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Baricitinib phosphate

Cat. No. M5315
Baricitinib phosphate Structure
Synonym:

INCB028050; LY3009104

Size Price Availability Quantity
5mg USD 180 In stock
10mg USD 260 In stock
50mg USD 580 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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. 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 469.41
Formula C16H20N7O6PS
CAS Number 1187595-84-1
Purity >98%
Solubility 10mM in DMSO
Storage at -20°C
References

Novel Oral Therapies for Psoriasis and Psoriatic Arthritis.
Yiu ZZ, et al. Am J Clin Dermatol. 2016 Jun;17(3):191-200. PMID: 26923915.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Baricitinib phosphate, INCB028050; LY3009104 supplier, JAK, inhibitors

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