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SKU | Size | Availability | Price | Qty |
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B127687-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $33.90 | |
B127687-10mg | 10mg | In stock | $51.90 | |
B127687-50mg | 50mg | In stock | $198.90 | |
B127687-250mg | 250mg | In stock | $893.90 | |
B127687-1g | 1g | In stock | $3,216.90 |
Highly potent JAK1 and JAK2 inhibitor; also inhibits JAK3 and Tyk2
Synonyms | Baricitinib|1187594-09-7|olumiant|INCB028050|LY3009104|INCB 028050|2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile|INCB-028050|UNII-ISP4442I3Y|LY-3009104|ISP4442I3Y|Baricitinib [USAN:INN]|1-(Ethylsulf |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | Highly potent JAK1 and JAK2 inhibitor (IC50values are 5.9 and 5.7 nM, respectively). Also inhibits Tyk2 (IC50= 53 nM). Displays >100-fold selectivity for JAK1/2 over JAK3 (IC50= 53 nM for JAK3). Binds AAK1, BIKE, GAK and MPSK1in vitro(Kdvalues are 17.2, 3 |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Tyrosine-protein kinase JAK2 inhibitor |
Note | 5mg、10mg卖完停产,不再备货 |
Product Description | Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. |
ALogP | -0.5 |
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Pubchem Sid | 488200979 |
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Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/488200979 |
IUPAC Name | 2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile |
INCHI | InChI=1S/C16H17N7O2S/c1-2-26(24,25)22-9-16(10-22,4-5-17)23-8-12(7-21-23)14-13-3-6-18-15(13)20-11-19-14/h3,6-8,11H,2,4,9-10H2,1H3,(H,18,19,20) |
InChi Key | XUZMWHLSFXCVMG-UHFFFAOYSA-N |
Canonical SMILES | CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3 |
Isomeric SMILES | CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3 |
PubChem CID | 44205240 |
Molecular Weight | 371.42 |
PubChem CID | 44205240 |
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ChEMBL Ligand | CHEMBL2105759 |
CAS Registry No. | 1187594-09-7 |
Wikipedia | Baricitinib |
RCSB PDB Ligand | 3JW |
Reactome Reaction | R-HSA-9678737, R-HSA-9678935, R-HSA-9678561, R-HSA-9679028 |
Reactome Drug | R-ALL-9678829 |
DrugCentral Ligand | 5202 |
PubChem SID | 488200979 |
Enter Lot Number to search for COA:
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Lot Number | Certificate Type | Date | Item |
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B1512012 | Certificate of Analysis | Apr 02, 2024 | B127687 |
G2304206 | Certificate of Analysis | May 31, 2023 | B127687 |
G2304222 | Certificate of Analysis | May 31, 2023 | B127687 |
G2304223 | Certificate of Analysis | May 31, 2023 | B127687 |
G2304224 | Certificate of Analysis | May 31, 2023 | B127687 |
G2304242 | Certificate of Analysis | May 31, 2023 | B127687 |
G2304250 | Certificate of Analysis | May 31, 2023 | B127687 |
G2304283 | Certificate of Analysis | May 31, 2023 | B127687 |
G2304287 | Certificate of Analysis | May 31, 2023 | B127687 |
G2304303 | Certificate of Analysis | May 31, 2023 | B127687 |
Solubility | Solvent:DMSO, Max Conc. mg/mL: 37.14, Max Conc. mM: 100 |
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Pictogram(s) | GHS08, GHS09, GHS07 |
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Signal | Danger |
Hazard Statements | H373:Causes damage to organs through prolonged or repeated exposure H411:Toxic to aquatic life with long lasting effects H302:Harmful if swallowed H360:May damage fertility or the unborn child |
Precautionary Statements | P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P270:Do not eat, drink or smoke when using this product. P391:Collect spillage. P330:Rinse mouth. P203:Obtain, read and follow all safety instructions before use. P301+P317:IF SWALLOWED: Get medical help. P318:if exposed or concerned, get medical advice. P319:Get medical help if you feel unwell. |
Starting at $70.90
1. Fridman JS, Scherle PA, Collins R, Burn TC, Li Y, Li J, Covington MB, Thomas B, Collier P, Favata MF et al.. (2010) Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050.. J Immunol, 184 (9): (5298-307). [PMID:20363976] |
2. Genovese MC, Kremer J, Zamani O, Ludivico C, Krogulec M, Xie L, Beattie SD, Koch AE, Cardillo TE, Rooney TP et al.. (2016) Baricitinib in Patients with Refractory Rheumatoid Arthritis.. N Engl J Med, 374 (13): (1243-52). [PMID:27028914] |
3. Kennedy Crispin M, Ko JM, Craiglow BG, Li S, Shankar G, Urban JR, Chen JC, Cerise JE, Jabbari A, Winge MC et al.. (2016) Safety and efficacy of the JAK inhibitor tofacitinib citrate in patients with alopecia areata.. JCI Insight, 1 (15): (e89776). [PMID:27699252] |
4. Mackay-Wiggan J, Jabbari A, Nguyen N, Cerise JE, Clark C, Ulerio G, Furniss M, Vaughan R, Christiano AM, Clynes R. (2016) Oral ruxolitinib induces hair regrowth in patients with moderate-to-severe alopecia areata.. JCI Insight, 1 (15): (e89790). [PMID:27699253] |
5. Xing L, Dai Z, Jabbari A, Cerise JE, Higgins CA, Gong W, de Jong A, Harel S, DeStefano GM, Rothman L et al.. (2014) Alopecia areata is driven by cytotoxic T lymphocytes and is reversed by JAK inhibition.. Nat Med, 20 (9): (1043-9). [PMID:25129481] |
6. Jabbari A, Dai Z, Xing L, Cerise JE, Ramot Y, Berkun Y, Sanchez GA, Goldbach-Mansky R, Christiano AM, Clynes R et al.. (2015) Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib.. EBioMedicine, 2 (4): (351-5). [PMID:26137574] |
7. Richardson P, Griffin I, Tucker C, Smith D, Oechsle O, Phelan A, Stebbing J. (2020) Baricitinib as potential treatment for 2019-nCoV acute respiratory disease.. Lancet, 395 (10223): (e30-e31). [PMID:32032529] |
8. Stebbing J, Phelan A, Griffin I, Tucker C, Oechsle O, Smith D, Richardson P. (2020) COVID-19: combining antiviral and anti-inflammatory treatments.. Lancet Infect Dis, 20 (4): (400-402). [PMID:32113509] |