| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
FPR1; FPR2/ALX
TC-FPR-43 targets formyl peptide receptor 1 (FPR1) and formyl peptide receptor 2 (FPR2), which was previously known as formyl peptide receptor-like 1 (FPRL1). These are G protein-coupled receptors involved in host defense and inflammation. By activating FPR2, TC-FPR-43 induces calcium flux and inhibits fMLP- and IL-8-induced neutrophil migration. |
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| ln Vitro |
FPR Agonist 43 (10-5-107 nM) exhibits active potency in the cAMP assay in FPR2/ALX over-expressing CHO cells[1].
FPR Agonist 43 is also active (IC50=207±51 nM) in the GTPγ binding assay[1]. FPR1 is the preferred receptor for FPR Agonist 43 in human neutrophils as well as possibly in mouse cells[2]. In vitro, TC-FPR-43 is a potent FPR2 agonist with an EC50 of 44 nM. It induces calcium flux in CHO cells expressing human FPR2, Ga15, and aequorin. The compound inhibits fMLP- and IL-8-induced neutrophil migration, demonstrating anti-inflammatory activity. It is a dual agonist of FPR1 and FPR2/ALX. |
| ln Vivo |
In vivo, TC-FPR-43 is orally active and has anti-inflammatory properties. By activating FPR2, the compound modulates inflammatory responses and neutrophil migration. It has potential applications in the study of inflammatory diseases where FPR signaling plays a role. The compound's oral bioavailability makes it suitable for oral administration in preclinical studies.
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| Enzyme Assay |
In vitro receptor binding assays for TC-FPR-43 measure its affinity for FPR1 and FPR2 using radioligand displacement techniques. Membranes prepared from cells expressing the receptors are incubated with a radiolabeled FPR ligand and varying concentrations of the compound. Functional assays measure calcium flux in CHO cells expressing human FPR2, with an EC50 of 44 nM.
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| Cell Assay |
Cell Line: Chinese hamster ovary (CHO) over-expressing human FPR2/ALX receptors
Concentration: 10-5, 10-3, 0.1, 10, 1000, 105, 107 nM Result: Actively potent in the cAMP assay in FPR2/ALX over-expressing CHO cells (IC50 =11.6±1.9 nM). In vitro cell-based assays for TC-FPR-43 use CHO cells expressing human FPR2, Ga15, and aequorin to measure calcium flux. Cells are treated with serial dilutions of the compound, and calcium-dependent luminescence is measured. Neutrophil migration assays are used to assess the compound's ability to inhibit fMLP- and IL-8-induced chemotaxis. |
| Animal Protocol |
In vivo animal models for TC-FPR-43 include models of inflammatory diseases such as acute lung injury, peritonitis, or other conditions involving neutrophil migration. The compound is administered orally, and its effects on inflammatory cell infiltration, cytokine production, and tissue damage are evaluated. Pharmacodynamic studies measure FPR2 activation and inhibition of neutrophil migration.
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| ADME/Pharmacokinetics |
TC-FPR-43 has a molecular formula of C20H21ClN4O2 and a molecular weight of 384.86 g/mol. It is stored at +4°C and has a purity of ≥98%. The compound is orally active and is soluble in DMSO. It is also known as FPR Agonist 43 and compound 43.
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| Toxicity/Toxicokinetics |
The toxicity profile of TC-FPR-43 is characterized in preclinical safety studies. As an FPR agonist, the compound may affect immune function and inflammatory responses. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
TC-FPR-43 is a potent dual formyl peptide receptor 1 (FPR1) and formyl peptide receptor 2 (FPR2)/ALX agonist. It is an orally active FPR2 agonist with an EC50 of 44 nM. TC-FPR-43 induces calcium flux in FPR2-expressing cells and inhibits fMLP- and IL-8-induced neutrophil migration. The compound is also known as FPR Agonist 43 and is intended for laboratory research use only.
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| Molecular Formula |
C20H21CLN4O2
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|---|---|
| Molecular Weight |
384.859343290329
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| Exact Mass |
384.14
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| Elemental Analysis |
C, 62.42; H, 5.50; Cl, 9.21; N, 14.56; O, 8.31
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| CAS # |
903895-98-7
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| PubChem CID |
24776341
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| Appearance |
White to light yellow solid powder
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
593
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CCLSQFCCNKQZLZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H21ClN4O2/c1-13(2)17-18(24(20(22)27)15-11-9-14(21)10-12-15)19(26)25(23(17)3)16-7-5-4-6-8-16/h4-13H,1-3H3,(H2,22,27)
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| Chemical Name |
N-(4-Chlorophenyl)-N-[2,3-dihydro-1-methyl-5-(1-methylethyl)-3-oxo-2-phenyl-1H-pyrazol-4-yl]-urea
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| Synonyms |
TC-FPR-43; TC FPR 43; TCFPR43
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: ~37.5 mg/mL (~97.4 mM)
H2O: < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5983 mL | 12.9917 mL | 25.9835 mL | |
| 5 mM | 0.5197 mL | 2.5983 mL | 5.1967 mL | |
| 10 mM | 0.2598 mL | 1.2992 mL | 2.5983 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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