| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
AG-09/1 targets formyl peptide receptor 1 (FPR1), a G protein-coupled receptor (GPCR) mainly expressed in phagocytic leukocytes but also found in many other cell types. FPR1 is a high-affinity receptor for N-formyl peptides such as fMLF and plays a crucial role in host defense and innate immunity by mediating leukocyte chemotaxis and activation. By acting as a specific FPR1 agonist, AG-09/1 activates FPR1-mediated signaling pathways.
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| ln Vitro |
Phagocyte activation by N-formyl peptide occurs via the G protein-coupled receptor known as FPR. The first cloned FPR, known as FPR1, encodes a high-affinity fMLF receptor [1].
In vitro, AG-09/1 is a selective and potent FPR1 agonist that activates chemotaxis in human neutrophils. It is a synthetic, non-peptide small molecule and a benzimidazole derivative. The compound's ability to activate FPR1 makes it valuable for studying neutrophil chemotaxis, phagocyte activation, and innate immune responses. However, specific EC50 values have not been detailed in the available literature. |
| ln Vivo |
In vivo, AG-09/1 has potential applications in studying host defense, innate immunity, and inflammatory responses. By activating FPR1, the compound may modulate immune cell recruitment and activation. However, specific in vivo efficacy data for AG-09/1 have not been detailed in the available literature. Further preclinical studies would be required.
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| Enzyme Assay |
For in vitro receptor binding and functional assays, cells expressing FPR1 or membrane preparations are incubated with radiolabeled ligands at various concentrations of AG-09/1 (0.1-1000 nM). Binding affinity is determined using radioligand binding assays. For functional assays, receptor activation is measured by assessing calcium mobilization using calcium-sensitive fluorescent dyes or by measuring chemotaxis in transwell assays.
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| Cell Assay |
For cell-based assays, human neutrophils or other FPR1-expressing cells are treated with AG-09/1 at concentrations ranging from 0.1-100 µM. Chemotaxis is assessed using transwell migration assays. Calcium mobilization is measured using fluorescent dyes. Cell activation markers such as CD11b expression and reactive oxygen species production can also be assessed.
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| Animal Protocol |
For in vivo studies, animal models of infection or inflammation would be used. AG-09/1 would be administered via appropriate routes at doses determined from pharmacokinetic studies. Immune cell recruitment, inflammatory responses, and host defense would be assessed. However, specific in vivo protocols for AG-09/1 have not been detailed in the available literature.
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| ADME/Pharmacokinetics |
AG-09/1 is soluble in DMSO at 100 mg/mL (279.04 mM). Storage is recommended at -20°C for powder (3 years) and -80°C for solutions (1 year). The compound is for research use only and is not intended for human or veterinary use. Standard laboratory safety precautions should be followed when handling this compound.
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| Toxicity/Toxicokinetics |
AG-09/1 is a research compound intended for laboratory use only and is not for human or veterinary use. As an FPR1 agonist, it may affect immune responses and should be handled with appropriate safety precautions. Comprehensive toxicology studies would be required before any clinical development.
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| References | |
| Additional Infomation |
AG-09/1 is a selective and potent formyl peptide receptor 1 (FPR1) agonist that activates chemotaxis in human neutrophils. It is a synthetic, non-peptide small molecule and a benzimidazole derivative. AG-09/1 is used in research to study FPR1 signaling, innate immunity, and host defense. It is a research tool and is not approved for clinical use.
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| Molecular Formula |
C16H14N4O4S
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|---|---|
| Molecular Weight |
358.3718
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| Exact Mass |
358.074
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| CAS # |
356776-32-4
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| PubChem CID |
3901842
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.806
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
481
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LYQDSNOFTIZWAX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14N4O4S/c1-24-12-6-7-13-14(8-12)19-16(18-13)25-9-15(21)17-10-2-4-11(5-3-10)20(22)23/h2-8H,9H2,1H3,(H,17,21)(H,18,19)
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| Chemical Name |
2-[(6-methoxy-1H-benzimidazol-2-yl)sulfanyl]-N-(4-nitrophenyl)acetamide
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~697.60 mM)
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| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7904 mL | 13.9521 mL | 27.9041 mL | |
| 5 mM | 0.5581 mL | 2.7904 mL | 5.5808 mL | |
| 10 mM | 0.2790 mL | 1.3952 mL | 2.7904 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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