SHR0302

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SHR0302是一种JAK抑制剂，与JAK1结合的亲和力比其他抑制剂更强（对JAK1的选择性是JAK2的10倍以上，JAK3的77倍以上，Tyk2的420倍以上）。

SHR0302 is a JAK inhibitor that binds JAK1 with stronger affinity than others (Selectivity for JAK1 is more than 10 times for JAK2, 77 times for JAK3, 420 times for Tyk2).

Ivarmacitinib (SHR0302; 1 nM-10 μM; 48 hours; HSCs) treatment displays an inhibitory effect on the proliferation of HSCs in a concentration-dependent manner.Ivarmacitinib (1 nM-10 μM) exerts an inhibitory effect on the activation, proliferation and migration of HSCs.Ivarmacitinib (1 nM-10 μM; 48 hours; HSCs) treatment induces the apoptosis of HSCs.Ivarmacitinib (1 nM-10 μM; 48 hours; HSCs) treatment significantly increases the activation of caspase-3 and Bax in HSCs, and decreases the expression of Bcl-2. SHR0302 also inhibits the activation of Akt signaling pathway. Cell Proliferation Assay Cell Line:Hepatic stellate cells (HSCs) Concentration:1 nM, 10 nM, 100 nM, 1μM, 10 μM Incubation Time:48 hours Result:Displayed an inhibitory effect on the proliferation of HSCs, and that inhibition ocurred in a concentration-dependent manner.Apoptosis Analysis Cell Line:Hepatic stellate cells (HSCs) Concentration:1 nM, 10 nM, 100 nM, 1μM, 10 μM Incubation Time:48 hours Result:Induced the apoptosis of HSCs.Western Blot Analysis Cell Line:Hepatic stellate cells (HSCs) Concentration:1 nM, 10 nM, 100 nM, 1μM, 10 μM Incubation Time:48 hours Result:Significantly increased the activation of caspase-3 and Bax in HSCs, and decreased the expression of Bcl-2. Also inhibited the activation of Akt signaling pathway.

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. 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. Animal Model:Male Sprague-Dawley (SD) rats (150-180 g) injected with complete Freund’s adjuvant (CFA)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.

ARQ252

Angiogenesis

JAK

JAK1

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1445987-21-2

414.48

C18H22N8O2S

>98% (HPLC)

DMSO:30mg/ml(72.38mM; Need ultrasonic)

CN(C(C1)C[C@@H](C2)[C@H]1CN2C(Nc1nc(OC)ns1)=O)c1ncnc2c1cc[nH]2

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(-20℃)

With Ice Pack

≥ 2 years