AF12198
Based on 6 publication(s) in Google Scholar
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 185413-30-3
- Formula: C96H123N19O22
- Molecular Weight:1895.12
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Storage:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) AF12198
More
Customer Validation & Images
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RT-PCR
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WB
Biological Activity
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IL-6 |
IL-8 |
IL1R1 8 nM (IC50) |
AF12198 competes for binding of 125I-IL-1α with an IC50 of 8.0 nM, nearly equal to that of IL-1ra, IC50 of 4.0 nM for the type I receptor[1].AF12198 (0-5 ng; 8 hours) inhibits IL-6 induction with an IC50 of 15 μM whereas IL-1ra inhibits with an IC50 of 2 nM in heparinized human primate blood. Meanwhile, With blood from cynomolgus monkeys, the IC50 values are 17 μM for AF12198 and 30 nM for IL-1ra. Additionally, AF12198 or IL-1RA alone does not induce IL-6 in blood from either humans or cynomolgus monkeys[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats[2]
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Dosage:16 mg/kg
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Administration:Intravenous infusion; 30 min before LPS intravenous injection
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Result:Decreased pulmonary microvascular leakage in rats.
Chemical Information
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CAS No. 185413-30-3
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Appearance Solid
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Molecular Weight 1895.12
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Formula C96H123N19O22
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Color White to off-white
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Sequence
Ac-Phe-Glu-Trp-Thr-Pro-Gly-Trp-Tyr-Gln-{Aze}-Tyr-Ala-Leu-Pro-Leu-NH2
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Sequence Shortening
Ac-FEWTPGWYQ-{Aze}-YALPL-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Publications (6)
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Journal Impact Factor
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Most Recent
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Small Methods
Electrical Sympathetic Neuromodulation Protects Bone Marrow Niche and Drives Hematopoietic Regeneration during Chemotherapy. [Abstract]2023 Jun;7(6):e2201300. PMID: 36843214 -
Toxicology
H3K18 lactylation-mediated SIX1 upregulation contributes to silica-induced epithelial-mesenchymal transition in airway epithelial cells. [Abstract]2025 Jun:514:154109. PMID: 40049282 -
J Inflamm Res
Interleukin 1β Mediates the Pathogenesis of Nasal Mucosal Epithelial Barrier Dysfunction in Allergic Rhinitis. [Abstract]2024 Nov 19:17:9071-9085. PMID: 39588138
AF12198 purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2024 Nov 19:17:9071-9085. [Abstract]
The changes of CLDN1 mRNA expression level in HNEpCs in each group using qPCR treated with AF12198 (10 nM).
AF12198 purchased from MedChemExpress. Usage Cited in: J Inflamm Res. 2024 Nov 19:17:9071-9085. [Abstract]
The changes of CLDN1 protein expression level in HNEpCs in each group using WB treated with AF12198 (10 nM).
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J Med Virol
Identification of RP-54745, an IL-1 Inhibitor Displaying Anticancer Activities for KSHV-Related Primary Effusion Lymphoma. [Abstract]2025 Feb;97(2):e70200. PMID: 39891599 -
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Solvent & Solubility
DMSO : 100 mg/mL (52.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (1.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. F Aimbire, et al. Low level laser therapy (LLLT) decreases pulmonary microvascular leakage, neutrophil influx and IL-1beta levels in airway and lung from rat subjected to LPS-induced inflammation. Inflammation [Content Brief]
[2]. A L Akeson, et al.AF12198, a novel low molecular weight antagonist, selectively binds the human type I interleukin (IL)-1 receptor and blocks in vivo responses to IL-1. J Biol Chem. 1996 Nov 29;271(48):30517-23. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.5277 mL | 2.6384 mL | 5.2767 mL | 13.1918 mL |
| 5 mM | 0.1055 mL | 0.5277 mL | 1.0553 mL | 2.6384 mL | |
| 10 mM | 0.0528 mL | 0.2638 mL | 0.5277 mL | 1.3192 mL | |
| 15 mM | 0.0352 mL | 0.1759 mL | 0.3518 mL | 0.8795 mL | |
| 20 mM | 0.0264 mL | 0.1319 mL | 0.2638 mL | 0.6596 mL | |
| 25 mM | 0.0211 mL | 0.1055 mL | 0.2111 mL | 0.5277 mL | |
| 30 mM | 0.0176 mL | 0.0879 mL | 0.1759 mL | 0.4397 mL | |
| 40 mM | 0.0132 mL | 0.0660 mL | 0.1319 mL | 0.3298 mL | |
| 50 mM | 0.0106 mL | 0.0528 mL | 0.1055 mL | 0.2638 mL |
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