ChemicalBook CAS DataBase List 1445987-21-2

1445987-21-2

Name	Cyclopenta[c]pyrrole-2(1H)-carboxamide, hexahydro-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, (3aα,5α,6aα)-
CAS	1445987-21-2
Molecular Formula	C18H22N8O2S
MDL Number	MFCD32701909
Molecular Weight	414.48
MOL File	1445987-21-2.mol

Chemical Properties

density	1.507±0.06 g/cm3(Predicted)
form	Solid
pka	11.81±0.40(Predicted)
color	Off-white to light yellow

Hazard Information

Uses

Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects[1][2].

in vivo

Ivarmacitinib (SHR0302; 0.3-3.0 mg/kg; intragastric administration; twice a day; for 14 days; male Sprague-Dawley (SD) rats) treatment suppresses the severity of AA rats by attenuating the arthritis index, arthritis global assessment and paw swelling degree, and alleviated histopathology of spleen and joint of AA rats^[1].
Ivarmacitinib can inhibit the proliferation of T, B and fibroblast-like synoviocytes (FLS), and down-regulates cytokines TNF-α, IL-1β, IL-17 and antibody IgG1, IgG2a levels, and suppresses the proportion of Th17 and total B, and inhibits JAK1-STAT3 phosphorylation^[1].

Animal Model:	Male Sprague-Dawley (SD) rats (150-180 g) injected with complete Freund’s adjuvant (CFA)^[1]
Dosage:	0.3 mg/kg,1.0 mg/kg, 3.0 mg/kg
Administration:	Intragastric administration; twice a day; for 14 days
Result:	Suppressed the severity of adjuvant-induced arthritis (AA) rats by attenuating the arthritis index, arthritis global assessment and paw swelling degree, and alleviated histopathology of spleen and joint of AA rats.

IC 50

JAK1; JAK2; JAK3; Tyk2

References

[1] Huaxun Wu, et al. JAK1-STAT3 Blockade by JAK Inhibitor SHR0302 Attenuates Inflammatory Responses of Adjuvant-Induced Arthritis Rats and Decreases Th17 and Total B Cells. Joint Bone Spine. 2016 Oct;83(5):525-32. DOI:10.1016/j.jbspin.2015.09.002
[2] Yuan-Jing Gu, et al. Targeted Blockade of JAK/STAT3 Signaling Inhibits Proliferation, Migration and Collagen Production as Well as Inducing the Apoptosis of Hepatic Stellate Cells. Int J Mol Med. 2016 Sep;38(3):903-11. DOI:10.3892/ijmm.2016.2692

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