1792180-81-4

Product Details:

CasNo： 1792180-81-4

Molecular Formula： C15H19N5O

Purity： 99%

Synonyms: PF-06651600; EOS-61890; 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one; 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2; CS-2733; PF-06651600; PF06651600; PF06651600; 1-[(2S,5R)-2-methyl-5(7H-pyrrolo[2,3-d]pyrimidine-4-ylamino)-1-piperidinly]-2-propen-1-onemalonate,PF06651600

Density: 1.272±0.06 g/cm3
Storage temp.: room temp
Solubility: DMSO: 100.0(Max Conc. mg/mL); 350.4(Max Conc. mM)
                 H2O: 5.0(Max Conc. mg/mL); 17.5(Max Conc. mM)
Pka: 13.03±0.50
Form: powder
Color: white to beige
InChI: InChI=1S/C15H19N5O/c1-3-13(21)20-8-11(5-4-10(20)2)19-15-12-6-7-16-14(12)17-9-18-15/h3,6-7,9-11H,1,4-5,8H2,2H3,(H2,16,17,18,19)/t10-,11+/m0/s1
InChIKey: CBRJPFGIXUFMTM-WDEREUQCSA-N
SMILES: C(N1C[C@H](NC2N=CN=C3NC=CC3=2)CC[C@@H]1C)(=O)C=C

Action mechanism:

The primary mechanism of action of Ritlecitinib involves inhibition of Janus kinase. Janus kinases are a class of enzymes that play a key role in the immune system, especially in the signaling process. The immune system uses Janus kinase to transmit information and regulate the activity of immune cells. In autoimmune diseases, the immune system mistakenly attacks and damages the body's own tissues, leading to inflammation and tissue damage. By inhibiting the Janus kinase, Ritlecitinib interferes with the abnormal activity of the immune system and reduces inflammation in the immune response, which is expected to reduce symptoms caused by autoimmune diseases, and this mechanism of action makes Ritlecitinib a potential treatment for autoimmune diseases.

Use:

Ritlecitinib is the second mature treatment for alopecia areata. It is a kinase inhibitor. Unlike the first drug, Olumiant, Ritlecitinib is approved not only for adult patients, but also for adolescents 12 years of age and older.

Ritlecitinib (PF-06651600) is a selective inhibitor of JAK3 with an IC50 of 33.1 nM. No activity on JAK1, JAK2 and TYK2 (IC50 > 10 000 nM).