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SML0116

GW788388 Hydrate

Name: GW788388 Hydrate
Brand: SIGMA

≥98% (HPLC), TGFβ signalling inhibitor, powder

Synonym(s):

4-{4-[3-(Pyridin-2-yl)-1H-pyrazol-4-yl]-pyridin-2-yl}-N-(tetrahydro-2H-pyran-4-yl)benzamide hydrate

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About This Item

Empirical Formula (Hill Notation):

C₂₅H₂₃N₅O₂ · xH₂O

Molecular Weight:

425.48 (anhydrous basis)

UNSPSC Code:

12352200

PubChem Substance ID:

329825168

NACRES:

NA.77

MDL number:

MFCD20527321

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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Product Name

GW788388 Hydrate, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to tan

solubility

DMSO: ≥8 mg/mL

originator

GlaxoSmithKline

storage temp.

2-8°C

SMILES string

O.O=C(NC1CCOCC1)c2ccc(cc2)-c3cc(ccn3)-c4c[nH]nc4-c5ccccn5

InChI

1S/C25H23N5O2.H2O/c31-25(29-20-9-13-32-14-10-20)18-6-4-17(5-7-18)23-15-19(8-12-27-23)21-16-28-30-24(21)22-3-1-2-11-26-22;/h1-8,11-12,15-16,20H,9-10,13-14H2,(H,28,30)(H,29,31);1H2

InChI key

VZRJMBZMFKADGR-UHFFFAOYSA-N

Related Categories

Bioactive Small Molecule Inhibitors

Bioactive Small Molecules

Biochem/physiol Actions

GW788388 is a potent selective inhibitor of TGF-beta type I receptor [activin receptor-like kinase 5 (ALK5)]. GW788388 is orally available with a half-life of approximately 4 hours.

TGFβ1 (ALK5) inhibitor; Potent, selective inhibitor of TGFβ signalling in vitro and renal fibrosis in vivo

Features and Benefits

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

pictograms

GHS06,GHS09

signalword

Danger

hcodes

H301,H400

pcodes

P273 - P301 + P310 + P330

Hazard Classifications

Acute Tox. 3 Oral - Aquatic Acute 1

Storage Class

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Ochratoxin A induces epithelial-to-mesenchymal transition and renal fibrosis through TGF-β/Smad2/3 and Wnt1/β-catenin signaling pathways in vitro and in vivo.

Min Cheol Pyo et al.

Archives of toxicology, 94(9), 3329-3342 (2020-07-04)

Ochratoxin A (OTA) is a toxin produced by fungi such as Aspergillus spp. and Penicillium spp. The key target organ of OTA toxicity is the kidney, and it is known that epithelial-to-mesenchymal transition (EMT) leading to fibrosis is enhanced after

Effects of TGF-β1 Receptor Inhibitor GW788388 on the Epithelial to Mesenchymal Transition of Peritoneal Mesothelial Cells.

Yunmee Lho et al.

International journal of molecular sciences, 22(9) (2021-05-06)

We investigated the effectiveness of the transforming growth factor beta-1 (TGF-β) receptor inhibitor GW788388 on the epithelial to mesenchymal transition (EMT) using human peritoneal mesothelial cells (HPMCs) and examined the effectiveness of GW788388 on the peritoneal membrane using a peritoneal

Glucocorticoid Receptor Maintains Vasopressin Responses in Kidney Collecting Duct Cells.

Hsiu-Hui Yang et al.

Frontiers in physiology, 13, 816959-816959 (2022-06-11)

Water permeability of the kidney collecting ducts is regulated in part by the amount of the molecular water channel protein aquaporin-2 (AQP2), whose expression, in turn, is regulated by the pituitary peptide hormone vasopressin. We previously showed that stable glucocorticoid

Capturing time-dependent activation of genes and stress-response pathways using transcriptomics in iPSC-derived renal proximal tubule cells.

Paul Jennings et al.

Cell biology and toxicology (2023-01-01)

Transcriptomic analysis is a powerful method in the utilization of New Approach Methods (NAMs) for identifying mechanisms of toxicity and application to hazard characterization. With this regard, mapping toxicological events to time of exposure would be helpful to characterize early

Global Trade Item Number

SKU	GTIN
SML0116-5MG	04061833236550
SML0116-25MG	04061833236543

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