of suppression of Th1 cells via inhibition of IL-12 is not directly inhibited by the compound [1].
Patients with CD responded within 14 days of treatment with apilimod and, after 28 days, the drug significantly reduced the Crohn's disease activity index (CDAI). Apilimod is currently in phase II clinical trials for rheumatoid arthritis, common variable immunodeficiency and CD. From the data available to date, apilimod appears to be a promising treatment for CD, and the oral formulation of this compound provides an advantage for apilimod over injectable therapies [2]. Oral administration of either 5 mg/kg or 20 mg/kg STA-5326 reduced the severity of EAU on day 14 and 18. In addition, mice treated with 20 mg/kg STA-5326 showed significantly decreased severity of EAU by histopathological analysis [3].
[1]. Wada Y, et al. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood. 2007 Feb 1;109(3):1156-64. [2]. Billich A. Drug evaluation: apilimod, an oral IL-12/IL-23 inhibitor for the treatment of autoimmune diseases and common variable immunodeficiency.IDrugs. 2007 Jan;10(1):53-9. [3]. Keino H, et al. Therapeutic effect of the potent IL-12/IL-23 inhibitor STA-5326 on experimental autoimmune uveoretinitis. Arthritis Res Ther. 2008;10(5):R122.
| Cas No. | 870087-36-8 | SDF | |
| 同義語 | STA 5326 mesylate | ||
| Canonical SMILES | CC1=CC=CC(/C=N/NC2=CC(N3CCOCC3)=NC(OCCC4=CC=CC=N4)=N2)=C1.CS(=O)(O)=O.CS(=O)(O)=O | ||
| Formula | C25H34N6O8S2 | M.Wt | 610.7 |
| 溶解度 | Water: 100 mg/mL (163.75 mM); DMSO: 12.5 mg/mL (20.47 mM) | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6375 mL | 8.1873 mL | 16.3747 mL |
| 5 mM | 327.5 μL | 1.6375 mL | 3.2749 mL |
| 10 mM | 163.7 μL | 818.7 μL | 1.6375 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)