N-acetyl-L-Carnosine
(Synonyms: N-乙酰肌肽,N-Acetyl-L-carnosine) 目录号 : GC41368
A dipeptide with antioxidant and anticataract activities
Cas No.:56353-15-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
N-acetyl-L-Carnosine (NAC) is a natural imidazole-containing dipeptide that has antioxidant activities in cells, particularly against lipid peroxidation. Formulations containing NAC may prevent or resolve cataracts when added to the eyes of animals, presumably through the conversion of NAC to another antioxidant, carnosine. NAC and related dipeptides, delivered in specific formulations, may also have protective effects for skin.
| Cas No. | 56353-15-2 | SDF | |
| 别名 | N-乙酰肌肽,N-Acetyl-L-carnosine | ||
| Canonical SMILES | OC([C@@H](NC(CCNC(C)=O)=O)CC1=CN=CN1)=O | ||
| 分子式 | C11H16N4O4 | 分子量 | 268.3 |
| 溶解度 | DMSO: 0.5 mg/ml,PBS (pH 7.2): 10 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 | 3.7272 mL | 18.6359 mL | 37.2717 mL |
| 5 mM | 0.7454 mL | 3.7272 mL | 7.4543 mL |
| 10 mM | 0.3727 mL | 1.8636 mL | 3.7272 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。
Phytosome-hyaluronic acid systems for ocular delivery of L-carnosine
Int J Nanomedicine 2016 Jun 14;11:2815-27.PMID:27366062DOI:10.2147/IJN.S104774.
This study reports on L-carnosine phytosomes as an alternative for the prodrug N-acetyl-L-Carnosine as a novel delivery system to the lens. L-carnosine was loaded into lipid-based phytosomes and hyaluronic acid (HA)-dispersed phytosomes. L-carnosine-phospholipid complexes (PC) of different molar ratios, 1:1 and 1:2, were prepared by the solvent evaporation method. These complexes were characterized with thermal and spectral analyses. PC were dispersed in either phosphate buffered saline pH 7.4 or HA (0.1% w/v) in phosphate buffered saline to form phytosomes PC1:1, PC1:2, and PC1:2 HA, respectively. These phytosomal formulations were studied for size, zeta potential, morphology, contact angle, spreading coefficient, viscosity, ex vivo transcorneal permeation, and cytotoxicity using primary human corneal cells. L-carnosine-phospholipid formed a complex at a 1:2 molar ratio and phytosomes were in the size range of 380-450 nm, polydispersity index of 0.12-0.2. The viscosity of PC1:2 HA increased by 2.4 to 5-fold compared with HA solution and PC 1:2, respectively; significantly lower surface tension, contact angle, and greater spreading ability for phytosomes were also recorded. Ex vivo transcorneal permeation parameters showed significantly controlled corneal permeation of L-carnosine with the novel carrier systems without any significant impact on primary human corneal cell viability. Ex vivo porcine lenses incubated in high sugar media without and with L-carnosine showed concentration-dependent marked inhibition of lens brunescence indicative of the potential for delaying changes that underlie cataractogenesis that may be linked to diabetic processes.
Effects of N-acetyl-L-Carnosine aluminum (CL-1700) on various acute gastric lesions and gastric secretion in rats
Jpn J Pharmacol 1981 Dec;31(6):941-50.PMID:7334737DOI:10.1254/jjp.31.941.
Effects of a newly synthesized compound, N-acetyl-L-Carnosine aluminum (CL-1700), on the formation of various types of acute gastric lesions were studied in rats. CL-1700 at 300 or 1,000 mg/kg (p.o.) significantly inhibited Shay ulcers and water-immersion stress- and aspirin-induced erosions in pylorus-ligated rats, and indomethacin- or phenylbutazone-induced erosions. CL-1700 had a weak effect on water-immersion stress-induced erosions in rats with an intact pylorus. CL-1700 at 100 or 300 mg/kg (i.p.) significantly inhibited Shay ulcers and water-immersion stress-induced erosions in rats with an intact pylorus. However, this compound (i.p.) had no effect on aspirin- and indomethacin-induced gastric erosions. CL-1700 at 1,000 mg/kg (i.d.) significantly reduced the gastric acid output in pylorus-ligated rats but at 300 or 1,000 mg/kg (p.o.) increased the volume, pepsin output and raised the pH value. The effects of CL-1700 on experimental gastric lesions were slightly weaker than those of aluminum sucrose sulfate but almost equal to or better than those of cimetidine. However, the effects of CL-1700 were much more potent than those of gefarnate. As CL-1700 appears to be a promising new anti-gastric lesion agent, the mechanisms of action are now under investigation.
Sodium Sulfite-Induced Mast Cell Pyroptosis and Degranulation
J Agric Food Chem 2021 Jul 14;69(27):7755-7764.PMID:34191510DOI:10.1021/acs.jafc.1c02436.
Sodium sulfite, a common food additive, has been proved to cause allergic reaction. Pyroptosis is an inflammatory form of programmed cell death with plasma membrane lysis. In this study, we found that sodium sulfite triggered pyroptosis, which depended on reactive oxygen species (ROS)/NOD-like receptor protein 3 (NLRP3) in RBL-2H3 mast cells. Sodium sulfite increased the generation of ROS and the expression of NLRP3, caspase-1, gasdermin D N-terminal (GSDMD-N), interleukin-1β (IL-1β), and interleukin-18 (IL-18). The ROS scavenger N-acetyl-L-Carnosine (NAC) and the NLRP3 inhibitor MCC950 reversed these effects. Furthermore, using a lactate dehydrogenase kit, propidium iodide staining, scanning electron microscopy, colocalization of GSDMD-N with histamine, and neutral red staining, we found that sodium sulfite notably induced cell membrane rupture. Because β-Hexosaminidase and histamine play a key role in allergic reactions, we detected the release of β-Hexosaminidase and histamine. The data showed that the release of β-Hexosaminidase and histamine induced by sodium sulfite was increased with dose independence, which were inhibited after treatment with NAC or MCC950. Overall, evidence suggested that pyroptosis induced by sodium sulfite may rupture the cell membrane and result in degranulation of mast cells. Our study may provide new insights for the mechanism by which sodium sulfite induces mast cell death and sensitization.
Effectuation of loading a natural acetyl carnosine derivative within a promising cross-linked cyclodextrin spongey-like nanospheres on Physicochemical characterization and release behavior
Pak J Pharm Sci 2021 Jan;34(1(Supplementary)):283-290.PMID:34275852doi
This study centered on the ability of the cross-linked nano-sponge system to load the drug and to improve its physicochemical and dissolution properties. A spectrophotometric method was used to determine the wavelength of maximum absorbance of the drug. The ultrasonic-assisted synthesis method was used for nano-sponge preparation. Solution-state interactions, encapsulation efficiency and production yield, and in-vitro release were also investigated. Nano-sponges were characterized by Transmission Electron-Microscopy (TEM), Scanning Electron-Microscopy (SEM), Fourier Transform-Infrared Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), and X-Ray Diffractometry (X-RD) studies. The maximum absorption wavelength of N-acetyl-L-Carnosine was found to be at 210 nm. Solution-state interaction studies revealed a bathochromic shift. The production yield of nano-sponges ranged from 59.58% to 72.54%. In-vitro release study showed a sustained drug release for 228 hours. TEM images showed regular spherical shapes and sizes of nano-sponges. Their average particle size ranged from 28 nm to 79.2 nm. DSC data documented the drug-polymer interactions. FT-IR determined the presence of functional groups. X-RD showed the physicochemical characteristics of nano-sponges. Proving successful development of N-acetyl-L-Carnosine polymeric nano-sponge system with a suitable drug delivery over an extended period beside a noticeable improvement in the physicochemical characterization.
Dermal peptide delivery using enhancer molecules and colloidal carrier systems--part I: carnosine
Skin Pharmacol Physiol 2012;25(6):281-7.PMID:22890441DOI:10.1159/000341085.
Due to the lipophilic properties of the uppermost skin layer of the stratum corneum (SC), it is highly challenging to attain therapeutic concentrations of active substances; hydrophilic drugs, in particular, penetrate poorly. The purpose of this study was the improvement of the topical bioavailability of the hydrophilic dipeptides L-carnosine and its related compound N-acetyl-L-Carnosine. Different strategies were investigated. On the one hand, an enhancer molecule, 1,2-pentylene glycol (PG), was added to a standard preparation, and on the other hand, a microemulsion (ME-PG) system was developed. Both were compared to the standard formulation without an enhancer molecule. For all 3 preparations, the penetration of the peptides in ex vivo human skin was investigated. This allows statements to be made regarding dermal penetration, localization and distribution of the active substances in each skin layer as well as the influence of vehicle variations, in this case, the addition of PG or the incorporation of N-acetyl-L-Carnosine in an ME-PG system. For L-carnosine and N-acetyl-L-Carnosine, the use of the standard preparation with PG resulted in a significant increase of the substance within the SC. Approximately 6-fold and higher dipeptide concentrations in the SC and in the viable skin layers were detected at all experimental periods compared to the formulation without the enhancer molecule and the ME-PG. High concentrations of the compounds were found after a short period of time in the viable skin layers after applying the enhancer molecule, even in concentrations of 5%. The application of the colloidal carrier system did not lead to a higher penetration rate of N-acetyl-L-Carnosine in comparison to both standard preparations, although it must be said that the microstructure of the investigated ME-PG might not have been optimal for the hydrophilic properties of the dipeptide.