Baricitinib [1187594-09-7]

Catalog number: HY-15315_100mg
Brand: MedChem Express
Packing: 100 mg
Other sizes: Also available in other sizes.
Price: € 207.00
Expected delivery time: 10 days
Quantity:

Product specifications for - Baricitinib [1187594-09-7]

Overview: 
Product group: Corona Related Products
Category: Other
CAS No.: 1187594-09-7
Properties: 
Purity: >98%
Molecular Formula: C16H17N7O2S
Molecular weight: 371.42
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: Baricitinib(INCB 028050, LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, 70 and 10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. IC50 Value: JAK1 (5.9 nM) and JAK2 (5.7 nM) [1]. Target: JAK1/2 in vitro: INCB028050 inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50 nM. Significant efficacy, as assessed by improvements in clinical, histologic and radiographic signs of disease, was achieved in the rat adjuvant arthritis model with doses of INCB028050 providing partial and/or periodic inhibition of JAK1/JAK2 and no inhibition of JAK3 [1]. in vivo: The efficacy following daily oral administration of INCB028050 was assessed at doses of 1, 3, or 10 mg/kg based on its pharmacokinetic profile in this species. Disease severity was assessed periodically, scoring clinical signs of disease. These doses were based on the PK/PD relationship established with the IL-6 WBA, with the goal of inhibiting JAK1/2 signaling by no more than 50% for half of the day. Relative to vehicle-treated animals, increasing doses of INCB028050 inhibited disease scores by 24% (p < 0.05), 57% (p < 0.01), and 81% (p < 0.01), respectively [1]. Baricitinib preferentially inhibits JAK1 and JAK2, with 10-fold selectivity over Tyk2 and 100-fold over JAK3. The observed effects of GLPG-0634 on the ACR20, albeit in a smaller study, appear to be at least as good as that seen with tofacitinib and superior to that of baricitinib, since baricitinib only moderately affect the ACR20 values in Phase IIa clinical studies [2]. Clinical trial: Baricitinib (LY3009104, INCB28050) against JAK1/JAK2 starting phase IIb for rheumatoid arthritis
Safety information: 
MSDS: MSDS
The target landscape of clinical kinase drugs', Klaeger S. Science. 2017 Dec 1;358(6367). pii: eaan4368. Read more