SHR0302

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

Product information

CAS Number: 1445987-21-2

Molecular Weight: 414.48

Formula: C18H22N8O2S

Chemical Name: (3aR,6aS)-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-[methyl({7H-pyrrolo[2,3-d]pyrimidin-4-yl})amino]-octahydrocyclopenta[c]pyrrole-2-carboxamide

Smiles: CN(C1C[C@@H]2CN(C[C@@H]2C1)C(=O)NC1=NC(=NS1)OC)C1N=CN=C2NC=CC2=1

InChiKey: DNBCBAXDWNDRNO-FOSCPWQOSA-N

InChi: InChI=1S/C18H22N8O2S/c1-25(15-13-3-4-19-14(13)20-9-21-15)12-5-10-7-26(8-11(10)6-12)18(27)23-17-22-16(28-2)24-29-17/h3-4,9-12H,5-8H2,1-2H3,(H,19,20,21)(H,22,23,24,27)/t10-,11+,12?

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 31.25 mg/mL (75.40 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

SHR0302 (1 nM-10 µM; 48 hours; HSCs) treatment displays an inhibitory effect on the proliferation of HSCs in a concentration-dependent manner. SHR0302 (1 nM-10 µM) exerts an inhibitory effect on the activation, proliferation and migration of HSCs. SHR0302 (1 nM-10 µM; 48 hours; HSCs) treatment induces the apoptosis of HSCs. SHR0302 (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.

In Vivo:

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. SHR0302 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.

Products are for research use only. Not for human use.