Lacidipine - CAS 103890-78-4
Catalog number:
103890-78-4
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C26H33NO6
Molecular Weight:
455.54
COA:
Inquire
Targets:
Calcium Channel
Description:
Lacidipine (Lacipil, Motens) is a L-type calcium channel blocker. Lacidipine (Lacipil, Motens) works by relaxing and opening up the blood vessels.
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Purity:
>98%
Synonyms:
GX-1048,GR-43659X,SN-305
MSDS:
Inquire
1. Inhibitors of transcription factor nuclear factor-kappa beta (NF-kb)-DNA binding
Rakesh Kumar Sharma,* Masami Otsuka, Garima Gabaa and Shilpa Mehta. RSC Adv., 2013, 3, 1282–1296
Using cultured Jurkat cells and EMSA, it was shown that chromium(VI) caused the induction of NF-kb. Reduction of Cr(VI) to lower oxidation states was required for Cr(VI)-induced NF-kb activation. Activation of NF-kB was decreased by diethylene triaminepentaacetic acid (DTPA). It significantly inhibits Cr(VI)-induced NF-kb activation by inhibiting .OH radical generation via chelation of Cr(V) and Cr(IV). Calcium chelators (e.g., EGTA, lacidipine) have been reported to inhibit H2O2 or stimulus-induced NF-kb activation. 1,3-dimethyl-2-thiourea (DMTU) prevents H2O2 generation and almost completely abolishes the enhanced NF-kb activity. Zinc chelators also exhibit an inhibitory effect on the DNA binding of NF-kb and/or homodimeric complexes of p50 and p65 subunits of NF-kb. Aurine tricarboxylic acid (ATA), which is a metal chelator consisting of dimethylaminopyridine and histidine, also inhibits the DNA-NF-kb binding at lower concentrations (500–1000 μm).
2. Interspecies prediction of oral pharmacokinetics of different lacidipine formulations from dogs to human: physiologically based pharmacokinetic modelling combined with biorelevant dissolution
Chunnuan Wu, Longfa Kou, Jin Sun*. RSC Adv.,2015, 5, 19844–19852
Three formulations of lacidipine were involved in this study. The two commercial formulations of lacidipine were formulation A LACIPIL® 4 mg tablet (GlaxoSmithKline, England) and formulation B Sileping™ 4 mg tablet (Harbin Pharmaceutical Group Sanchine Corporation, Harbin, China). Formulation C was lacidipine micronized tablet which was prepared by a wet granulation compression method after micronizing the APIs with air-flow crushing by jet mill.
3. The biorelevant concentration of Tween 80 solution is a simple alternative medium to simulated fasted state intestinal fluid
Bin Yang, Chunnuan Wu, Jin Sun*. RSC Adv.,2015, 5,104846–104853
Preparation of micronized tablets of lacidipine. Lacidipine was micronized with the air-flow crushing method by jet mill. Then the particle size distribution and the crystal form were investigated. The lacidipine micronized tablets were prepared by a wet granulation compression method.
4. One pot synthesis of acridine analogues from 1,2-diols as key reagents
Narasashetty Jagadishbabu and Kalegowda Shivashankar*. RSC Adv.,2015, 5,95240–95246
The synthesis of acridine derivatives, which contain 1,4-dihydropyridines parent nucleus is an important reaction, as these scaffolds are found to be a very important core in numerous synthetic, pharmaceutical and a wide variety of biologically active compounds. A large number of compounds bearing 1,4-dihydropyridines have entered preclinical and clinical trials over the last few years. Many commercially available drugs (Fig. 1) including nifedipine, clevidipine, lacidipine and nisoldipine (calcium channel blocker), nicardipine, manidipine and felodipine (antihypertensive compounds), amlodipine (used in coronary artery disease) are derived from 1,4-dihydropyridines core entities.
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CAS 103890-78-4 Lacidipine

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