TFC 007
Based on 1 Customer Validation
TFC-007 is a selective and orally effective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, with an IC50 of 71 nM for H-PGDS. TFC-007 shows weak effects on L-PGDS and various arachidonic acid-related enzymes and receptors. TFC-007 inhibits PGD2 production in KU812 cells without decreasing H-PGDS protein levels. TFC-007 can be used for research on H-PGDS/PGD2 signaling and allergic rhinitis.
For research use only. We do not sell to patients.
- Purity : 98.01%
- CAS No.: 927878-49-7
- Formula: C27H29N5O4
- Molecular Weight:487.55
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
Biological Activity
Description
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H-PGDS 0.32 μM (IC50) |
H-PGDS 71 nM (IC50) |
H-PGDS 211.2 nM (IC50) |
H-PGDS 0.083 μM (IC50) |
In Vitro
The logD of TFC-007 is 3.06[1].
The PBS solubility of TFC-007 (100 μM; 10 min) is 3.17 μM[1].
TFC-007 (4 h) exhibits a Papp of 3.01 × 10-6 cm/s in the PAMPA artificial membrane system[1].
After incubation in human liver microsomes for 10 and 60 min, TFC-007 (10-60 min) retains 96% and 80% of the unchanged product, respectively[1].
TFC-007 binds to H-PGDS in a competitive fluorescence polarization assay with an IC50 of 0.32 μM[2].
TFC-007 (10 μM; 3 h) inhibits ligand binding to the H1 receptor in human recombinant CHO cell membranes by 17%[5].
TFC-007 inhibits H-PGDS enzymatic activity with an IC50 of 71 nM[2].
TFC-007 (1 μM; in combination with 1 μM Pomalidomide (HY-10984); 6 h) does not effectively reduce H-PGDS protein levels in KU812 cells[2].
TFC-007 (10-100 nM; 24 h) does not decrease H-PGDS protein levels in KU812 cells[2].
TFC-007 (10-100 nM; 24 h; after 4 washes and incubation in compound-free medium for 6 h) still does not induce a decrease in H-PGDS protein in KU812 cells[2].
TFC-007 (10-100 nM; 24 h; followed by stimulation with 5 μM A23187 (HY-N6687) for 30 min in the presence of TFC-007) decreases PGD2 production in KU812 cells[2].
The inhibitory effect of TFC-007 (10-100 nM; 24 h; after 4 washes and 6 h incubation without compound; followed by stimulation with 5 μM A23187 for 30 min) on PGD2 production in KU812 cells disappears, and PGD2 production recovers[2].
TFC-007 exhibits an IC50 of 211.2 nM against H-PGDS in a competitive fluorescence polarization assay[4].
TFC-007 (10 μM; combined with 1 nM PROTAC 2; 6 h) inhibits PROTAC 2-induced H-PGDS protein reduction in KU812 cells[4].
TFC-007 (10 nM; 24 h; followed by stimulation with 5 μM A23187 for 30 min) decreases PGD2 levels in the culture medium of KU812 cells[4].
TFC-007 (0.1-100 μM; preincubation for 5 min; PGH2 reaction for 1 min) concentration-dependently inhibits human recombinant H-PGDS activity with an IC50 of 0.083 μM[5].
TFC-007 (10 μM; 30 min) shows an inhibition rate of -1% on ligand binding to the CysLT1 receptor in human recombinant CHO-K1 cell membranes[5].
TFC-007 (10 μM; 30 min) shows an inhibition rate of -2% on ligand binding to human recombinant HEK-293 cell membrane TP receptors[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KU812 cells
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Concentration:TFC-007 1 μM; Pomalidomide 1 μM
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Incubation Time:6 h
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Result:Did not effectively decrease H-PGDS protein levels.
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Cell Line:KU812 cells
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Concentration:10 nM
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Incubation Time:24 h + 5 μM A23187 for 30 min
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Result:Decreased PGD2 levels compared with the DMSO control.
Produced less PGD2 suppression than the corresponding PROTACs at 10 nM.
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Cell Line:KU812 cells
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Concentration:10, 100 nM
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Incubation Time:24 h
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Result:Did not reduce H-PGDS protein levels at either concentration.
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Cell Line:KU812 cells
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Concentration:10, 100 nM
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Incubation Time:24 h + four washes + 6 h compound-free incubation
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Result:Did not induce persistent H-PGDS protein reduction after compound removal.
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Cell Line:KU812 cells
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Concentration:TFC-007 10 μM + PROTAC 2 1 nM
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Incubation Time:6 h
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Result:Suppressed the PROTAC 2-induced reduction of H-PGDS protein levels.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUC0-24 | Plasma Concentration |
|---|---|---|---|---|---|---|---|
| Pig[5] | 30 mg/kg | p.o. | 6.8 μM | 2 h | 6.6 h | 68.6 μM·h | 2.8 μM |
In Vivo
TFC-007 (30 mg/kg; p.o.; single dose; 1 h before challenge) almost completely inhibits the increase in PGD2 in nasal lavage fluid 20 min after antigen challenge and reduces the increase in PGD2 at 5 h in Japanese cedar pollen-induced allergic rhinitis male Hartley guinea pigs, but does not inhibit the increases in CysLTs and TXB2 at 20 min or 5 h[5].
TFC-007 (30 mg/kg; p.o.; single dose; 1 h before challenge) does not inhibit the increase in eosinophils in nasal lavage fluid 5 h after antigen challenge in Japanese cedar pollen-induced allergic rhinitis male Hartley guinea pigs, nor does it affect the increases in monocyte populations and neutrophils[5].
TFC-007 (30 mg/kg; p.o.; single dose; 1.5 h after challenge) markedly inhibits the increase in PGD2 in nasal lavage fluid 5 h after antigen challenge in Japanese cedar pollen-induced allergic rhinitis male Hartley guinea pigs, but does not alleviate nasal obstruction 2-8 h after challenge[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Hartley (male, 4-week-old)[5]
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Dosage:30 mg/kg
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Administration:p.o.; single administration; 1 h after challenge
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Result:Almost completely suppressed the increase in PGD2 in NCLF at 20 min and reduced the increase at 5 h after challenge.
Attenuated late-phase nasal blockage during 3-8 h.
Did not affect sneezing or early-phase nasal blockage during 0-3 h.
Did not suppress increases in eosinophils, mononuclear cells, or neutrophils.
Did not inhibit increases in CysLTs or TXB2 at 20 min or 5 h after challenge.
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Animal Model:Hartley (male, 4-week-old)[5]
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Dosage:30 mg/kg
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Administration:p.o.; single administration; 1.5 h after challenge
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Result:Strongly suppressed the increase in PGD2 in NCLF at 5 h after challenge.
Did not reduce nasal blockage during 2-8 h after challenge.
Chemical Information
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CAS No. 927878-49-7
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Appearance Solid
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Molecular Weight 487.55
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Formula C27H29N5O4
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Color White to light yellow
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SMILES
O=C(N1CCOCC1)C2CCN(C3=CC=C(NC(C4=CN=C(OC5=CC=CC=C5)N=C4)=O)C=C3)CC2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 1 mg/mL (2.05 mM; Need ultrasonic and warming; 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. 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. 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)
Purity & Documentation
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Data Sheet (288 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0511 mL | 10.2554 mL | 20.5107 mL | 51.2768 mL |
TFC 007 Related Classifications
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