Bioactivity | Hydrochlorothiazide-15N2,13C,d2 is 15N and deuterated labeled Hydrochlorothiazide (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3]. |
Invitro | 氢、碳和其他元素的稳定重同位素已被纳入药物分子中,主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注,因为它可能影响药物的药代动力学和代谢谱[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Hydrochlorothiazide-15N2,13C,d2 相关抗体: |
In Vivo | Hydrochlorothiazide (HCTZ; orally bygavage; 12.5 mg/kg/d; 8 weeks) has improved cardiac function, reduced cardiac interstitial fibrosis and collagen volume fraction, decreased expression of AT1, TGF-β and Smad2 in the cardiac tissues in adult male Sprague Dawley rats. In addition, hydrochlorothiazide reduces plasma angiotensin II and aldosterone levels. Furthermore, hydrochlorothiazide inhibits angiotensin II-induced TGF-β1 and Smad2 protein expression in the neonatal rat ventricular fibroblasts[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
CAS | 2140316-81-8 |
Formula | C613CH6D2ClN15N2O4S2 |
Molar Mass | 302.73 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [2]. Magdy M Abdelquader, et al. Inhibition of Co-Crystallization of Olmesartan Medoxomil and Hydrochlorothiazide for Enhanced Dissolution Rate in Their Fixed Dose Combination. AAPS PharmSciTech. 2018 Dec 17;20(1):3. [3]. Duarte, J.D. and R.M. Cooper-DeHoff, Mechanisms for blood pressure lowering and metabolic effects of thiazide and thiazide-like diuretics. Expert Rev Cardiovasc Ther, 2010. 8(6): p. 793-802. [4]. Jinghong Luo, et al. Hydrochlorothiazide modulates ischemic heart failure-induced cardiac remodeling via inhibiting angiotensin II type 1 receptor pathway in rats. Cardiovasc Ther. 2017 Apr;35(2). |