GW788388 - 10mM in DMSO , CAS No.452342-67-5

CAS: 452342-67-5 Cat. No.: G408606 Fórmula: C₂₅H₂₃N₅O₂ Peso molecular: 425.48

GRADE & PURITY 10mM in DMSO

Synonyms

4-(4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)benzamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

Information

GW788388 is a potent and selective inhibitor ofALK5withIC50of 18 nM in a cell-free assay, also inhibitsTGF-βtype II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor.
In vitro

GW788388 shows anti-TGF-β activity with IC50 of 93 nM in cellular assay. GW788388 shows some inhibitory to activin type II receptor (ActRII) but no inhibitory to bone morphogenic protein (BMP) type II receptor. GW788388 shows no toxicity in Namru murine mammary gland (NMuMG), MDA-MB-231, renal cell carcinoma (RCC)4, and U2OS cells at 4 nM to 15 μM. GW788388 blocks TGF-β-induced Smad activation and target gene expression, while decreasing epithelial-mesenchymal transitions and fibrogenesis. GW788388 inhibits ALK5, ALK4, ALK7 and TGF-β-mediated growth arrest.

In vivo

GW788388 exhibits an adequate pharmacokinetic profile in rats (plasma clearance less than 40 mL/min/kg and half-life more than 2 hours). GW788388 significantly reduces the expression of collagen IA1 mRNA by 80% in a model of puromycin aminonucleoside-induced renal fibrosis at 10 mg/kg. GW788388 attenuates TGF-β signalling and effectively reduces hallmarks of fibrogenesis in mice suffering from late-stage diabetic nephropathy at 2 mg/kg. Treatment with GW788388 significantly attenuates systolic dysfunction in the myocardial infarction (MI) animals, together with the attenuation of the activated (phosphorylated) Smad2, α-smooth muscle actin, and collagen I in the noninfarct zone of MI rats. Cardiomyocyte hypertrophy in MI hearts is also attenuated by GW788388 inhibition. GW788388 reduces the fibrotic response in bleomycin-injected animals at 2 mg/kg.
Cell Data

cell lines：Human primary Schwann and schwannoma cells

Concentrations：4 nM - 15 μM

Incubation Time：72 hours

Powder Purity:≥99%

Specifications

Sinónimos

4-(4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)benzamide

Especificações e pureza

10mM in DMSO

Mecanismos bioquímicos e fisiológicos

GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM in a cell-free assay, also inhibits TGF-β type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

INHIBITOR

Nomes e identificadores

SMILES isoméricas

C1COCCC1NC(=O)C2=CC=C(C=C2)C3=NC=CC(=C3)C4=C(NN=C4)C5=CC=CC=N5

Peso molecular

425.48

Reaxy-Rn

25792837

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25792837&ln=

Alvos associados (humanos)

TGFBR1 Tchem TGF-beta receptor type-1 (2 Activities)

Discover Target: TGFBR1

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

Propriedades químicas e físicas

• Solubilidade: Solubility (25°C) In vitro DMSO: 48 mg/mL warmed with 50ºC Water: bath (201.51 mM); Water: Insoluble; Ethanol: Insoluble

Perguntas frequentes

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 452342-67-5, the molecular formula is C25H23N5O2, and the molecular weight is 425.48 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.