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Cité dans 0 publications à comité de lecture couvrant la chromatographie, la synthèse organique et les réactions de couplage croisé.
Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 ( Tyk2 ) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a K i value of 0.086 nM for Tyk2 JH2 and an IC 50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis
In Vitro
Tyk2-IN-5 inhibits Jak1-3 with IC 50 values of >2 μM and displays the Jak1-3 dependent cellular activities of >12.5 μM (IC 50 values). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Tyk2-IN-5 (5, 10 mg/kg; p.o.; twice daily for 20 days) shows highly efficacious in a rat adjuvant arthritis model . Tyk2-IN-5 (1, 10 mg/kg; p.o.; single) inhibits IL-12/IL-18 induced IFNγ production in a dose-dependent manner . Tyk2-IN-5 (10 mg/kg; p.o.; single) shows a high oral exposure and bioavailability (114%) in rat . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Lewis male rats (rat adjuvant arthritis model) . Dosage: 5, 10 mg/kg Administration: Oral administration; twice daily for 20 days Result: Demonstrated full efficacy to prevent the rats′ paw from swelling. Animal Model: Lewis male rats (IL-12/IL-18-induced) . Dosage: 1, 10 mg/kg Administration: Oral administration; single Result: Inhibited IL-12/IL-18 induced IFNγ production by 45% and 77% at doses of 1 and 10 mg/kg, respectively. Animal Model: Lewis male rats, mouse . Dosage: 10 mg/kg Administration: Oral administration; single Result: 1.19 Pharmacokinetic Parameters of Tyk2-IN-5 in mouse and rat . PO (10 mg/kg) mouse rat C max (μM) 15 9.4 AUC 0-24 (μM•h) 19 57 CL (mL/min/kg) 16 7.8 F (%) 86 114
Form:Solid
IC50& Target:Tyk2 JH2 0.086 nM (Ki) IFNα 25 nM (IC 50 )
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<<<<<<< HEAD Télécharger la SDS → ======= Télécharger la SDS → >>>>>>> release248-p3Données qualité spécifiques au lot. Saisissez votre numéro de lot pour récupérer le COA exact.
Rechercher le COA →Résumé de référence rapide des spécifications et applications du produit.
Voir la fiche technique →Attributs de qualité complets et critères d'acceptation pour cette qualité.
Voir la fiche de spécifications →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organic acids and derivatives |
| Classe | Carboxylic acids and derivatives |
| Subclass | Carboxylic acid derivatives |
| Intermediate Tree Nodes | Carboxylic acid amides |
| Direct Parent | 2-heteroaryl carboxamides |
| Alternative Parents | Secondary alkylarylamines Pyridinones Aminopyridazines Aminopyridines and derivatives Carbonylimidazoles Dihydropyridines N-substituted imidazoles Imidolactams Heteroaromatic compounds Secondary carboxylic acid amides Amino acids and derivatives Lactams Azacyclic compounds Organic oxides Alkyl fluorides Organofluorides Organooxygen compounds Organopnictogen compounds Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | 2-heteroaryl carboxamide - Pyridinone - Aminopyridazine - Aminopyridine - Secondary aliphatic/aromatic amine - Imidazole-4-carbonyl group - Dihydropyridine - N-substituted imidazole - Pyridazine - Pyridine - Imidolactam - Hydropyridine - Azole - Imidazole - Heteroaromatic compound - Secondary carboxylic acid amide - Lactam - Amino acid or derivatives - Azacycle - Organoheterocyclic compound - Secondary amine - Organooxygen compound - Amine - Alkyl halide - Alkyl fluoride - Hydrocarbon derivative - Organic oxide - Organopnictogen compound - Organic oxygen compound - Organic nitrogen compound - Organonitrogen compound - Organohalogen compound - Organofluoride - Aromatic heteropolycyclic compound |
| Description | This compound belongs to the class of organic compounds known as 2-heteroaryl carboxamides. These are compounds containing a heteroaromatic ring that carries a carboxamide group. |
| External Descriptors | Not available |
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Solubilité | DMSO : 43.33 mg/mL (99.74 mM; Need ultrasonic) |
|---|---|
| Poids moléculaire | 434.400 g/mol |
| XLogP3 | 1.900 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 8 |
| Rotatable Bond Count | 6 |
| Exact Mass | 434.162 Da |
| Monoisotopic Mass | 434.162 Da |
| Topological Polar Surface Area | 117.000 Ų |
| Heavy Atom Count | 32 |
| Formal Charge | 0 |
| Complexity | 807.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 2 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
