Ivarmacitinib (SHR0302)

Chemical Structure : Ivarmacitinib

CAS No.: 1445987-21-2

Catalog No.: PC-73423Not For Human Use, Lab Use Only.

Ivarmacitinib (SHR0302) is a potent highly selective, Janus kinase 1 (JAK1) inhibitor with IC50 of 0.1 nM, 9-fold selectivity over JAK2 and >70-fold over JAK3 and TYK2.

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2 mg	$198	In stock
5 mg	$328	In stock
10 mg	$528	In stock
25 mg	$898	In stock
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Biological Activity

Ivarmacitinib (SHR0302) is a potent highly selective, Janus kinase 1 (JAK1) inhibitor with IC50 of 0.1 nM, 9-fold selectivity over JAK2 and >70-fold over JAK3 and TYK2.
SHR0302 is a synthetic molecule that potently inhibits all members of the JAK family, particularly JAK1.
SHR0302 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.
SHR0302 inhibited the proliferation of T, B and FLS, and down-regulated cytokines TNF-α, IL-1β, IL-17 and antibody IgG1, IgG2a levels, and suppressed the proportion of Th17 and total B, and inhibited JAK1-STAT3 phosphorylation.
SHR0302 (1-10,000 nM) exerted an inhibitory effect on the activation, proliferation and migration of hepatic stellate cells (HSCs).

Physicochemical Properties

M.Wt	414.488
Formula	C18H22N8O2S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	rel-(3aR,5s,6aS)-N-(3-Methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxamide

References

1. Wu H, et al. Joint Bone Spine. 2016 Oct;83(5):525-32.

2. Gu YJ, et al. Int J Mol Med. 2016 Sep;38(3):903-11.

3. Zhao Y, et al. Am J Clin Dermatol. 2021 Nov;22(6):877-889.