O-Desaryl ranolazine - CAS 172430-46-5
Catalog number:
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
O-Desaryl Ranolazine, a piperazine derivative, has been found to be a ranolazine metabolite which is a partial fatty acid oxidation inhibitor and could be used as an anti-myocardial ischemia agent.
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4-(2,3-Dihydroxypropyl)-N-(2,6-dimethylphenyl)-1-piperazineacetamide;CVT-2512;O-Desaryl Ranolazine;RS 88640
Store in a cool and dry place and at 0 - 4 °C for short term (days to weeks) or -20 °C for long term (months to years).
A metabolite of Ranolazine.
Quality Standard:
In-house standard
Canonical SMILES:
1.Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine.
Koltun DO1, Parkhill EQ1, Elzein E1, Kobayashi T1, Jiang RH1, Li X1, Perry TD1, Avila B1, Wang WQ2, Hirakawa R2, Smith-Maxwell C2, Wu L2, Dhalla AK2, Rajamani S2, Mollova N3, Stafford B3, Tang J3, Belardinelli L2, Zablocki JA1. Bioorg Med Chem Lett. 2016 Mar 26. pii: S0960-894X(16)30328-6. doi: 10.1016/j.bmcl.2016.03.096. [Epub ahead of print]
Previously we disclosed the discovery of potent Late INa current inhibitor 2 (GS-458967, IC50 of 333nM) that has a good separation of late versus peak Nav1.5 current, but did not have a favorable CNS safety window due to high brain penetration (3-fold higher partitioning into brain vs plasma) coupled with potent inhibition of brain sodium channel isoforms (Nav1.1, 1.2, 1.3). We increased the polar surface area from 50 to 84Å2 by adding a carbonyl to the core and an oxadiazole ring resulting in 3 GS-462808 that had lower brain penetration and serendipitously lower activity at the brain isoforms. Compound 3 has an improved CNS window (>20 rat and dog) relative to 2, and improved anti-ischemic potency relative to ranolazine. The development of 3 was not pursued due to liver lesions in 7day rat toxicology studies.
2.Pharmacokinetic drug-drug interaction study of ranolazine and metformin in subjects with type 2 diabetes mellitus.
Zack J1, Berg J2, Juan A3, Pannacciulli N1, Allard M1, Gottwald M1, Zhang H1, Shao Y1, Ben-Yehuda O4, Jochelson P1. Clin Pharmacol Drug Dev. 2015 Mar;4(2):121-9. doi: 10.1002/cpdd.174. Epub 2015 Jan 22.
Ranolazine and metformin may be frequently co-administered in subjects with chronic angina and co-morbid type 2 diabetes mellitus (T2DM). The potential for a drug-drug interaction was explored in two phase 1 clinical studies in subjects with T2DM to evaluate the pharmacokinetics and safety of metformin 1000 mg BID when administered with ranolazine 1000 mg BID (Study 1, N = 28) or ranolazine 500 mg BID (Study 2, N = 25) as compared to metformin alone. Co-administration of ranolazine 1000 mg BID with metformin 1000 mg BID resulted in 1.53- and 1.79-fold increases in steady-state metformin Cmax and AUCtau , respectively; co-administration of ranolazine 500 mg BID with metformin 1000 mg BID resulted in 1.22- and 1.37-fold increases in steady-state metformin Cmax and AUCtau , respectively. Co-administration of ranolazine and metformin was well tolerated in these T2DM subjects, with no serious adverse events or drug-related adverse events leading to discontinuation.
3.The combined effects of ranolazine and dronedarone on human atrial and ventricular electrophysiology.
Hartmann N1, Mason FE1, Braun I1, Pabel S1, Voigt N2, Schotola H3, Fischer TH1, Dobrev D2, Danner BC4, Renner A5, Gummert J5, Belardinelli L6, Frey N7, Maier LS8, Hasenfuss G9, Sossalla S10. J Mol Cell Cardiol. 2016 Apr 4;94:95-106. doi: 10.1016/j.yjmcc.2016.03.012. [Epub ahead of print]
INTRODUCTION: Pharmacological rhythm control of atrial fibrillation (AF) in patients with structural heart disease is limited. Ranolazine in combination with low dose dronedarone remarkably reduced AF-burden in the phase II HARMONY trial. We thus aimed to investigate the possible mechanisms underlying these results.
4.Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine.
Koltun DO1, Parkhill EQ1, Elzein E1, Kobayashi T1, Notte GT1, Kalla R1, Jiang RH1, Li X1, Perry TD1, Avila B1, Wang WQ2, Smith-Maxwell C2, Dhalla AK2, Rajamani S2, Stafford B3, Tang J3, Mollova N3, Belardinelli L2, Zablocki JA1. Bioorg Med Chem Lett. 2016 Mar 30. pii: S0960-894X(16)30331-6. doi: 10.1016/j.bmcl.2016.03.101. [Epub ahead of print]
We started with a medium throughput screen of heterocyclic compounds without basic amine groups to avoid hERG and β-blocker activity and identified [1,2,4]triazolo[4,3-a]pyridine as an early lead. Optimization of substituents for Late INa current inhibition and lack of Peak INa inhibition led to the discovery of 4h (GS-458967) with improved anti-arrhythmic activity relative to ranolazine. Unfortunately, 4h demonstrated use dependent block across the sodium isoforms including the central and peripheral nervous system isoforms that is consistent with its low therapeutic index (approximately 5-fold in rat, 3-fold in dog). Compound 4h represents our initial foray into a 2nd generation Late INa inhibitor program and is an important proof-of-concept compound. We will provide additional reports on addressing the CNS challenge in a follow-up communication.
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CAS 172430-46-5 O-Desaryl ranolazine

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