| Identification | Back Directory | [Name]
2-Pyridinecarboxamide, 4-[[2-[[(R)-(1,4-dimethyl-1H-pyrazol-3-yl)(1-methylcyclopentyl)methyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]-3-hydroxy-N,N-dimethyl- | [CAS]
2413693-96-4 | [Synonyms]
PF-07054894
DE-07054894
(R)-4-[[2-[[(1,4-Dimethyl-3-pyrazolyl)(1-methylcyclopentyl)methyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]-3-hydroxy-N,N-dimethylpyridine-2-carboxamide
2-Pyridinecarboxamide, 4-[[2-[[(R)-(1,4-dimethyl-1H-pyrazol-3-yl)(1-methylcyclopentyl)methyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]-3-hydroxy-N,N-dimethyl- | [Molecular Formula]
C24H30N6O4 | [MOL File]
2413693-96-4.mol | [Molecular Weight]
466.53 |
| Chemical Properties | Back Directory | [Boiling point ]
706.6±70.0 °C(Predicted) | [density ]
1.39±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
3.25±0.50(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
PF-07054894 is an orally active and potent C-C Chemoattractant Cytokine (Chemokine) Receptor 6 (CCR6) antagonist that blocks CCR6-mediated chemotaxis with an IC50 value of 5.7 nM in vitro. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease[1][2][3][4]. | [in vivo]
PF-07054894 (10 mg/kg, p.o., twice a day for 6 consecutive days) increases circulating CCR6+ T cells in na ve cynomolgus monkeys[2][3].
PF-07054894 (100 mg/kg, p.o., once or twice per day for 12 days) is efficacious in interleukin-23-induced inflammation in skin inflammation mouse model[2].
| Animal Model: | Na?ve cynomolgus monkeys[2][3] | | Dosage: | 10 mg/kg | | Administration: | p.o., twice a day for 6 consecutive days | | Result: | Resulted in an increase in the frequency of most circulating CCR6+ T lymphocytes populations examined (CCR6+ CD4+ and CD8+ cells including total, effector, memory, Th17, and Th1/17 cells). |
| Animal Model: | Skin inflammation mouse model[2] | | Dosage: | 100 mg/kg | | Administration: | p.o., once or twice per day for 12 days | | Result: | Inhibited mouse ear swelling induced by interleukin-23 intradermal injection. |
| [IC 50]
CCR6 | [References]
[1] Gómez S, et, al. Desarrollo de anticuerpos terapéuticos contra el receptor CCR6 humano.
[2] Li W, et al. A Novel C-C Chemoattractant Cytokine (Chemokine) Receptor 6 (CCR6) Antagonist (PF-07054894) Distinguishes between Homologous Chemokine Receptors, Increases Basal Circulating CCR6+ T Cells, and Ameliorates Interleukin-23-Induced Skin Inflammation. J Pharmacol Exp Ther. 2023 Jul;386(1):80-92. DOI:10.1124/jpet.122.001452
[3] Li W, et al. A novel CCR6 antagonist (PF-07054894) that distinguishes between homologous chemokine receptors, increases basal circulating CCR6+ T cells, and ameliorates interleukin-23-induced skin inflammation[J]. Journal of Pharmacology and Experimental Therapeutics, 2023.
[4] Chinigo G M, et al. Early Process Development of PF-07054894, a Squaramide-Based Antagonist of C–C Chemokine Receptor Type 6 (CCR6)[J]. Organic Process Research & Development, 2024. |
|
| Company Name: |
ChemCell Biomedicine Co.,Ltd.
|
| Tel: |
020-13556033878 2965585218 13556033878 |
| Website: |
http://m.approvedhomemanagement.com/ShowSupplierProductsList15061/0.htm |
| Company Name: |
DC Chemicals
|
| Tel: |
021-58447131 13564518121 |
| Website: |
http://m.approvedhomemanagement.com/ShowSupplierProductsList927327/0.htm |
|