Amiodarone-d4 (hydrochloride)
(Synonyms: 盐酸胺碘酮-d4) 目录号 : GC46842
An internal standard for the quantification of amiodarone
Cas No.:1216715-80-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Amiodarone-d4 is intended for use as an internal standard for the quantification of amiodarone by GC- or LC-MS. Amiodarone is a class III antiarrhythmic agent, in that it prolongs both cardiac action potential and refractoriness by blocking potassium currents.1 It inhibits the voltage-gated potassium channel hERG, also known as KCNH2, with an IC50 value of 1 µM.2 In addition, amiodarone binds with high affinity to the sigma-1 opioid receptor, 3-β-hydroxysteroid δ8δ7 isomerase, and C-8 sterol isomerase (Kis = 1, 25, and 62 nM, respectively) and inhibits human thyroid hormone receptors α and β (IC50s = 0.6 and 0.65 µM, respectively).3,4 It also inhibits the cytochrome P450 (CYP) isoforms CYP2C8 and CYP3A4 in vitro at low micromolar concentrations.5
1.Campbell, T.J., and Williams, K.M.Therapeutic drug monitoring: Antiarrhythmic drugsBr. J. Clin. Pharmacol.52307-319(1998) 2.Sinha, N., and Sen, S.Predicting hERG activities of compounds from their 3D structures: Development and evaluation of a global descriptors based QSAR modelEur. J. Med. Chem.46(2)618-630(2011) 3.Laggner, C., Schieferer, C., Fiechtner, B., et al.Discovery of high-affinity ligands of σ1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screeningJ. Med Chem.48(15)4754-4764(2005) 4.Carlsson, B., Singh, B.N., Temciuc, M., et al.Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodaroneJournal of Medicinal Chemistry45(3)623-630(2002) 5.Polasek, T.M., Elliott, D.J., Lewis, B.C., et al.Mechanism-based inactivation of human cytochrome P4502C8 by drugs in vitroJ. Pharmacol. Exp. Ther.311(3)996-1007(2004)
| Cas No. | 1216715-80-8 | SDF | |
| 别名 | 盐酸胺碘酮-d4 | ||
| Canonical SMILES | CCCCc1oc2ccccc2c1C(=O)c1cc(I)c(OCCN(CC)CC)c(I)c1Cl | ||
| 分子式 | C25H25D4I2NO3.HCl | 分子量 | 685.8 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml,Ethanol: 5 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4582 mL | 7.2908 mL | 14.5815 mL |
| 5 mM | 0.2916 mL | 1.4582 mL | 2.9163 mL |
| 10 mM | 0.1458 mL | 0.7291 mL | 1.4582 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Nifekalant hydrochloride and Amiodarone hydrochloride Result in Similar Improvements for 24-Hour Survival in Cardiopulmonary Arrest Patients: The SOS-KANTO 2012 Study
J Cardiovasc Pharmacol 2015 Dec;66(6):600-9.PMID:26317166DOI:10.1097/FJC.0000000000000310.
Background: Amiodarone (AMD), nifekalant (NIF), and lidocaine (LID) hydrochlorides are widely used for ventricular tachycardia/fibrillation (VT/VF). This study retrospectively investigated the NIF potency and the differential effects of 2 initial AMD doses (≤150 mg or 300 mg) in the Japanese SOS-KANTO 2012 study population. Methods and results: From 16,164 out-of-hospital cardiac arrest cases, 500 adult patients using a single antiarrhythmic drug for shock-resistant VT/VF were enrolled and categorized into 4 groups (73 LID, 47 NIF, 173 AMD-≤150, and 207 AMD-300). Multivariate analyses evaluated the outcomes of NIF, AMD-≤150, or AMD-300 groups versus LID group. Odds ratios (ORs) for survival to admission were 3.21 [95% confidence interval (CI): 1.38-7.44, P < 0.01] in NIF and 3.09 (95% CI: 1.55-6.16, P < 0.01) in AMD-≤150 groups and significantly higher than those of the LID group. However, the OR was 1.78 (95% CI: 0.90-3.51, P = 0.10) in AMD-300 group and was not significant than LID group. ORs for 24-hour survival were 6.68 in NIF, 4.86 in AMD-≤150, and 2.97 in AMD-300, being significantly higher in these groups. Conclusions: NIF and AMD result in similar improvements for 24-hour survival in cardiopulmonary arrest patients, and this suggest the necessity of a randomized control study.
Nalfurafine hydrochloride, a κ-Opioid Receptor Agonist, Induces Melanophagy via PKA Inhibition in B16F1 Cells
Cells 2022 Dec 29;12(1):146.PMID:36611940DOI:10.3390/cells12010146.
Selective autophagy controls cellular homeostasis by degrading unnecessary or damaged cellular components. Melanosomes are specialized organelles that regulate the biogenesis, storage, and transport of melanin in melanocytes. However, the mechanisms underlying melanosomal autophagy, known as the melanophagy pathway, are poorly understood. To better understand the mechanism of melanophagy, we screened an endocrine-hormone chemical library and identified nalfurafine hydrochlorides, a κ-opioid receptor agonist, as a potent inducer of melanophagy. Treatment with nalfurafine hydrochloride increased autophagy and reduced melanin content in alpha-melanocyte-stimulating hormone (α-MSH)-treated cells. Furthermore, inhibition of autophagy blocked melanosomal degradation and reversed the nalfurafine hydrochloride-induced decrease in melanin content in α-MSH-treated cells. Consistently, treatment with other κ-opioid receptor agonists, such as MCOPPB or mianserin, inhibited excessive melanin production but induced autophagy in B16F1 cells. Furthermore, nalfurafine hydrochloride inhibited protein kinase A (PKA) activation, which was notably restored by forskolin, a PKA activator. Additionally, forskolin treatment further suppressed melanosomal degradation as well as the anti-pigmentation activity of nalfurafine hydrochloride in α-MSH-treated cells. Collectively, our data suggest that stimulation of κ-opioid receptors induces melanophagy by inhibiting PKA activation in α-MSH-treated B16F1 cells.
Antiparasitic activities of new lawsone Mannich bases
Arch Pharm (Weinheim) 2019 Nov;352(11):e1900128.PMID:31536649DOI:10.1002/ardp.201900128.
A series of new lawsone Mannich bases derived from salicylaldehydes or nitrofurfural were prepared and tested for their activities against Leishmania major, Toxoplasma gondii, and Trypanosoma brucei brucei parasites. The hydrochloride salts 5a and 6a of the Mannich bases 2a and 3a, derived from unsubstituted salicylaldehyde and long-chained alkyl amines, were selectively and strongly active against T. gondii cells and appear to be new promising drug candidates against this parasite. Compound 6a showed an even higher activity against T. gondii than the known lawsone Mannich base 1b. Compound 4a, derived from salicylaldehyde and 2-methylaminopyridine, was also distinctly active against T. gondii cells. The derivatives 3a (salicyl derivative), 3b (3,5-dichloro-2-hydroxyphenyl derivative), and 3d (5-nitrofuranyl derivative) as well as the hydrochlorides 6a and 6b were also efficacious against T. b. brucei cells with compounds 3a and 3b being more selective for T. b. brucei over Vero cells when compared with the known control compound 1b. The derivatives 5a, 5c, 6a, and 6c proved to be up to five times more active than 1b against L. major promastigotes and up to four times more efficacious against L. major amastigotes.
Iodine-Catalyzed Diazenylation with Arylhydrazine Hydrochlorides in Air
J Org Chem 2018 Apr 6;83(7):3537-3546.PMID:29486127DOI:10.1021/acs.joc.7b03149.
A mild approach to diazenylation of active methylene compounds and N-heterocyclic compounds with arylhydrazine hydrochlorides in the presence of iodine under basic aerobic conditions was developed. The reaction could be executed either under heating or in the presence of blue LED light, though the latter condition was found to be relatively efficient. Presumably, the aryldiazene produced by oxidation of arylhydrazine hydrochloride acts as a nitrogen scavenger of the radical intermediate generated from the active methylene compound in the presence of iodine to produce the diazo compounds. The scope and limitations of the protocol are presented.
Green Formation of Novel Pyridinyltriazole-Salicylidene Schiff Bases
Curr Org Synth 2019;16(2):309-313.PMID:31975681DOI:10.2174/1570179416666181207145951.
Aim and objective: In this work, water was used as solvent for the eco-friendly synthesis of imines under microwave irradiation. In the first step of the study, 5-pyridinyl-3-amino-1,2,4-triazole hydrochlorides were synthesized in the reaction of amino guanidine hydrochloride with different pyridine carboxylic acids under acid catalysis. A green method for 5-pyridinyl-3-amino-1,2,4-triazoles was developed with the assistance of microwave synthesis. In the second step, the eco-friendly synthesis of imines was achieved by reacting 5- pyridinyl-2H-1,2,4-triazol-3-amine hydrochlorides with salicylic aldehyde derivatives to produce 2-(5- pyridinyl-2H-1,2,4-triazol-3-ylimino)methyl)phenol imines. Materials and methods: Microwave experiments were done using a monomode Anton Paar Monowave 300 microwave reactor (2.45 GHz). Reaction temperatures were monitored by an IR sensor. Microwave experiments were carried out in sealed microwave process vials G10 with maximum reaction volume of 10 mL. Results: When alternative methods were used, it was impossible to obtain good yields from ethanol. Nevertheless, the use of water was successful for this reaction. After 1-h microwave irritation, a yellow solid was obtained in 82% yield. Conclusion: In this work an eco-friendly protocol for the synthesis of Schiff bases from 5-(pyridin-2-, 3- or 4- yl)-3-amino-1,2,4-triazoles and substituted salicylic aldehydes in water under microwave irradiation was developed. Under the found conditions the high yields for the products were achieved at short reaction time and with an easy isolation procedure.