| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
TFC-007 selectively targets hematopoietic prostaglandin D synthase (H-PGDS). H-PGDS is a key enzyme in the biosynthesis of prostaglandin D2 (PGD2), a potent inflammatory mediator involved in allergic responses. By inhibiting H-PGDS, TFC-007 suppresses PGD2 production. The compound has an IC50 of 83 nM for H-PGDS. It exhibits negligible effects on COX-1, suggesting selectivity for the PGD2 synthesis pathway. TFC-007 can be conjugated with pomalidomide (a cereblon ligand) to form a PROTAC degrader.
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| ln Vitro |
TFC-007 demonstrates potent in vitro inhibition of H-PGDS enzyme activity. The compound inhibits H-PGDS with an IC50 of 83 nM. This high potency makes it a valuable tool for studying the role of PGD2 in inflammatory and allergic diseases. The compound's negligible effects on COX-1 indicate selectivity for the prostaglandin D2 synthesis pathway. Specific details on assay conditions and comparative data against other prostaglandin synthases are not extensively provided in the available literature.
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| ln Vivo |
TFC-007 has been studied in an animal model of allergic rhinitis. In cedar pollen-induced guinea pigs, TFC-007 inhibits PGD2 production and late phase nasal blockage. This demonstrates the compound's in vivo efficacy in suppressing PGD2-mediated allergic responses. The compound's ability to inhibit late phase nasal blockage suggests therapeutic potential for allergic rhinitis and other PGD2-related inflammatory conditions. Specific dosing regimens, routes of administration, and detailed efficacy data are not extensively provided in the available literature.
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| Enzyme Assay |
In vitro enzyme assays for TFC-007 involve measuring hematopoietic prostaglandin D synthase (H-PGDS) activity. Recombinant human H-PGDS enzyme is incubated with its substrate prostaglandin H2 (PGH2) and varying concentrations of TFC-007 (typically 0.1-1000 nM) in appropriate buffer. The reaction is initiated by addition of substrate and terminated by acidification or addition of stop solution. PGD2 production is quantified by ELISA or LC-MS/MS. IC50 values are calculated from concentration-response curves. Control experiments with known H-PGDS inhibitors are included for comparison. COX-1 and COX-2 inhibitory activity can also be assessed using similar protocols.
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| Cell Assay |
For in vitro cell-based assays, cells expressing H-PGDS (e.g., mast cells, dendritic cells, or transfected cell lines) are cultured and stimulated with appropriate inflammatory stimuli (e.g., calcium ionophore, LPS) to induce PGD2 production. Cells are pre-incubated with TFC-007 at various concentrations (typically 0.1-1000 nM) for 1-4 hours prior to stimulation. PGD2 levels in cell culture supernatants are measured by ELISA. Cell viability is assessed using MTT or similar assays. Inflammatory cytokine levels (e.g., IL-4, IL-5, IL-13) can also be measured to assess broader anti-inflammatory effects.
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| Animal Protocol |
In vivo animal studies for TFC-007 use a cedar pollen-induced allergic rhinitis model in guinea pigs. Animals are sensitized with cedar pollen extract, followed by intranasal challenge with pollen to induce allergic rhinitis symptoms. TFC-007 is administered orally or intranasally at doses determined from pharmacokinetic studies. Nasal blockage is assessed by measuring nasal airway resistance or by observing clinical symptoms. PGD2 levels in nasal lavage fluid are measured by ELISA. Late phase nasal blockage is monitored over several hours post-challenge. Histological examination of nasal tissues assesses inflammation and eosinophil infiltration.
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| ADME/Pharmacokinetics |
TFC-007 is a small molecule with molecular formula C27H29N5O4 and molecular weight 487.55. The compound is soluble in DMSO (<1 mg/mL, insoluble or slightly soluble). It should be stored at low temperature as powder at -20°C for up to 3 years and in solvent at -80°C for up to 1 year. Detailed pharmacokinetic parameters (absorption, distribution, metabolism, excretion, half-life, bioavailability) are not extensively characterized in the available literature. As a small molecule inhibitor, it would be expected to be orally bioavailable if formulated appropriately.
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| Toxicity/Toxicokinetics |
Specific toxicity data for TFC-007 are not extensively provided in the available literature. As an H-PGDS inhibitor, it would be expected to have a safety profile related to modulation of the prostaglandin D2 pathway. The compound exhibits negligible effects on COX-1, suggesting reduced risk of gastrointestinal and cardiovascular side effects associated with non-selective COX inhibition. Standard toxicology assessments would be required for therapeutic development, including acute, subchronic, and chronic toxicity studies, as well as genotoxicity and reproductive toxicity evaluations.
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| References | |
| Additional Infomation |
TFC-007 is a selective and potent hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with an IC50 of 83 nM. It suppresses inflammatory factors and inhibits PGD2 production. TFC-007 can be used to synthesize H-PGDS degrader PROTAC (H-PGDS)-1 by conjugating with pomalidomide (a cereblon ligand). The compound has been studied in a cedar pollen-induced guinea pig model of allergic rhinitis, where it inhibits late phase nasal blockage. It exhibits negligible effects on COX-1. No approved therapeutic status is reported. Further research is ongoing to explore its potential in allergic and inflammatory diseases.
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| Molecular Formula |
C27H29N5O4
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|---|---|
| Molecular Weight |
487.56
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| Exact Mass |
487.221
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| CAS # |
927878-49-7
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| PubChem CID |
16040067
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.639
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| LogP |
1.82
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
36
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| Complexity |
703
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CN(CCC1C(=O)N2CCOCC2)C3=CC=C(C=C3)NC(=O)C4=CN=C(N=C4)OC5=CC=CC=C5
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| InChi Key |
NLSSUSRERAMBTA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H29N5O4/c33-25(21-18-28-27(29-19-21)36-24-4-2-1-3-5-24)30-22-6-8-23(9-7-22)31-12-10-20(11-13-31)26(34)32-14-16-35-17-15-32/h1-9,18-20H,10-17H2,(H,30,33)
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| Chemical Name |
N-[4-[4-(morpholine-4-carbonyl)piperidin-1-yl]phenyl]-2-phenoxypyrimidine-5-carboxamide
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| Synonyms |
TFC007; TFC 007; TFC-007
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.0510 mL | 10.2551 mL | 20.5103 mL | |
| 5 mM | 0.4102 mL | 2.0510 mL | 4.1021 mL | |
| 10 mM | 0.2051 mL | 1.0255 mL | 2.0510 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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