GSK 269962 - CAS 850664-21-0
Catalog number: 850664-21-0
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C29H30N8O5
Molecular Weight:
570.60
COA:
Inquire
Targets:
ROCK
Description:
GSK 269962 is a potent ROCK inhibitor with IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively, which displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases. It may be used in OAB treatment. It has been shown to block the generation of inflammatory cytokines in lipopolysaccharide-stimulated monocytes and to induce vasorelaxation in preconstricted rat aorta (IC50 = 35 nM). It lowers blood pressure in a rat model of hypertension. It induced a reduction in blood pressure of approximately 10, 20, and 50 mm Hg at doses of 1, 3, and 30 mg/kg. It represent a novel class of ROCK inhibitors that have profound effects in the vasculature, which may enable us to further evaluate the potential beneficial effects of ROCK inhibition in animal models of cardiovascular as well as other chronic diseases.
Purity:
>99 %
Appearance:
Solid powder
Synonyms:
GSK269962A;N-[3-[[2-(4-Aminofurazan-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yl]oxy]phenyl]-4-[[2-(4-morpholinyl)ethyl]oxy]benzamide;Aminofurazanyl-azabenzimidazole 6n;N-[3-[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethylimidazo[4,5-c]pyridin-6-yl]oxyphenyl]-4-(2-morpholin-4-ylethoxy)benzamide
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
GSK 269962 may be used in OAB treatment. It represent a novel class of ROCK inhibitors.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams-Kilos
Density:
1.45±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
YOVNFNXUCOWYSG-UHFFFAOYSA-N
InChI:
InChI=1S/C29H30N8O5/c1-2-37-24-17-25(31-18-23(24)33-28(37)26-27(30)35-42-34-26)41-22-5-3-4-20(16-22)32-29(38)19-6-8-21(9-7-19)40-15-12-36-10-13-39-14-11-36/h3-9,16-18H,2,10-15H2,1H3,(H2,30,35)(H,32,38)
Canonical SMILES:
CCN1C2=CC(=NC=C2N=C1C3=NON=C3N)OC4=CC=CC(=C4)NC(=O)C5=CC=C(C=C5)OCCN6CCOCC6
1.The effect of combined treatment with a β
Wróbel A;Rechberger T Neurourol Urodyn. 2017 Mar;36(3):580-588. doi: 10.1002/nau.22978. Epub 2016 Feb 16.
AIMS: ;The objective of the study was to evaluate the efficacy and safety of the combined treatment with the β;3; AR agonist and ROCK inhibitor in the rat model of detrusor overactivity induced by retinyl acetate instillation.;METHODS: ;The ROCK inhibitor (GSK 269962) and/or the β;3; AR agonist (BRL 37344) were administered in single doses and a cystometry was carried out, along with a 24 hr measurement of cardiovascular parameters and diuresis.;RESULTS: ;The combined use of GSK 269962 and BRL 37344 in doses ineffective in monotherapies, ameliorated DO. An increase was found in voided volume, voiding efficiency, volume threshold, intercontraction interval, bladder compliance, and volume threshold to elicit nonvoiding contractions, accompanied by a decrease in basal pressure, threshold pressure, detrusor overactivity index, nonvoiding contractions amplitude, and frequency. The combination therapy in question proved to have no effect on micturition voiding pressure, post-void residual, bladder contraction duration, or relaxation time. A 24 hr observation of female rats who received GSK 269962 and/or BRL 37344 did not show any significant changes in urine production. BRL 37344 increased heart rate and blood pressure proportionately to the applied dose.
2.Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.
Doe C;Bentley R;Behm DJ;Lafferty R;Stavenger R;Jung D;Bamford M;Panchal T;Grygielko E;Wright LL;Smith GK;Chen Z;Webb C;Khandekar S;Yi T;Kirkpatrick R;Dul E;Jolivette L;Marino JP Jr;Willette R;Lee D;Hu E J Pharmacol Exp Ther. 2007 Jan;320(1):89-98. Epub 2006 Oct 3.
Increased Rho kinase (ROCK) activity contributes to smooth muscle contraction and regulates blood pressure homeostasis. We hypothesized that potent and selective ROCK inhibitors with novel structural motifs would help elucidate the functional role of ROCK and further explore the therapeutic potential of ROCK inhibition for hypertension. In this article, we characterized two aminofurazan-based inhibitors, GSK269962A [N-(3-{[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4, 5-c]pyridin-6-yl]oxy}phenyl)-4-{[2-(4-morpholinyl)ethyl]-oxy}benzamide] and SB-7720770-B [4-(7-{[(3S)-3-amino-1-pyrrolidinyl]carbonyl}-1-ethyl-1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine], as members of a novel class of compounds that potently inhibit ROCK enzymatic activity. GSK269962A and SB-772077-B have IC50 values of 1.6 and 5.6 nM toward recombinant human ROCK1, respectively. GSK269962A also exhibited more than 30-fold selectivity against a panel of serine/threonine kinases. In lipopolysaccharide-stimulated monocytes, these inhibitors blocked the generation of inflammatory cytokines, such as interleukin-6 and tumor necrosis factor-alpha. Furthermore, both SB-772077-B and GSK269962A induced vasorelaxation in preconstricted rat aorta with an IC50 of 39 and 35 nM, respectively.
3.The Influence of Maxacalcitol, Vitamin D3 Analog, on Detrusor Overactivity in Conscious Rats.
Wróbel A;Rechberger T Urology. 2016 Jul;93:224.e7-224.e15. doi: 10.1016/j.urology.2016.03.008. Epub 2016 Mar 23.
OBJECTIVES: ;To test the hypothesis that maxacalcitol, vitamin D3 analog, would ameliorate detrusor overactivity (DO) induced by retinyl acetate instillation; to test the outcome of the combined administration of maxacalcitol and the rho kinase inhibitor - GSK 269962, amlodipine besylate, or oxybutynin chloride in this model.;METHODS: ;The rats were treated with maxacalcitol for 14 days. Then, cystometric studies were performed during which the animals were administered test compounds.;RESULTS: ;Maxacalcitol in a dose of 30 but not 15 µg/kg/day induced reduction in DO index, non-voiding contractions frequency (FNVC), and amplitude (ANVC), while increasing volume threshold to elicit non-voiding contractions (VTNVC). The 14-day-long administration of maxacalcitol at a dose of 15 µg/kg/day to animals, followed by GSK 269962 at a single dose of 10 mg/kg, led to a statistically significant reduction of intercontraction interval and bladder compliance, and an increase in DO index, without any effect on ANVC, FNVC, and VTNVC. The assessment of the combined effect of maxacalcitol (15 µg/kg/day) and amlodipine besylate (0.25 mg/kg) demonstrated an increase in intercontraction interval, bladder compliance and VTNVC, with a decrease in FNVC.
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CAS 850664-21-0 GSK 269962

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