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1187595-84-1 | Baricitinib (phosphate)

Baricitinib (phosphate) NLT 98%

SKU : MC509857

CAS Number : 1187595-84-1

Molecular Formula : C16H17N7O2S | Molecular Weight : 371.42

Synonyms : LY3009104 (phosphate);INCB028050 (phosphate)

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Purity NLT 98%
Storage at 20ºC 2 years

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Chemical Name Baricitinib (phosphate)
CAS Number 1187595-84-1
MDL Number MFCD21608464
Molecular Formula C16H17N7O2S
Molecular Weight 371.42
Synonyms LY3009104 (phosphate);INCB028050 (phosphate)
Introduction of 1187595-84-1 :

Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively. IC50 & Target: IC50: 5.9 nM (JAK1), 5.7 nM (JAK2), >400 nM (JAK3), 53 nM (Tyk2)[1] In Vitro: In cell-based assays, Baricitinib phosphate (INCB028050 phosphate) proves to be a potent inhibitor of JAK signaling and function. In PBMCs, Baricitinib inhibits IL-6-stimulated phosphorylation of the canonical substrate STAT3 (pSTAT3) and subsequent production of the chemokine MCP-1 with IC50 values of 44 nM and 40 nM, respectively. In isolated naive T-cells, INCB028050 also inhibits pSTAT3 stimulated by IL-23 (IC50=20 nM). Importantly, this inhibition prevented the production of two pathogenic cytokines (IL-17 and IL-22) produced by Th17 cells-a subtype of helper T cells with demonstrable inflammatory and pathogenic properties-with an IC50 value of 50 nM. In stark contrast, the structurally similar but ineffective JAK1/2 inhibitors INCB027753 and INCB029843 has no significant effect in any of these assays systems when tested at concentrations up to 10 μM[1]. In Vivo: Baricitinib phosphate (INCB028050 phosphate) treatment, compares with vehicle, inhibits the increase in hind paw volumes during the 2 wk of treatment by 50% at a dose of 1 mg/kg and >95% at doses of 3 or 10 mg/kg. Because baseline paw volume measurements are taken on treatment day 0-in animals with significant signs of disease-it is possible to have >100% inhibition in animals showing marked improvement in swelling[1]. Baricitinib (0.7 mg/day) treated mice exhibits substantially reduced inflammation as assessed by H&E staining, reduced CD8 infiltration, and reduced MHC class I and class II expression when compared with vehicle-control treated mice. CD8+NKG2D+ cells, critical effectors of disease in murine and human alopecia areata (AA), are greatly diminished in Baricitinib treated mice compare with vehicle control treated mice[2].

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