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Baricitinib phosphate salt

CAS No.
1187595-84-1
Chemical Name:
Baricitinib phosphate salt
Synonyms
INCB-28050;LY-3009104 phosphate;INCB028050 phosphate);INCB-28050; LY3009104;Baricitinib (phosphate);Baricitinib phosphate salt;INCB424-Analogue (INCB-28050);Baricitinib phosphate (LY3009104 phosphate;Baricitinib phosphate (LY-3009104, INCB-028050, Olumiant);BARICITINIB PHOSPHATE (LY3009104 PHOSPHATE; INCB028050 PHOSPHATE)
CBNumber:
CB72621127
Molecular Formula:
C16H20N7O6PS
Molecular Weight:
469.412061
MDL Number:
MFCD25976707
MOL File:
1187595-84-1.mol
MSDS File:
SDS
Last updated:2024-03-18 11:47:05

Baricitinib phosphate salt Properties

storage temp. Store at -20°C
solubility insoluble in EtOH; insoluble in H2O; ≥172.6 mg/mL in DMSO
form White powder.
FDA UNII XIB47S8NNB

SAFETY

Risk and Safety Statements

Baricitinib phosphate salt price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
TRC B118693 BaricitinibPhosphate 1187595-84-1 5mg $45 2021-12-16 Buy
TRC B118693 BaricitinibPhosphate 1187595-84-1 50mg $205 2021-12-16 Buy
ApexBio Technology A3222 Baricitinibphosphate 1187595-84-1 50mg $210 2021-12-16 Buy
AK Scientific SYN1117 Baricitinibphosphate 1187595-84-1 5mg $295 2021-12-16 Buy
Adipogen Life Sciences SYN-1117-M010 Baricitinibphosphatesalt ≥95% 1187595-84-1 10mg $416 2021-12-16 Buy
Product number Packaging Price Buy
B118693 5mg $45 Buy
B118693 50mg $205 Buy
A3222 50mg $210 Buy
SYN1117 5mg $295 Buy
SYN-1117-M010 10mg $416 Buy

Baricitinib phosphate salt Chemical Properties,Uses,Production

IC50 & Target

JAK2: 5.7 nM (IC50)  JAK1: 5.9 nM (IC50)   Tyk2: 53 nM (IC50)   JAK3: 560 nM (IC50) 

In Vivo

Baricitinib 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.

Uses

Baricitinib is a JAK1 and JAK2 inhibitor and have been used as a promising treatment for rheumatoid arthritis.

Biological Activity

direct and indirect inhibition of the jaks has demonstrated rapid and sustained improvement in clinical measures of disease. baricitinib phosphate (incb 028050) is a selective jak1 and jak2 inhibitor.

in vitro

In cell-based assays, Baricitinib 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.

in vivo

significant efficacy was achieved in the rat adjuvant arthritis model with doses of baricitinib phosphate providing partial and/or periodic inhibition of jak1/jak2 and no inhibition of jak3. baricitinib phosphate was also effective in multiple murine models of arthritis, with no evidence of suppression of humoral immunity or adverse hematologic effects [2].

References

[1] fridman js, scherle pa, collins r, burn tc, li y, li j, covington mb, thomas b, collier p, favata mf, wen x, shi j, mcgee r, haley pj, shepard s, rodgers jd, yeleswaram s, hollis g, newton rc, metcalf b, friedman sm, vaddi k. selective inhibition of jak1 and jak2 is efficacious in rodent models of arthritis: preclinical characterization of incb028050. j immunol. 2010;184(9):5298-307.

1187594-09-7
1187595-84-1
Synthesis of Baricitinib phosphate salt from Baricitinib

Baricitinib phosphate salt Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 117)Suppliers
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View Lastest Price from Baricitinib phosphate salt manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Baricitinib phosphate salt pictures 2024-04-22 Baricitinib phosphate salt
1187595-84-1
US $50.00-30.00 / KG 1KG 99.9% 500 hebei hongtan Biotechnology Co., Ltd
Baricitinib phosphate salt pictures 2022-09-27 Baricitinib phosphate salt
1187595-84-1
US $0.00 / kg 1kg 99% 1000kg henan kanbei chemical co.,ltd
Baricitinib phosphate salt pictures 2021-07-02 Baricitinib phosphate salt
1187595-84-1
US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd

Baricitinib phosphate salt Spectrum

1187595-84-1(Baricitinib phosphate salt)Related Search:

2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile phosphate Baricitinib phosphate salt INCB-28050 INCB-28050; LY3009104 Baricitinib (phosphate) [1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl]acetonitrile phosphate INCB424-Analogue (INCB-28050) INCB-028050;LY-3009104;INCB 028050;LY 3009104;INCB028050;LY3009104 Baricitinib phosphate (LY3009104 phosphate BARICITINIB PHOSPHATE (LY3009104 PHOSPHATE; INCB028050 PHOSPHATE) INCB028050 phosphate) LY-3009104 phosphate Baricitinib phosphate (LY-3009104, INCB-028050, Olumiant) 1187595-84-1 C16H17N7O2SH3PO4 C16H20N7O6PS C16H17N7O2SH3O4P Inhibitors