ChlorthalidoneCAS# 77-36-1 |
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| Cas No. | 77-36-1 | SDF | Download SDF |
| PubChem ID | 2732 | Appearance | Powder |
| Formula | C14H11ClN2O4S | M.Wt | 338.77 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 41 mg/mL (121.03 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-chloro-5-(1-hydroxy-3-oxo-2H-isoindol-1-yl)benzenesulfonamide | ||
| SMILES | C1=CC=C2C(=C1)C(=O)NC2(C3=CC(=C(C=C3)Cl)S(=O)(=O)N)O | ||
| Standard InChIKey | JIVPVXMEBJLZRO-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C14H11ClN2O4S/c15-11-6-5-8(7-12(11)22(16,20)21)14(19)10-4-2-1-3-9(10)13(18)17-14/h1-7,19H,(H,17,18)(H2,16,20,21) | ||
| 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 | Chlorthalidone is a thiazide-like diuretic used to treat hypertension.In Vivo:Chlorthalidone is a thiazide-like diuretic. After oral intake, peak serum concentrations are achieved in 2-6 hours. The half-life of Chlorthalidone is approximately 42 (range 29-55) hours, reaching 45-60 hours after long-term dosing. However, interindividual variability in the half-life of Chlorthalidone is wide. Chlorthalidone is excreted unchanged by the kidneys. The natriuretic effect of Chlorthalidone is maximal at 18 hours and lasts more than 48 hours. Comparing different doses of Chlorthalidone, it has been observed that 25 mg daily is nearly as effective as higher doses, but with less risk of hypokalemia[1]. Chlorthalidone reduces calcium oxalate calculous recurrence but magnesium hydroxide does not. The effectiveness of Chlorthalidone or magnesium hydroxide is examined in the prevention of recurrent calcium oxalate kidney calculi. In a double-blind random allocation design daily dosages of 25 or 50 mg. Chlorthalidone, 650 or 1,300 mg. magnesium hydroxide, or an identical placebo are administered. All groups showed significantly decreased calculous events compared to the pretreatment rates. During the trial 56.1 per cent fewer calculi than predicted developed in the placebo group (p less than 0.01), whereas the groups receiving low and high dosage magnesium hydroxide showed 73.9 and 62.3 per cent fewer calculi, respectively (p less than 0.001 and less than 0.01, respectively). Chlorthalidone treatment results in a 90.1 per cent decrease from predicted rates and both dosages yielded similar results. When the treatments are compared Chlorthalidone is significantly better than the placebo or magnesium hydroxide (p less than 0.01). The large decreases in calculous events seen when placebo or ineffective therapy is given underscore the positive treatment bias that occurs when historical controls are used and they demonstrate the need for proper experimental design[2]. References: | |||||
Chlorthalidone Dilution Calculator
Chlorthalidone Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.9519 mL | 14.7593 mL | 29.5186 mL | 59.0371 mL | 73.7964 mL |
| 5 mM | 0.5904 mL | 2.9519 mL | 5.9037 mL | 11.8074 mL | 14.7593 mL |
| 10 mM | 0.2952 mL | 1.4759 mL | 2.9519 mL | 5.9037 mL | 7.3796 mL |
| 50 mM | 0.059 mL | 0.2952 mL | 0.5904 mL | 1.1807 mL | 1.4759 mL |
| 100 mM | 0.0295 mL | 0.1476 mL | 0.2952 mL | 0.5904 mL | 0.738 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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Chlorthalidone is a thiazide-like diuretic used to treat hypertension.
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The simultaneous UPLC-MS/MS determination of emerging drug combination; candesartan and chlorthalidone in human plasma and its application.[Pubmed:28178366]
Biomed Chromatogr. 2017 Sep;31(9).
A novel, precise, sensitive and accurate ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method has been developed for the simultaneous determination of a novel drug combination, candesartan (CAN) and Chlorthalidone (CHL), in human plasma. Chromatographic separation was achieved on Waters Acquity UPLC BEH C18 (50 x 2.1 mm, 1.7 mum). Mobile phase consisting of 1 mm ammonium acetate in water-acetonitrile (20:80 v/v) was used. The total chromatographic runtime was 1.9 min with retention times for CAN and CHL at 0.7 and 1.1 min respectively. Ionization and detection of analytes and internal standards was performed on a triple quadrupole mass spectrometer, operating in the multiple reaction monitoring and negative ionization mode. Quantitation was done to monitor protonated precursor --> product ion transition of m/z 439.2 --> 309.0 for CAN, 337.0 --> 189.8 for CHL and 443.2 --> 312.1 for candesartan D4 and 341.0 --> 189.8 for Chlorthalidone D4. The method was validated over a wide dynamic concentration range of 2.0-540.0 ng/mL for candesartan and 1.0-180.0 ng/mL for Chlorthalidone. The validated method was successfully applied for the assay of CAN and CHL in healthy volunteers.
Pharmacokinetic-pharmacodynamic modeling of the antihypertensive interaction between azilsartan medoxomil and chlorthalidone in spontaneously hypertensive rats.[Pubmed:28190245]
Naunyn Schmiedebergs Arch Pharmacol. 2017 May;390(5):457-470.
A pharmacokinetic-pharmacodynamic (PK-PD) model was developed to describe the time course of blood pressure following oral administration of azilsartan medoxomil (AZM) and/or Chlorthalidone (CLT) in spontaneously hypertensive (SH) rats. The drug concentration and pharmacological effects, including systolic blood pressure (SBP) and diastolic blood pressure (DBP) were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS) and tail-cuff manometry, respectively. Sequential PK-PD analysis was performed, wherein the plasma concentration-time data was modeled by one compartmental analysis. Subsequently PD parameters were calculated to describe the time-concentration-response relationship using indirect response (IDR) PK-PD model. The combination of AZ and CLT had greater BP lowering effect compared to AZ or CLT alone, despite of no pharmacokinetic interaction between two drugs. These findings suggest synergistic antihypertensive pharmacodynamic interaction between AZ and CLT noncompetitively, which was simulated by inhibitory function of AZ and stimulatory function of CLT after concomitant administration of the two drugs. The present model was able to capture the turnover of blood pressure adequately at different time points at two different dose levels. The current PK-PD model was successfully utilized in the simulation of PD effect at a dose combination of 0.5 and 2.5 mg/kg for AZ and CLT, respectively. The developed preclinical PK-PD model may provide guidance in the optimization of dose ratio of individual drugs in the combined pharmacotherapy of AZ and CLT at clinical situations.
Chlorthalidone Plus Amiloride Reduces the Central Systolic Blood Pressure in Stage 1 Hypertension Patients.[Pubmed:28197292]
Cardiol Res. 2016 Dec;7(6):196-201.
BACKGROUND: Hypertension reduction strategies use blood pressure in the brachial artery as the primary endpoint. Individuals who achieve the target blood pressure reduction with antihypertensive treatment have residual cardiovascular risk attributed to the difference in pressure between the aorta and brachial artery. Antihypertensive treatment affects the intrinsic properties of the vascular wall and arterial stiffness markers and consequently the central pressure. Recent publications stress the importance of adequate control of the central compared to peripheral blood pressure. Related clinical implications suggest that individuals with normal peripheral but high central blood pressure should not receive antihypertensive drugs that act on the central pressure. Therefore, they are at greater cardiovascular risk. The aim of the study was to evaluate the effect of treatment with a thiazide diuretic versus losartan on the central blood pressure in stage 1 hypertensive patients. METHODS: Twenty-five patients were randomized to the Chlorthalidone 25 mg/amiloride 5 mg group (q.d.) and 25 patients received losartan 50 mg (b.i.d). The central systolic blood pressure (CSBP) and augmentation index (AIx 75) were assessed using applanation tonometry. The paired t-test was used to compare the systolic blood pressure (SBP), diastolic blood pressure (DBP), mean arterial pressure (MAP), pulse pressure (PP), CSBP and AIx 75 between the thiazide and losartan groups at baseline and after 6 months of treatment. RESULTS: Significant reductions in CSBP (123.3 +/- 14.2 vs. 113.4 +/- 111.4, P = 0.0103) and AIx 75 (87.7 +/- 9.6 vs. 83.8 +/- 8.9, P = 0.0289) were observed after 6 months of drug treatment with Chlorthalidone 25 mg/amiloride 5 mg (q.d.). The administration of losartan 50 mg (b.i.d) did not reduce the CSBP and there were insignificant changes in the AIx 75. CONCLUSIONS: Six-month treatment of Chlorthalidone/amiloride but not losartan reduces the CSBP and AIx 75 in adults with stage 1 hypertension.
Chlorthalidone Versus Amlodipine for Hypertension in Kidney Transplant Recipients Treated With Tacrolimus: A Randomized Crossover Trial.[Pubmed:28259499]
Am J Kidney Dis. 2017 Jun;69(6):796-804.
BACKGROUND: Chlorthalidone is a very effective antihypertensive drug, but it has not been studied prospectively in kidney transplant recipients with hypertension. Recent data indicate that calcineurin inhibitors activate the thiazide-sensitive sodium chloride cotransporter, providing further rationale to test thiazides in this population. STUDY DESIGN: Randomized noninferiority crossover trial (noninferiority margin, -2.8mmHg). SETTING & PARTICIPANTS: Hypertensive kidney transplant recipients using tacrolimus (median duration, 2.4 years after transplantation; mean estimated glomerular filtration rate, 63+/-27 [SD] mL/min/1.73m(2); mean systolic blood pressure [SBP], 151+/-12mmHg). INTERVENTION: Amlodipine (5-10mg) and Chlorthalidone (12.5-25mg) for 8 weeks (separated by 2-week washout). OUTCOMES: Average daytime (9 am to 9 pm) ambulatory SBP. MEASUREMENTS: Blood pressure and laboratory parameters. RESULTS: 88 patients underwent ambulatory blood pressure monitoring, of whom 49 (56%) with average daytime SBP>140mmHg were enrolled. 41 patients completed the study. Amlodipine and Chlorthalidone both reduced ambulatory SBP after 8 weeks (mean changes of 150+/-12 to 137+/-12 [SD] vs 151+/-12 to 141+/-13mmHg; effect size, -4.2 [95% CI, -7.3 to 1.1] mmHg). Despite these similar blood pressure responses, Chlorthalidone reduced proteinuria by 30% (effect size, -65 [95% CI, -108 to -35] mg/g) and also reduced physician-assessed peripheral edema (22% to 10%; P<0.05 for both). In contrast, Chlorthalidone temporarily reduced kidney function and increased both serum uric acid and glycated hemoglobin levels. LIMITATIONS: Open-label design, short follow-up, per-protocol analysis. CONCLUSIONS: Chlorthalidone is an antihypertensive drug equally effective as amlodipine after kidney transplantation.
