Art. -Nr.: HY-110167

TFC 007

Name: TFC 007
Brand: MedChemExpress
SKU: HY-110167
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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.

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Reinheit : 98.01%
CAS. Nr.: 927878-49-7
Formel: C₂₇H₂₉N₅O₄
Molecular Weight:487.55

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

TFC 007 Chemical Structure

CAS. Nr.: 927878-49-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[2]^[4]^[5]

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

OthersLipid Inflammatory Mediators

Others

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 P_app 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].

Lipid Inflammatory Mediators

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.

Western Blot Analysis^[2]

Cell Line:

KU812 cells
Concentration:

TFC-007 1 μM; Pomalidomide 1 μM
Incubation Time:

6 h
Result:

Did not effectively decrease H-PGDS protein levels.

ELISA Assay^[4]

Cell Line:

KU812 cells
Concentration:

10 nM
Incubation Time:

24 h + 5 μM A23187 for 30 min
Result:

Decreased PGD2 levels compared with the DMSO control.
Produced less PGD2 suppression than the corresponding PROTACs at 10 nM.

Western Blot Analysis^[2]

Cell Line:

KU812 cells
Concentration:

10, 100 nM
Incubation Time:

24 h
Result:

Did not reduce H-PGDS protein levels at either concentration.

Western Blot Analysis^[2]

Cell Line:

KU812 cells
Concentration:

10, 100 nM
Incubation Time:

24 h + four washes + 6 h compound-free incubation
Result:

Did not induce persistent H-PGDS protein reduction after compound removal.

Western Blot Analysis^[4]

Cell Line:

KU812 cells
Concentration:

TFC-007 10 μM + PROTAC 2 1 nM
Incubation Time:

6 h
Result:

Suppressed the PROTAC 2-induced reduction of H-PGDS protein levels.

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2	AUC_0-24	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

OthersInnate ImmunityLipid Inflammatory Mediators

Others

TFC-007 (30 mg/kg; p.o.; single dose; 1 h before challenge) attenuates late-phase nasal obstruction 3-8 h after antigen challenge in Japanese cedar pollen-induced allergic rhinitis male Hartley guinea pigs, but does not affect the sneezing response within 1 h after challenge or early-phase nasal obstruction 0-3 h^[5].
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].

Innate Immunity

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].

Lipid Inflammatory Mediators

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.

Animal Model:

Hartley (male, 4-week-old)^[5]
Dosage:

30 mg/kg
Administration:

p.o.; single administration; 1 h after challenge
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.

Animal Model:

Hartley (male, 4-week-old)^[5]
Dosage:

30 mg/kg
Administration:

p.o.; single administration; 1.5 h after challenge
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

CAS. Nr. 927878-49-7
Appearance Solid
Molecular Weight 487.55
Formel C₂₇H₂₉N₅O₄
Color White to light yellow
SMILES

O=C(N1CCOCC1)C2CCN(C3=CC=C(NC(C4=CN=C(OC5=CC=CC=C5)N=C4)=O)C=C3)CC2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0511 mL

10.2554 mL

20.5107 mL

5 mM

---

10 mM

---

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Osawa H, et al. CRBN ligand expansion for hematopoietic prostaglandin D synthase (H-PGDS) targeting PROTAC design and their in vitro ADME profiles. Bioorganic & medicinal chemistry. 2023 Apr 15;84:117259.

[2]. Yokoo H, et al. Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer. ACS medicinal chemistry letters. 2021 Feb 11;12(2):236-241. [Content Brief]

[3]. Osawa H, et al. Optimizing linker rigidity to improve intracellular behavior of PROTACs targeting hematopoietic prostaglandin D synthase. RSC medicinal chemistry. 2025 Oct 15;16(10):4721-4730.

[4]. Murakami Y, et al. Structure-activity relationship study of PROTACs against hematopoietic prostaglandin D2 synthase. RSC Med Chem. 2022;13:1495-1503.

[5]. Nabe T, et al. Inhibition of hematopoietic prostaglandin D synthase improves allergic nasal blockage in guinea pigs. Prostaglandins & other lipid mediators. 2011 Aug;95(1-4):27-34.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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TFC 007