| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
FPR-A14 targets the formyl peptide receptor (FPR), a G protein-coupled receptor that plays a central role in the innate immune response by detecting bacterial peptides and initiating chemotaxis of immune cells. Activation of FPR by agonists like FPR-A14 triggers a signaling cascade that includes the mobilization of intracellular calcium, activation of mitogen-activated protein kinases, and the reorganization of the actin cytoskeleton, leading to cell migration and other functional responses.
|
|---|---|
| ln Vitro |
In human neutrophils, FPR-A14 (Compound 14) triggers Ca2+ release with an EC50 of 630 nM. With an EC50 value of 42 nM, FPR-A14 is a neutrophil chemoattractant that causes neutrophil migration in a dose-dependent manner [1]. In mouse neuroblastoma N2a cells, FPR-A14 (1–10 μM; 48 hours) significantly increased the proportion of cell differentiation at 4 μM (32.0%), 6 μM (64.9%), 8 μM (89.1%), and 10 μM (93.3%). FPRa14 at 100μM had comparable effects on SH-SY5Y and IMR-32 cells [2].
In vitro, FPR-A14 acts as a potent activator of neutrophil function. It promotes neutrophil Ca2+ release with an EC50 of 630 nM and acts as a chemoattractant with an EC50 of 42 nM. Furthermore, in mouse neuroblastoma N2a cells, FPR-A14 (10 μM) is able to increase cell differentiation by 93.3%. These activities demonstrate its potent and broad effects on FPR-mediated cellular responses. |
| ln Vivo |
In vivo activity data for FPR-A14 are not extensively detailed in the provided search results. As a potent FPR agonist, it is a valuable tool for studying the role of FPR in immune cell recruitment and inflammation in animal models. It could be used to induce neutrophil chemotaxis in vivo, but specific protocols are not mentioned.
|
| Enzyme Assay |
For non-cellular in vitro receptor binding assays, FPR-A14 is used to characterize its binding affinity to the FPR. Typically, this involves radioligand binding displacement assays, where the ability of FPR-A14 to compete with a labeled agonist for binding to the receptor is measured to determine its affinity and confirm its specificity for FPR.
|
| Cell Assay |
For in vitro cellular assays, the activity of FPR-A14 is evaluated in cells expressing FPR, such as human neutrophils or cell lines like HL-60 or N2a. Key functional assays include measuring the increase in intracellular calcium using a fluorescent dye, and assessing chemotaxis using Boyden chamber assays. The EC50 values of 630 nM for Ca2+ release and 42 nM for chemoattractant activity are determined in such assays. Cell differentiation is assessed by morphological changes and the expression of differentiation markers.
|
| Animal Protocol |
In vivo animal studies with FPR-A14 would typically be conducted in mouse models to investigate the role of FPR in inflammation. For example, it could be administered to induce neutrophil recruitment in a model of peritonitis, or to study its effects on immune cell infiltration in other inflammatory conditions. The compound is soluble in DMSO, facilitating formulation for injection.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for FPR-A14 are not extensively documented. As a small-molecule agonist with a molecular weight of 404.42, it is expected to have moderate oral bioavailability. It is soluble in DMSO at 83.33 mg/mL (206.05 mM), which aids in formulation for both in vitro and in vivo applications. However, specific parameters such as half-life and clearance are not available in the provided search results.
|
| Toxicity/Toxicokinetics |
Toxicological data for FPR-A14 are limited. As a research compound, it is intended for laboratory use only and not for human therapeutic applications. Its safety profile has not been established for clinical use. At the concentrations used in research, it is generally considered to have low toxicity, but standard laboratory safety practices should always be followed.
|
| References |
|
| Additional Infomation |
FPR-A14 is a potent small-molecule agonist of the formyl peptide receptor (FPR). It activates neutrophils, promoting Ca2+ release (EC50 = 630 nM) and chemotaxis (EC50 = 42 nM). It also induces cell differentiation in N2a cells. FPR-A14 is a key tool for studying FPR-mediated immune signaling, inflammation, and cell differentiation.
|
| Molecular Formula |
C23H20N2O5
|
|---|---|
| Molecular Weight |
404.42
|
| Exact Mass |
404.137
|
| CAS # |
329691-12-5
|
| PubChem CID |
5503194
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.157
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
30
|
| Complexity |
580
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=C(C=CC(=C1)/C=N\NC(=O)C2=CC3=C(C=C2)OCO3)OCC4=CC=CC=C4
|
| InChi Key |
ULOKADSYVZOTTL-CFRMEGHHSA-N
|
| InChi Code |
InChI=1S/C23H20N2O5/c1-27-21-11-17(7-9-19(21)28-14-16-5-3-2-4-6-16)13-24-25-23(26)18-8-10-20-22(12-18)30-15-29-20/h2-13H,14-15H2,1H3,(H,25,26)/b24-13-
|
| Chemical Name |
N-[(Z)-(3-methoxy-4-phenylmethoxyphenyl)methylideneamino]-1,3-benzodioxole-5-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 125 mg/mL (309.08 mM)
|
|---|---|
| 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 | 2.4727 mL | 12.3634 mL | 24.7268 mL | |
| 5 mM | 0.4945 mL | 2.4727 mL | 4.9454 mL | |
| 10 mM | 0.2473 mL | 1.2363 mL | 2.4727 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
