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Purity: ≥98%
Delgocitinib (formerly LEO-124249; JTE052; LEO124249; JTE-052; Corectim) is a potent and selective JAK inhibitor with anti-inflammatory activities and has been approved in 2020 for use in Japan for the treatment of autoimmune disorders and hypersensitivity, including inflammatory skin conditions (e.g. atopic dermatitis). It inhibits JAK1, JAK2, JAK3 and Tyk2 with IC50s of 2.8, 2.6, 13 and 58 nM, respectively. JTE-052 reduces skin inflammation and ameliorates chronic dermatitis in Comparison with conventional therapeutic agents. JTE-052 regulates contact hypersensitivity by downmodulating T cell activation and differentiation.
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| ln Vitro |
Delgocitin potently inhibits all JAK subtypes in the enzymatic assays; the IC50 values for JAK1, JAK2, JAK3, and Tyk2 are 2.8±0.6, 2.6±0.2, 13±0, and 58±9 nM, respectively. Lineweaver-Burk plots demonstrate that dexgocitinib inhibits all JAKs in a competitive manner with ATP, with Ki values for JAK1, JAK2, JAK3, and Tyk2 being 2.1±0.3, 1.7±0.0, 5.5±0.3, and 14±1 nM, respectively. Delgocitinib had IC50 values of 40±9, 33±14, 84±11, 304±22, and 18±3 nM, respectively, to block the phosphorylation of Stat proteins produced by IL-2, IL-6, IL-23, GM-CSF, and IFN-α in these cell-based cytokine signaling tests. Similar in potency to CP-690550 (IC50=16 nM), delogocitinib likewise inhibits T cell proliferation caused by IL-2 in a concentration-dependent manner (IC50=8.9±3.6 nM)[1].
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| ln Vivo |
IFN-γ production is decreased by delognocitinib; however, the potency of the treatment one hour previously is greater than that of the administration six hours prior (ED50=0.24 versus 1.3 mg/kg). Delgocitinib, when taken as prescribed from day 1, inhibits the growth of edema in the hind paw as well as histological alterations such as synovial cell hyperplasia and inflammatory cell infiltration. Delgocitinib prevents bone and cartilage deterioration seen in radiography and histology. When administered starting on day 15, delocitinib reduces paw swelling in a way that is dose-dependent. Moreover, Delgocitinib reduces the degradation of cartilage and bone, hyperplasia of synovial cells, and infiltration of inflammatory cells in the histological and radiographic examinations at the conclusion of the study[1].
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| References |
[1]. Tanimoto A, et al. Pharmacological properties of JTE-052: a novel potent JAK inhibitor that suppresses various inflammatory responses in vitro and in vivo. Inflamm Res. 2015 Jan;64(1):41-51
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| Molecular Formula |
C16H18N6O
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| Molecular Weight |
310.35372209549
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| CAS # |
1263774-59-9
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| Related CAS # |
2064338-33-4 (EtOH);1263774-59-9 (free);2064338-35-6 (CHCl3);
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| SMILES |
N#CCC(N1C[C@H](C)[C@]12CN(C3=C4C(NC=C4)=NC=N3)CC2)=O
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| InChi Key |
LOWWYYZBZNSPDT-ZBEGNZNMSA-N
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| InChi Code |
InChI=1S/C16H18N6O/c1-11-8-22(13(23)2-5-17)16(11)4-7-21(9-16)15-12-3-6-18-14(12)19-10-20-15/h3,6,10-11H,2,4,7-9H2,1H3,(H,18,19,20)/t11-,16-/m0/s1
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| Chemical Name |
3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile
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| Synonyms |
LEO-124249 JTE-052 LEO 124249JTE 052LEO124249 JTE052
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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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| Solubility (In Vitro) |
DMSO : ≥ 58 mg/mL (~186.89 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.06 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.06 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (1.61 mM) (saturation unknown) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2222 mL | 16.1108 mL | 32.2217 mL | |
| 5 mM | 0.6444 mL | 3.2222 mL | 6.4443 mL | |
| 10 mM | 0.3222 mL | 1.6111 mL | 3.2222 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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