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-

Product Name2-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-
CAS2413693-96-4
MFC24H30N6O4
MW466.53
EINECS
MOL File2413693-96-4.mol

Chemical Properties

Boiling point	706.6±70.0 °C(Predicted)
Density	1.39±0.1 g/cm3(Predicted)
pka	3.25±0.50(Predicted)
form	Solid
color	Light yellow to yellow

Usage And Synthesis

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:	Nave 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.

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- Supplier

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