KC 12291 hydrochlorideOrally active atypical Na+ channel blocker; cardioprotective CAS# 181936-98-1 |
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| Cas No. | 181936-98-1 | SDF | Download SDF |
| PubChem ID | 22902387 | Appearance | Powder |
| Formula | C22H28ClN3O3S | M.Wt | 449.99 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 25 mM in water and to 50 mM in DMSO | ||
| Chemical Name | N-[2-(3,4-dimethoxyphenyl)ethyl]-N-methyl-3-[(5-phenyl-1,2,4-thiadiazol-3-yl)oxy]propan-1-amine;hydrochloride | ||
| SMILES | CN(CCCOC1=NSC(=N1)C2=CC=CC=C2)CCC3=CC(=C(C=C3)OC)OC.Cl | ||
| Standard InChIKey | KIJPRQYBNQKUAU-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C22H27N3O3S.ClH/c1-25(14-12-17-10-11-19(26-2)20(16-17)27-3)13-7-15-28-22-23-21(29-24-22)18-8-5-4-6-9-18;/h4-6,8-11,16H,7,12-15H2,1-3H3;1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Orally active atypical voltage-gated sodium channel blocker. Inhibits sustained sodium currents (INaL) and prevents diastolic contracture in isolated atria in vitro (IC50 values are 9.6 and 0.55 - 0.79 μM respectively). Displays anti-ischemic, bradycardic and cardioprotective activity in vivo. |
KC 12291 hydrochloride Dilution Calculator
KC 12291 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2223 mL | 11.1114 mL | 22.2227 mL | 44.4454 mL | 55.5568 mL |
| 5 mM | 0.4445 mL | 2.2223 mL | 4.4445 mL | 8.8891 mL | 11.1114 mL |
| 10 mM | 0.2222 mL | 1.1111 mL | 2.2223 mL | 4.4445 mL | 5.5557 mL |
| 50 mM | 0.0444 mL | 0.2222 mL | 0.4445 mL | 0.8889 mL | 1.1111 mL |
| 100 mM | 0.0222 mL | 0.1111 mL | 0.2222 mL | 0.4445 mL | 0.5556 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Pharmacological characterisation of sodium channels in sinoatrial node pacemaking in the rat heart.[Pubmed:16368090]
Eur J Pharmacol. 2006 Jan 20;530(3):243-9.
Blockade of sodium channels located in the sinoatrial node can slow diastolic depolarisation rate, recorded in vitro. The objective was therefore to determine whether these blockers could slow heart rate in vivo. The heart rate was firstly measured in spontaneously beating, isolated rat heart atria in the presence of different voltage gated sodium channel blockers. Tetrodotoxin and lidocaine slightly reduced heart rate whereas KC 12291 and R 56865, which mainly interact with the persistent component of the sodium current, concentration dependently and potently induced bradycardia. In the pithed rat, tetrodotoxin induced statistically significant decreases heart rate, maximal effects were: -32.2+/-6.1 beat per min. KC 12291 and R 56865 dose-dependently induced bradycardia (Delta heart rate obtained, -55.1+/-5.2 beat per min, P<0.05, and -71.9+/-8.5 bpm, P<0.05, respectively). In conclusion, voltage gated sodium channel blockers rather selective for the persistent current, exert a potent bradycardic effect in the rat.
KC 12291: an atypical sodium channel blocker with myocardial antiischemic properties.[Pubmed:14978516]
Cardiovasc Drug Rev. 2004 Spring;22(1):17-26.
KC 12291 was designed as a voltage-gated sodium channel (VGSC) blocker with cardioprotective properties. KC 12291 has moderate inhibitory effects on peak (or rapid) Na+ current, and markedly reduces sustained (or slowly or non-inactivating) Na+ current. This distinguishes KC 12291 from conventional VGSC blockers such as local anesthetics or antiarrhythmics, which have little or no cardioprotective properties. Since VGSCs represent the main pathway for ischemic Na+ loading by failing to inactivate fully, KC 12291 exerts pronounced antiischemic activity principally by reducing the amplitude of sustained Na+ current. In isolated atria and Langendorff-perfused hearts, KC 12291 inhibits diastolic contracture, renowned for its resistance to pharmacological inhibition, reduces ischemic Na+ loading and preserves cardiac energy status. KC 12291 exerts oral antiischemic activity in vivo in the absence of major hemodynamic effects. Cardiac VGSC blockers such as KC 12291, which block cardiac VGSCs in atypical fashion by effectively inhibiting the sustained component of Na+ current, represent, therefore, promising potential antiischemic and cardioprotective drugs.
Anti-ischemic compound KC 12291 prevents diastolic contracture in isolated atria by blockade of voltage-gated sodium channels.[Pubmed:12198320]
J Cardiovasc Pharmacol. 2002 Sep;40(3):346-55.
Several lines of evidence support a fundamental role for voltage-gated sodium channels in mediating ischemic Na rise. We examined the effect of the novel anti-ischemic compound KC 12291 on veratridine-stimulated and lysophosphatidylcholine (LPC)-induced sustained sodium current (I(NAL)) mediated by sodium channels in isolated myocytes obtained from guinea-pig atria, by using the whole-cell patch-clamp technique. We also analyzed the effect of KC 12291 on veratridine- and LPC-induced contractures in isolated guinea-pig atria. Veratridine as well as LPC increased I(NAL) measured at 20 ms of a 2 s pulse evoked from -100 to -30 mV (47.5 and 12 pA/pF in the presence of 40 microM veratridine and 10 microM LPC, respectively, vs. 6.7 pA/pF under control conditions). A significant reduction by KC 12291 in the quantity of charge carried by veratridine-stimulated I(NAL) in the range of test potentials between -50 mV and +10 mV was observed and similar effects were obtained on LPC-induced I(NAL). Thus, the quantity of charge carried by LPC-induced I(NAL) over a 2 s pulse to -30 mV was reduced by 48% in the presence of 10 microM KC 12291 vs. a reduction by 50% of veratridine-stimulated I(NAL) at the same test potential. Veratridine- and LPC-induced submaximal contractures in isolated atria were significantly inhibited by KC 12291 in a concentration-dependent manner, with an IC of 0.55 microM and 0.79 microM, respectively. The data indicate that veratridine- and LPC-induced increases in diastolic tension are inhibited by KC 12291 by a mechanism that involves blockade of voltage-gated sodium channels mediating sustained sodium current.
