927878-49-7
Chemical Structure
TFC 007
- CAS No.: 927878-49-7
- Formula:C27H29N5O4
- Molecular Weight:487.55
IUPAC Name: N-(4-(4-(morpholine-4-carbonyl)piperidin-1-yl)phenyl)-2-phenoxypyrimidine-5-carboxamide
InChIKey: NLSSUSRERAMBTA-UHFFFAOYSA-N
SMILES: O=C(N1CCOCC1)C2CCN(C3=CC=C(NC(C4=CN=C(OC5=CC=CC=C5)N=C4)=O)C=C3)CC2
Biological Activity: 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[1][2][3][4][5].
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TFC 007 | 98.01% | 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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References
- [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.