GDC-2394 - ≥99% , CAS No.2238822-07-4

CAS: 2238822-07-4 Cat. No.: G647065 Fórmula: C₂₀H₂₅N₅O₄S Peso molecular: 431.51

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Descripción general

GDC-2394 is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC 50 s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation.

In Vitro

GDC-2394 (20 μM; 30 min) inhibits NLRP3-induced apoptosis associated speck-like protein containing CARD (ASC) speck formation in THP-1 cells. GDC-2394 (1 nM-10 μM; 7 d) inhibits human macrophage IL-1β and IL-18 production after activation of the NLRP3 inflammasome. GDC-2394 (0-20 μM; 30 min) inhibits NLRP3-dependent caspase-1 activation (IC 50 =51 nM) in THP-1 cells, also inhibits NLRP3-dependent IL-1β release (IC 50 =63 nM) and NLRC4-dependent IL-1β release (IC 50 >20 μM) in mouse bone marrow-derived macrophages (mBMDMs). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GDC-2394 (compound 20) (1 mg/kg, 10 mg/kg; p.o.; single dose) inhibits production of IL-1β in an acute mouse peritonitis model . GDC-2394 (25 mg/kg; once daily for 7 d) reduces paw swelling and pain in a functional rat model of gouty arthritis . Preclinical PK of GDC-2394 . Species Mouse Rat Dog Cyno CL p (mL/min/kg) 10.1 1.3 11.7 4.1 V ss (L/kg) 0.72 0.29 0.67 0.18 T 1/2 (h) 1.2 4.4 0.99 0.89 %F (1 mg/kg) 80 33 78 53 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Acute mouse peritonitis model Dosage: 1 mg/kg and 10 mg/kg Administration: Oral gavage; 2 h later treated with 1.25 μg LPS (i.p.) followed by 1 mg monosodium urate crystals (i.p.) a further 2 h later. Result: Resulted in a dose-dependent decrease in peritoneal IL-1β concentrations after MSU treatment, and decreased the level of IL-1β by 66.8 and 81.3% at 1 and 10 mg/kg compared with the control. Animal Model: Functional rat model of gouty arthritis Dosage: 25 mg/kg Administration: Interventional injection; once daily for 7 days Result: Significantly inhibited knee swelling after 48 h.

Form:Solid

Specifications

Especificaciones y pureza

≥99%

Mecanismos bioquímicos y fisiológicos

GDC-2394 is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC 50 s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activatio

Condiciones de almacenamiento de almacenamiento

Store at -20°C

Enviado en

Ice chest + Ice pads

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

INHIBITOR

Pureza

≥99%

Nombres e identificadores

• Peso molecular: 431.51

Propiedades químicas y físicas

• Solubilidad: DMSO : 50 mg/mL (115.87 mM; ultrasonic and warming and heat to 60°C)

Preguntas frecuentes

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

The CAS Number is 2238822-07-4, the molecular formula is C20H25N5O4S, and the molecular weight is 431.51 g/mol.

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

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.