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| 25mg |
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Purity: ≥98%
Upadacitinib tartrate (formerly ABT494; ABT-494; rinvoq), the tartrate salt of Upadacitinib, is a novel, potent and selective Janus kinase (JAK) 1 inhibitor approved in 2019 for the treatment of rheumatoid arthritis. It inhibits JAK1 with an IC50 of 43 nM, and was developed for the treatment of several autoimmune disorders, e.g. rheumatoid arthritis. ABT-494 is approximately 74 fold selective for Jak1 over Jak2 in cellular assays dependent on specific, relevant cytokines. ABT-494 demonstrates efficacy in rat arthritis models. Preliminary evidence suggests that compared to tofacitinib, ABT-494 may spare Jak2 and Jak3 dependent signaling.
| ln Vitro |
Upadatinib tartrate tetrahydrate has been shown in biochemical testing to be 74 times more selective for JAK-1 than JAK-2 (which is involved in erythropoiesis) and 58 times more selective for JAK-1 than JAK-3 (which is involved in immune surveillance) [1].
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| ln Vivo |
In a rat arthritic model, upadacitinib tartrate tetrahydrate (0.1–10 mg/kg; oral gavage; twice daily for 10 days) has demonstrated effectiveness [3].
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| Animal Protocol |
Animal/Disease Models: Female Lewis rat (rat adjuvant-induced arthritis model) [3]
Doses: 0.1, 0.3, 1, 3, 10 mg/kg Route of Administration: po (oral gavage); twice a day for 10 days Experimental Results: Inhibition of disease pathology in adjuvant-induced arthritis in rats. |
| References |
[1]. Nakayamada S, et al. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Oct;30(5):407-419.
[2]. J. Voss, et al. THU0127 Pharmacodynamics of A Novel JAK1 Selective Inhibitor in Rat Arthritis and Anemia Models and in Healthy Human Subjects. doi 10.1136/annrheumdis-2014-eular.3823. [3]. Parmentier JM, et al. In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494). BMC Rheumatol. 2018 Aug 28;2:23. |
| CAS # |
1607431-21-9
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| Related CAS # |
Upadacitinib;1310726-60-3;Upadacitinib-15N,d2
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| SMILES |
O=C(N1C[C@@H](CC)[C@@H](C2=CN=C3C=NC(NC=C4)=C4N32)C1)NCC(F)(F)F.O=C(O)[C@H](O)[C@@H](O)C(O)=O
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| InChi Key |
WQDBPGWQDBPVQZ-NBCXFSEXSA-N
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| InChi Code |
InChI=1S/C17H19F3N6O.C4H6O6/c1-2-10-7-25(16(27)24-9-17(18,19)20)8-11(10)13-5-22-14-6-23-15-12(26(13)14)3-4-21-15;5-1(3(7)8)2(6)4(9)10/h3-6,10-11,21H,2,7-9H2,1H3,(H,24,27);1-2,5-6H,(H,7,8)(H,9,10)/t10-,11+;1-,2-/m11/s1
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| Chemical Name |
(3S,4R)-3-ethyl-4-(3H-imidazo(1,2-a)pyrrolo(2,3-e)pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide (2R,3R)-2,3-dihydroxybutanedioate
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| Synonyms |
ABT-494 tartrate; ABT 494 tartrate; ABT494; rinvoq
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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