中文名称

巴瑞克替尼磷酸盐.

中文别名

[1-(乙基磺酰基)-3-[4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基]氮杂环丁烷-3-基]乙腈磷酸盐;巴瑞克替尼磷酸盐;INCB-28050

英文名称

Baricitinib phosphate

英文别名

INCB-28050;Baricitinib phosphate;2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile,phosphoric acid;[1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl]acetonitrile phosphate;Baricitinib phosphate salt;INCB 028050;INCB-028050;LY 3009104;LY-3009104;Baricitinib (phosphate);XIB47S8NNB;INCB28050;baricitinib-phosphate;Baricitinib?Phosphate;3-Azetidineacetonitrile, 1-(ethylsulfonyl)-3-(4-(7H-pyrrolo(2,3-d)pyrimidin-4-yl)-1H-pyrazol-1-yl)-, phosphate (1:1);SYN1117;FBPOWTFFUBBKBB-UHFFFAOYSA-N;C16H17N7O2S.H3PO4;BCP15527;[1-(Ethylsulfonyl)-3-[4-(7H-p

Cas No.

1187595-84-1

分子式

C16N7O6PSH20

分子量

469.41

包装储存

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

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.

性状

Solid

IC50 & Target[1][2]

JAK2

5.7 nM (IC50)

JAK1

5.9 nM (IC50)

Tyk2

53 nM (IC50)

JAK3

560 nM (IC50)

体外研究(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. 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. CD8NKG2D 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)