Baricitinib Manufacturer 1187594-09-7 For Anticancer CAS NO.1187594-09-7

Min.Order Quantity:: 10 Gram

Purity:: 99%

Port:: Wuhan

Payment Terms:: T/T,MoneyGram

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99%min Baricitinib
Baricitinib Manufacturer
For Anticancer

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ProName: Baricitinib Manufacturer 1187594-09-7 ...
CasNo: 1187594-09-7
Molecular Formula: C16H17N7O2S
Appearance: White Powder
Application: It Can Be Used As Pharmaceutical Inte...
DeliveryTime: 2-4 days after confirming your payment...
PackAge: 100g/ bag, 2 kg/ bag, 25kg/ carton or ...
Port: Wuhan
ProductionCapacity: 10000 Metric Ton/Month
Purity: 99%
Storage: Store in sealed containers at cool & d...
Transportation: By DHL, TNT, FedEx, HKEMS, UPS, Etc
LimitNum: 10 Gram

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hubei xinrunde chemical co., ltd is a renowned pharmaceutical manufacturer. we can offer high quality products at competitive price in quick delivery with 100% custom pass guaranteed. never stop striving to offer our best service is our philosophy. we have flexible and untraceable payment terms. as a leading manufacture, our products have been exported to germany, norway, poland, finland, spain, uk, france, russia, usa, brazil, mexico, australia, japan, korea, thailand, indonesia, uruguay and many other countries.

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baricitinib basic information

description bioactivity in vitro in vivo references

product name:	baricitinib
synonyms:	1-(ethylsulfonyl)-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]-3-azetidineacetonitrile;baricitinib;incb 028050;ly 3009104;baricitinib (ly3009104);baricitinib/incb 028050/ly3009104;baricitinib (ly3009104, incb028050);2-(3-(4-(3h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile
cas:	1187594-09-7
mf:	c16h17n7o2s
mw:	371.41688
einecs:	1592732-453-0
product categories:	inhibitor;jak/stat;inhibitors;api;jak;stat
mol file:	1187594-09-7.mol

baricitinib chemical properties

density

1.56

baricitinib usage and synthesis

description	baricitinib is known as 1-(ethylsulfonyl)-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]-3-azetidineacetonitrile chemically, which is a orally administrated inhibitor of janus kinase 1 and 2 (jak1/2) (a key enzyme involved in cytokine signaling, inflammation and immune function). it has certain anti-inflammatory, immunomodulating and antineoplastic activities. it takes effect through directly biding to jak1/2, inhibiting the jak1/2 activation and further inhibiting the jak-signal transducers and activators of transcription (stat) signaling pathway. as a consequence, the production of the inflammatory cytokines is reduced and the inflammatory response is inhibited. it can also induce apoptosis and inhibit the growth of related tumor cells. phase ii and phase iii have confirmed its efficacy for treatment of rheumatoid arthritis.
bioactivity	baricitinib (ly3009104, incb028050) is a selective jak1 and jak2 inhibitor with ic50 of 5.9 nm and 5.7 nm in cell-free assays, ~70 and ~10-fold selective versus jak3 and tyk2, no inhibition to c-met and chk2. phase 3.
in vitro	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 pbmcs. baricitinib also inhibits pstat3 stimulated by il-23 with ic50 od 20 nm in isolated naive t-cells.
in vivo	baricitinib inhibits il-6–stimulated phosphorylation of stat3 in whole blood with an ic50 of 128 nm. baricitinib (10 mg/kg p.o.) is expected to inhibit jak1/2 signaling (by ≥50%) in rats for about 8 hours. baricitinib (10 mg/ml, p.o.) inhibits disease scores in dose-dependent manner in rats with established disease in the adjuvant arthritis model. baricitinib treatment, compared with vehicle, inhibits the increase in hind paw volumes during the 2 weeks of treatment by 50% at a dose of 1 mg/kg and >95% at doses of 3 mg/kg or 10 mg/kg. baricitinib treatment, compared with vehicle, also inhibits composite score of immune infiltrate, edema, and periarticular tissue appearance by 27% at a dose of 1 mg/kg, 64% at doses of 3 mg/kg and 82% at doses of 10 mg/kg in rats with established disease in the adjuvant arthritis model. baricitinib reduces bone resorption by 15%, 61%, and 67% with increasing dose level (1, 3, and 10 mg/kg) in rats with established disease in the adjuvant arthritis model. baricitinib (10 mg/kg, daily for 2 wk, p.o.) results in radiographic improvements with restoration of the normal architecture and appearance to the ankle and tarsals in rats with established disease in the adjuvant arthritis model. baricitinib reduces levels of pstat3 in a dose-and time-dependent manner in the peripheral blood of raia animals. baricitinib (10 mg/ml, p.o.) improves a composite score of joint damage by 47% in the murine cia model. baricitinib (10 mg/kg) reduces pannus (74%) and bone damage (78%) and improves cartilage damage (43%) and signs of inflammation (33%), resulting in a 53% improvement in an aggregate score of disease in the collagen ab-induced arthritis (caia) murine model. baricitinib (10 mg/kg) inhibits the delayed-type hypersensitivity response by 48% in both the cia and caia models. baricitinib is efficacious in active rheumatoid arthritis patients refractory to disease modifying drugs and biologics. 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. [3] baricitinib has the dose-limiting side-effect of inducing anaemia which has been attributed to its effects on jak2 but has clearly shown efficacy.

uses	baricitinib is a jak1 and jak2 inhibitor and have been used as a promising treatment for rheumatoid arthritis.