Adrenalone HCl
(Synonyms: 肾上腺酮盐酸盐) 目录号 : GC13814
Decoyinine (Angustmycin A), a specific inhibitor of bacterial GMPS, has been isolated from Streptomyces .
Cas No.:62-13-5
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
|
Cell lines |
SK-Mel-28 and SK-Mel103 cells |
|
Preparation Method |
Cells were incubated with 2 mM Decoyinine (Angustmycin A) for 24h before invasion assay. Where indicated, cells were supplemented with 100 µM guanosine. Control cells were treated with equal volumes of DMSO. Drug treatments were maintained throughout the experimental procedure. |
|
Reaction Conditions |
2 mM;24h |
|
Applications |
Treatment of SK-Mel-28 and SK-Mel103 cells with 2 mM of Decoyinine(Angustmycin A) reduced their invasion by ~30% compared with vehicle-treated cells. |
| Animal experiment [2]: | |
|
Animal models |
4-6-week-old female SCID mice |
|
Preparation Method |
SK-Mel-103 and SK-Mel-28 cells were inoculated into both flanks of SCID mice. When tumors reached 100 mm3 in size, mice were randomly assigned to different treatment groups and treated with daily i.p. injection of Decoyinine (Angustmycin A) (120 mg/kg in 10% DMSO in PBS), Mycophenolate Mofetil, or the correspondent vehicle control. |
|
Dosage form |
120 mg/kg; i.p., 10-27days |
|
Applications |
In SK-Mel-103 cells mcie, Decoyinine (Angustmycin A) treatment resulted in a 36% reduction of xenografts volume while MMF caused only 19% volume reduction. In SK-Mel-28 cells mcie, the xenograft volume reduction caused by Decoyinine (Angustmycin A) and MMF were of 62% and 30%, respectively. |
|
References: [1]. Bianchi-Smiraglia A, Wawrzyniak JA, et,al.Pharmacological targeting of guanosine monophosphate synthase suppresses melanoma cell invasion and tumorigenicity. Cell Death Differ. 2015 Nov;22(11):1858-64. doi: 10.1038/cdd.2015.47. Epub 2015 Apr 24. PMID: 25909885; PMCID: PMC4648332. | |
Decoyinine (Angustmycin A), a specific inhibitor of bacterial GMPS, has been isolated from Streptomyces hygroscopius as a potential antibiotic with sporulation-inducing activity in Bacillus subtilis[1-3]. Angustmycin A was also recently found to be a promising cytokinin that induces adventitious root or bud differentiation[5].
With 2 mM of Angustmycin A treatment of SK-Mel-28 and SK-Mel103 cells reduced their invasion by ~30% compared with vehicle-treated cells[4]. Decoyinine (Angustmycin A) (>1mM) enabled the S. griseus IFO 13189 cells to develop aerial mycelia in the suppressed cultures at concentrations which only partially inhibited growth[6].
Decoyinine (Angustmycin A)(120 mg/kg; i.p., 10days) treatment resulted in a 36% reduction of xenografts volume while MMF caused only 19% volume reduction in SK-Mel-103 mcie. In SK-Mel-28 mcie, the xenograft volume reduction caused by angustmycin A(120 mg/kg; i.p., 27days) and MMF were of 62% and 30%, respectively[4].
References:
[1]. Vasantha N, Freese E. Enzyme changes during Bacillus subtilis sporulation caused by deprivation of guanine nucleotides. J Bacteriol. 1980 Dec;144(3):1119-25. doi: 10.1128/jb.144.3.1119-1125.1980. PMID: 6777366; PMCID: PMC294778.
[2]. Ikehara K, Okamoto M, et,al. Induction of Bacillus subtilis sporulation by decoyinine and the concomitant disappearance of ppGpp in vegetative cells. J Biochem 1982; 91: 1089-1092.
[3]. Mitani T, Heinze JE, et,al. Induction of sporulation in Bacillus subtilis by decoyinine or hadacidin. Biochem Biophys Res Commun 1977; 77: 1118-1125.
[4]. Bianchi-Smiraglia A, Wawrzyniak JA, et,al.Pharmacological targeting of guanosine monophosphate synthase suppresses melanoma cell invasion and tumorigenicity. Cell Death Differ. 2015 Nov;22(11):1858-64. doi: 10.1038/cdd.2015.47. Epub 2015 Apr 24. PMID: 25909885; PMCID: PMC4648332.
[5]. Hong-Yuan, X., Hong-Zhang, X., et,al. in Biotechnology and Sustainable Agriculture 2006 and Beyond (eds. Xu, Z., Li, J., Xue, Y. & Yang, W.) 97-101 (Springer Netherlands, 2010).
[6]. Ochi K. Metabolic initiation of differentiation and secondary metabolism by Streptomyces griseus: significance of the stringent response (ppGpp) and GTP content in relation to A factor. J Bacteriol. 1987 Aug;169(8):3608-16. doi: 10.1128/jb.169.8.3608-3616.1987. PMID: 3112126; PMCID: PMC212439.
| Cas No. | 62-13-5 | SDF | |
| 别名 | 肾上腺酮盐酸盐 | ||
| 化学名 | 1-(3,4-dihydroxyphenyl)-2-(methylamino)ethanone;hydrochloride | ||
| Canonical SMILES | CNCC(=O)C1=CC(=C(C=C1)O)O.Cl | ||
| 分子式 | C9H11NO3.HCl | 分子量 | 217.65 |
| 溶解度 | ≥ 10.88mg/mL in DMSO | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 4.5945 mL | 22.9727 mL | 45.9453 mL |
| 5 mM | 0.9189 mL | 4.5945 mL | 9.1891 mL |
| 10 mM | 0.4595 mL | 2.2973 mL | 4.5945 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。
A comparative study between 0.5% centbucridine HCl and 2% lignocaine HCl with adrenaline (1:2,00,000)
Even today the ability to provide the patient with clinically adequate pain control with minimum systemic side effects is one of the major concerns all over the world. Lignocaine, the most commonly used local anesthetic agent in oral surgery due to its rapid onset & reasonably good potency, does not have adequate duration of action, unless used with Adrenaline, a drug known for its cardiovascular effects. Centbucridine, a non-ester, non-amide group local anesthetic agent developed in India at C D R I Lucknow, has advantage of inherent vasoconstrictor property. This study was planned to compare 0.5% Centbucridine and 2% Lignocaine with Adrenaline, in exodontia patients. The results were recorded for their efficacy and C V S action and statistically analyzed. Centbucridine was found to be an ideal local anesthetic agent with no effects on cardiovascular parameters and exhibiting a sufficient degree of local anesthetic activity suitable for use in routine minor surgery cases. This will be advantageous where Adrenaline is absolutely contraindicated due to systemic problems.
Anesthetic efficacy and safety of 2% lidocaine hydrochloride with 1:100,000 adrenaline and 4% articaine hydrochloride with 1:100,000 adrenaline as a single buccal injection in the extraction of maxillary premolars for orthodontic purposes
Background: Palatal injection of local anesthetics is the most painful injection. To obviate the need for palatal injections, local anesthetic agents with diffusibility are being investigated. Hence the present study was designed to analyze the anesthetic efficacy of 2% lidocaine hydrochloride (HCl) with 1:100,000 adrenaline and 4% articaine hydrochloride (HCl) with 1:100,000 adrenaline using single buccal infiltration for the extraction of maxillary premolars.
Methods: A prospective, double-blind, crossover, randomized clinical study was performed on 60 consecutive systemically healthy patients with an age range of 15-30 years, requiring extraction of asymptomatic bilateral maxillary premolars for orthodontic purposes. They received 1ml buccal infiltration of 4% articaine HCl with 1:100,000 adrenaline on one side and 2% lidocaine HCl with 1:100,000 adrenaline on the other side. The extraction procedure on either side was scheduled 14 days apart. Parameters assessed were the time of onset of anesthesia, intraoperative discomfort, hemodynamic parameters, and the duration of analgesia. Analysis of the data was done using the Mann-Whitney test, the Wilcoxon test, the Kruskal-Wallis ANOVA test, and the chi-square test. Statistical significance was established at P < 0.05.
Results: Articaine showed a faster time of onset and longer duration of analgesia than lidocaine. However, the difference in the intraoperative discomfort and hemodynamic parameters was statistically insignificant.
Conclusion: Within the limitations of the study, it can be concluded that the extraction of maxillary premolars can be performed with a single buccal infiltration of 2% lidocaine HCl with 1:100,000 adrenaline, which is one of the most commonly used local anesthetic agent.
The effects of formulation and addition of adrenaline to cocaine for haemostasis in intranasal surgery
Twenty patients presenting for submucous resection of the nasal septum under general anaesthesia were randomly allocated to four groups to receive either 1.0 ml 25% cocaine HCl in paraffin paste, 1.0 ml 25% cocaine HCl combined with 0.1% adrenaline in paraffin paste, 4.0 ml aqueous 4% cocaine HCl combined with 0.05% adrenaline or 4.0 ml aqueous 4% cocaine HCl on ribbon gauze applied to the nasal mucosa. Mean intraoperative blood loss was significantly decreased when the 25% cocaine 0.1% adrenaline combination in paraffin paste was used (11 (SD 8) ml, 60 (SD 30) ml, P less than 0.05, for adrenaline and plain paste respectively). Combination of adrenaline with cocaine in the aqueous formulation was not associated with a significant decrease in blood loss compared with aqueous cocaine alone (75 (SD 51), 96 (SD 66) ml respectively). Cocaine adrenaline paste and plain cocaine paste were associated with higher mean maximum cocaine blood concentrations (1.6 (SD 1.4), 2.0 (SD 1.5) micrograms/ml respectively) when compared with aqueous cocaine adrenaline and aqueous cocaine alone (0.03 (SD 0.003), 0.5 (SD 0.3) microgram/ml respectively). Heart rate and blood pressure changes were similar in all four groups and cardiovascular toxicity was not observed. One ml of topical intranasal 25% cocaine HCl with 0.1% adrenaline in paraffin paste provided the best haemostasis for nasal septal surgery.
[New anesthetics]
Since the introduction of cocaine local analgesia in 1886, and the subsequent development of procaine (1904) and other closely related ester-type compounds, dentistry has prided itself on being as close to 'painless' as possible. In the late 1940s the newest group of the local anesthetic compounds, the amides, was introduced. The initial amide local analgesic, lignocaine (Xylocaine), revolutionised pain control in dentistry worldwide. In succeeding years other amide-type local anesthetics, mepivacaine, prilocaine, bupivacaine and etidocaine, were introduced. They gave the dental practitioner a local anesthetic armamentarium which provided pulpal analgesia for periods of from 20 minutes (mepivacaine) to as long as three hours (bupivacaine and etidocaine with adrenaline). In addition these popular drugs proved to be more rapid-acting than the older ester-type drug and, at least from the perspective of allergenicity, more safe. In 1976, in Germany, the newest amide local analgesic, carticaine HCl was introduced into dentistry. Articaine (the generic name was changed) possesses properties similar to lignocaine but has additional properties which made the drug quite attractive to the general dental practitioner. In 1986 articaine was introduced in North America (Canada) where it has become the most used local anesthetic, supplanting lignocaine. Articaine has been approved for use in the United Kingdom. In this introductory discussion we review the development of articaine and discuss its place in the dental local analgesic armamentarium.
Comparative evaluation of hemodynamic, vasoconstrictive, and SpO2 variability during different stages of periodontal surgery performed using 0.5% ropivacaine or 2% lignocaine HCl (1:80,000 adrenaline) local anesthesia: A randomized, double-blind, split-mouth pilot study
Aim: The aim of this study is to compare anesthetic, hemodynamic, vasoconstrictive, and SpO2 variability of 0.5% ropivacaine to the "gold standard" lignocaine (2%) with epinephrine (1:80,000) during periodontal surgery.
Materials and methods: A total of 20 systemically healthy controls meeting the inclusion criteria were selected from the Outpatient Department of Sri Sai College of Dental Surgery. Preoperatively, all participants were infiltrated with 0.5 ml of 0.5% ropivacaine intradermally as test solution to record any allergic reaction. Open flap debridement was performed using local anesthesia containing 2% lignocaine hydrochloride with 1:80,000 epinephrine or 0.5% ropivacaine. Recordings were made of the time of onset, duration of action, the intensity, and depth of anesthesia and various hemodynamic changes throughout the surgical procedure. In addition, blood loss volume and postoperative pain were also assessed.
Results: Ropivacaine showed statistically longer duration of action (mean±SD =5.3±0.71 hrs) than lignocaine with epinephrine (mean=2.14±0.98 hrs). Blood loss during flap surgery was comparatively less when performed under ropivacaine. No statistical differences were observed in systolic BP, diastolic BP, SpO2 and heart rate during different stages of periodontal surgery between either of the local anesthetic agents.
Conclusion: Ropivacaine demonstrates comparable efficacy as lignocaine with added advantage of longer duration of action and superior postoperative pain control. No adverse events from this newer anesthetic were noted, and hence, it can be used safely as a viable local anesthetic for periodontal surgical procedures.