Delgocitinib

SKU: orb1308395

Description

Delgocitinib

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	1263774-59-9
MW	310.35
Purity	99.95%
Formula	C₁₆H₁₈N₆O
SMILES	C[C@H]1CN(C(=O)CC#N)[C@]11CCN(C1)c1ncnc2[nH]ccc12
Target	JAK,Tyrosine Kinases
Solubility	DMSO:240 mg/mL (773.32 mM)

Bioactivity

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Target IC50	JAK3:13 nM\|TYK2:58 nM\|JAK2:2.6 nM\|JAK1:2.8 nM
In Vivo	Delgocitinib (oral; mice) effectively suppresses inflammatory responses. Orally administered Delgocitinib 1 or 6 hours before IL-2 injection, Delgocitinib can reduc the production of IFN-γ, bu the efficacy of administration in the first 1 hour is higher than that of administration in the first 6 hours (ED50 = 0.24 vs. 1.3 mg/kg). Delgocitinib (oral; 0.1, 1, or 10 mg/kg; mouse) ameliorates rat collagen-induced arthritis model. Delgocitinib prevente the development of hind paw swelling and histological Changes in inflammatory cell infiltration and synoviocyte proliferation befor the onset of rat collagen-induced arthritis (administration starting on day 1). Delgocitinib reduced paw swelling in a dose-dependent manner afte the onset of rat collagen-induced arthritis (administration starting on day 15), with improvement in paw swelling noted as early a the second day after administration. These findings suggest that Delgocitinib has a Protective effect against joint inflammation and joint destruction. Read more...
In Vitro	In cytokine signaling assays, Delgocitinib demonstrates Inhibition of Stat protein phosphorylation induced by IL-2, IL-6, IL-23, GM-CSF, and IFN-α, with IC50 Values of 4 ± , 3 ± 4, 8 ± 1, 30 ± 2, and 1 ± nM. It concentration dependently suppresses IL-2-induced T cell proliferation IC50 8. ± .6 nM), exhibiting a potency comparable to Tofacitinib IC50 16 nM). in the enzymatic assays, Delgocitinib effective Inhibition of All JAK subtypes, with IC50 Values of 2. ± .6, 2. ± .2, 1 ± , and 5 ± nM for JAK1, JAK2, JAK3, and Tyk2, respectively Lineweaver-Burk plots display tha the Inhibition mode of Delgocitinib toward All JAKs is competitive with ATP (Ki: 2. ± .3, 1. ± .0, 5. ± .3 and 1 ± nM for JAK1, JAK2, JAK3 and Tyk2, respectively. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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TyrosineKinases, Tyrosine Kinases, Tyk2, Corectim, Corectim(Delgocitinib), Delgocitinib, Inhibitor, JAK, JAK1, JAK2, Janus kinase, JAK3, JTE052, JTE-052, JTE 052, inhibit

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Compound Identifiers

PubChem CID

50914062 ↗

Key Properties

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No computed properties available.

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CAS Number:	2064338-33-4
MW:	356.43
Formula:	C₁₈H₂₄N₆O₂

Delgocitinib

Description

Research Area

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Key Properties

Bioactivity

Storage & Handling

Alternative Names

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