GW788388
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 401488

CAS#: 452342-67-5

Description: GW788388 is a new TGF-beta type I receptor inhibitor with a much improved pharmacokinetic profile compared with SB431542. We studied its effect in vitro and found that it inhibited both the TGF-beta type I and type II receptor kinase activities, but not that of the related bone morphogenic protein type II receptor. Further, it blocked TGF-beta-induced Smad activation and target gene expression, while decreasing epithelial-mesenchymal transitions and fibrogenesis.


Price and Availability

Size
Price

10mg
USD 150
100mg
USD 750
1g
USD 2450
Size
Price

25mg
USD 250
200mg
USD 1250
2g
USD 3750
Size
Price

50mg
USD 450
500mg
USD 1750
5g
Ask price

GW788388, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 200mg may be 2 weeks.


Chemical Structure

img

Theoretical Analysis

MedKoo Cat#: 401488
Name: GW788388
CAS#: 452342-67-5
Chemical Formula: C25H23N5O2
Exact Mass: 425.18518
Molecular Weight: 425.48242
Elemental Analysis: C, 70.57; H, 5.54; N, 16.46; O, 7.52


Synonym: GW788388; GW-788388; GW 788388

IUPAC/Chemical Name: 4-(4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)benzamide

InChi Key: SAGZIBJAQGBRQA-UHFFFAOYSA-N

InChi Code: InChI=1S/C25H23N5O2/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)

SMILES Code: O=C(NC1CCOCC1)C2=CC=C(C3=NC=CC(C4=CNN=C4C5=NC=CC=C5)=C3)C=C2


Technical Data

Appearance:
solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

 
 
 
 


References

1: Tan SM, Zhang Y, Connelly KA, Gilbert RE, Kelly DJ. Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. Am J Physiol Heart Circ Physiol. 2010 May;298(5):H1415-25. Epub 2010 Feb 12. PubMed PMID: 20154262.

2: Lagares D, García-Fernández RA, Jiménez CL, Magán-Marchal N, Busnadiego O, Lamas S, Rodríguez-Pascual F. Endothelin 1 contributes to the effect of transforming growth factor beta1 on wound repair and skin fibrosis. Arthritis Rheum. 2010 Mar;62(3):878-89. PubMed PMID: 20131241.

3: Noma K, Smalley KS, Lioni M, Naomoto Y, Tanaka N, El-Deiry W, King AJ, Nakagawa H, Herlyn M. The essential role of fibroblasts in esophageal squamous cell carcinoma-induced angiogenesis. Gastroenterology. 2008 Jun;134(7):1981-93. Epub 2008 Mar 4. PubMed PMID: 18439605; PubMed Central PMCID: PMC2562524.

4: Petersen M, Thorikay M, Deckers M, van Dinther M, Grygielko ET, Gellibert F, de Gouville AC, Huet S, ten Dijke P, Laping NJ. Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis. Kidney Int. 2008 Mar;73(6):705-15. Epub 2007 Dec 12. PubMed PMID: 18075500.

5: Frazier K, Thomas R, Scicchitano M, Mirabile R, Boyce R, Zimmerman D, Grygielko E, Nold J, DeGouville AC, Huet S, Laping N, Gellibert F. Inhibition of ALK5 signaling induces physeal dysplasia in rats. Toxicol Pathol. 2007 Feb;35(2):284-95. PubMed PMID: 17366323.

6: Gellibert F, de Gouville AC, Woolven J, Mathews N, Nguyen VL, Bertho-Ruault C, Patikis A, Grygielko ET, Laping NJ, Huet S. Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. J Med Chem. 2006 Apr 6;49(7):2210-21. PubMed PMID: 16570917.