Chlorthalidone - CAS 77-36-1
Catalog number: 77-36-1
Category: Inhibitor
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Molecular Formula:
C14H11ClN2O4S
Molecular Weight:
338.76
COA:
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Targets:
Na+/Cl- Cotransporter
Description:
Chlorthalidone is a nonthiazide diuretic that inhibits the Na+-Cl- cotransporter in the distal convoluted tubule of the kidney. It prevents reabsorption of sodium and chloride leading to a reduction in plasma volume and cardiac output. It also effectively inhibits the activity of most platelet carbonic anhydrase isozymes (IC50s = 2.8 nM - 11 µM), which has been attributed to the sustained vasodilator capability of this compound. It inhibits sodium ion transport across the renal tubular epithelium increasing the delivery of sodium to the distal renal tubule and indirectly increasing potassium excretion via the sodium-potassium exchange mechanism. It also promotes Ca++ reabsorption by an unknown mechanism. It may be a better drug in preventing cardiovascular events than hydrochlorothiazide. It has been used independently or in combination with other antihypertensive agents to lower arterial blood pressure, and also as an adjuvant to address edema caused by cardiac or renal disorders.
Purity:
>98%
Appearance:
White to Off-White Solid
Synonyms:
Phthalamudine;Chlorphthalidolone;Hygroton;Saluretin;2-Chloro-5-(1-hydroxy-3-oxo-2H-isoindol-1-yl)benzenesulfonamide;2-Chloro-5-(2,3-dihydro-1-hydroxy-3-oxo-1h-isoindol-1-yl)benzenesulfonamide;1-Keto-3-(3’-sulfamyl-4’-chlorophenyl)-3-hydroxyisoindoline;1-Oxo-3-(3-sulfamyl-4-chlorophenyl)-3-hydroxyisoindoline
Solubility:
DMSO: ≥ 41 mg/mL
Storage:
-20°C Freezer
MSDS:
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Application:
Chlorthalidone prevents reabsorption of sodium and chloride leading to a reduction in plasma volume and cardiac output. It also effectively inhibits the activity of most platelet carbonic anhydrase isozymes. It inhibits sodium ion transport across the renal tubular epithelium increasing the delivery of sodium to the distal renal tubule and indirectly increasing potassium excretion via the sodium-potassium exchange mechanism. It may be a better drug in preventing cardiovascular events than hydrochlorothiazide. It has been used independently or in combination with other antihypertensive agents to lower arterial blood pressure, and also as an adjuvant to address edema caused by cardiac or renal disorders.
Quality Standard:
EP standard
Shelf Life:
2 month in rt, long time
Quantity:
Kilogram to ton
Melting Point:
239 °C
Density:
1.601±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
JIVPVXMEBJLZRO-UHFFFAOYSA-N
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)
Canonical SMILES:
C1=CC=C2C(=C1)C(=O)NC2(C3=CC(=C(C=C3)Cl)S(=O)(=O)N)O
Current Developer:
Original research factory is Sanofi. It has been approved the listing.
1.The effects of genes implicated in cardiovascular disease on blood pressure response to treatment among treatment-naive hypertensive African Americans in the GenHAT study.
Do AN1, Lynch AI1, Claas SA1, Boerwinkle E2, Davis BR3, Ford CE3, Eckfeldt JH4, Tiwari HK5, Arnett DK1, Irvin MR1. J Hum Hypertens. 2016 Jan 21. doi: 10.1038/jhh.2015.121. [Epub ahead of print]
African Americans have the highest prevalence of hypertension in the United States. Blood pressure (BP) control is important to reduce cardiovascular disease-related morbidity and mortality in this ethnic group. Genetic variants have been found to be associated with BP response to treatment. Previous pharmacogenetic studies of BP response to treatment in African Americans suffer limitations of small sample size as well as a limited number of candidate genes, and often focused on one antihypertensive treatment. Using 1131 African-American treatment-naive participants from the Genetics of Hypertension Associated Treatment Study, we examined whether variants in 35 candidate genes might modulate BP response to four different antihypertensive medications, including an angiotensin-converting enzyme inhibitor (lisinopril), a calcium channel blocker (amlodipine), and an a-adrenergic blocker (doxazosin) as compared with a thiazide diuretic (chlorthalidone) after 6 months of follow-up.
2.Diuretics for Hypertension: A Review and Update.
Roush GC1, Sica DA2. Am J Hypertens. 2016 Apr 5. pii: hpw030. [Epub ahead of print]
This review and update focuses on the clinical features of hydrochlorothiazide (HCTZ), the thiazide-like agents chlorthalidone (CTDN) and indapamide (INDAP), potassium-sparing ENaC inhibitors and aldosterone receptor antagonists, and loop diuretics. Diuretics are the second most commonly prescribed class of antihypertensive medication, and thiazide-related diuretics have increased at a rate greater than that of antihypertensive medications as a whole. The latest hypertension guidelines have underscored the importance of diuretics for all patients, but particularly for those with salt-sensitive and resistant hypertension. HCTZ is 4.2-6.2 systolic mm Hg less potent than CTDN, angiotensin-converting enzyme inhibitors, beta blockers, and calcium channel blockers by 24-hour measurements and 5.1mm Hg systolic less potent than INDAP by office measurements. For reducing cardiovascular events (CVEs), HCTZ is less effective than enalapril and amlodipine in randomized trials, and, in network analysis of trials, it is less effective than CTDN and HCTZ-amiloride.
3.Diuretics in the treatment of hypertension.
Blowey DL1. Pediatr Nephrol. 2016 Mar 16. [Epub ahead of print]
Diuretics have long been used for the treatment of hypertension. Thiazide diuretics are the most commonly prescribed diuretics for hypertension, but other classes of diuretics may be useful in alternative circumstances. Although diuretics are no longer considered the preferred agent for treatment of hypertension in adults and children, they remain acceptable first-line options. Diuretics effectively decrease blood pressure in hypertensive patients, and in adults with hypertension reduce the risk of adverse cardiovascular outcomes. Because of varied pharmacokinetic and pharmacodynamic differences, chlorthalidone may be the preferred thiazide diuretic in the treatment of primary hypertension. Other types of diuretics (e.g., loop, potassium sparing) may be useful for the treatment of hypertension related to chronic kidney disease (CKD) and other varied conditions. Common side effects of thiazides are mostly dose-related and involve electrolyte and metabolic abnormalities.
4.Effectiveness of chlorthalidone/amiloride versus losartan in patients with stage I hypertension: results from the PREVER-treatment randomized trial.
Fuchs FD1, Scala LC, Vilela-Martin JF, de Mello RB, Mosele F, Whelton PK, Poli-de-Figueiredo CE, de Alencastro PR, E Silva RP, Gus M, Bortolotto LA, Schlatter R, Cesarino EJ, Castro I, Neto JA, Chaves H, Steffens AA, Alves JG, Brandão AA, de Sousa MR, Jar J Hypertens. 2016 Apr;34(4):798-806. doi: 10.1097/HJH.0000000000000837.
OBJECTIVES: To compare the blood pressure (BP)-lowering efficacy of a chlorthalidone/amiloride combination pill with losartan, during initial management of stage I hypertension.
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CAS 77-36-1 Chlorthalidone

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