Tyk2-IN-5 - 10mM in DMSO , CAS No.1797432-62-2

CAS: 1797432-62-2 Cat. No.: T656011 Summenformel: C₂₁H₁₉FN₈O₂ Molekulargewicht: 434.43 PubChem CID: 91809175

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

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

IC50& Target:Tyk2 JH2 0.086 nM (Ki) IFNα 25 nM (IC 50 )

Specifications

Spezifikationen & Reinheit

10mM in DMSO

Biochemische und physiologische Mechanismen

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 i

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Namen und Kennungen

• Isomere SMILES: CNC1=CC(=NN2C1=NC=C2C(=O)N[C@@H]3C[C@@H]3F)NC4=CC=CN(C4=O)C5=CC=CC=N5
• PubChem CID: 91809175
• Molekulargewicht: 434.43

Zugehörige Ziele (menschlich)

TYK2 Tclin Non-receptor tyrosine-protein kinase TYK2 (2 Activities)

Discover Target: TYK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Häufig gestellte Fragen

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1797432-62-2, the molecular formula is C21H19FN8O2, and the molecular weight is 434.43 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.