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GSK269962A

Cat. No. M5168
GSK269962A Structure
Synonym:

GSK 269962

Size Price Availability Quantity
10mM/1mL USD 90  USD100 In stock
5mg USD 76.5  USD85 In stock
10mg USD 139.5  USD155 In stock
50mg USD 558  USD620 In stock
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Quality Control
Biological Activity

GSK269962A is a potent ROCK inhibitor with IC50 values of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2, respectively. GSK269962A displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases. GSK269962A induces vasorelaxation in preconstricted rat aorta (IC50 = 35 nM). GSK269962A induced a reduction in blood pressure of approximately 10, 20, and 50 mm Hg at doses of 1, 3, and 30 mg/kg. GSK269962A represents a novel class of ROCK inhibitors that have profound effects in the vasculature and may enable us to further evaluate the potential beneficial effects of ROCK inhibition in animal models of cardiovascular as well as other chronic diseases.

Product Citations
Customer Product Validations & Biological Datas
Source Clin Cancer Res (2018). Figure 5. ROCK inhibitor (Abmole Bioscience)
Method
Cell Lines CP50 PDX-O
Concentrations 10 μM
Incubation Time 30 to 45 minutes
Results Nuclear BRD4 expression increased significantly (p=0.008) as patients progressed from HSPC
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 570.6
Formula C29H30N8O5
CAS Number 850664-21-0
Purity 100.00%
Solubility DMSO 10 mM
Storage at -20°C
References

Lipopolysaccharide promotes contraction of uterine myocytes via activation of Rho/ROCK signaling pathways.
Hutchinson JL, et al. FASEB J. 2014 Jan;28(1):94-105. PMID: 24076962.

Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.
Doe C, et al. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98. PMID: 17018693.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK269962A, GSK 269962 supplier, ROCK, inhibitors

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