Benztropine-13C-d3 (mesylate)
(Synonyms: NSC 169913-13C-d3) 目录号 : GC46097
A neuropeptide with diverse biological activities
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
Benztropine-13C-d3 is intended for use as an internal standard for the quantification of benztropine by GC- or LC-MS. Benztropine is an antagonist of M1 muscarinic acetylcholine receptors (Ki = 0.59 nM in rat brain membranes).1 It is selective for M1 receptors over the serotonin transporter (Ki = 5,150 nM), however, it also binds to the dopamine transporter and inhibits dopamine reuptake (Kis = 237 and 130 nM, respectively).1,2,3 Benztropine also inhibits acid sphingomyelinase by 87% when used at a concentration of 10 mM.4 Formulations containing benztropine have been used in the management of Parkinson's disease symptoms such as involuntary tremor and dystonia.
|1. Zhang, Y., Joseph, D.B., Bowen, W.D., et al. Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues. J. Med. Chem. 44(23), 3937-3945 (2001).|2. Schmitt, K.C., Zhen, J., Kharkar, P., et al. Interaction of cocaine-, benztropine-, and GBR12909- like compounds with wildtype and mutant human dopamine transporters: Molecular features that differentially determine antagonist binding properties. J. Neurochem. 107(4), 928-940 (2008).|3. Ukairo, O.T., Bondi, C.D., Newman, A.H., et al. Recognition of benztropine by the dopamine transporter (DAT) differs from that of the classical dopamine uptake inhibitors cocaine, methylphenidate, and mazindol as a function of a DAT transmembrane 1 aspartic acid residue. J. Pharmacol. Exp. Ther. 314(2), 575-583 (2005).|4. Kornhuber, J., Muehlbacher, M., Trapp, S., et al. Identification of novel functional inhibitors of acid sphingomyelinase. PLoS One 6(8), 1-13 (2011).
| Cas No. | N/A | SDF | |
| 别名 | NSC 169913-13C-d3 | ||
| Canonical SMILES | [2H][13C]([2H])([2H])N1[C@@H]2C[C@@H](OC(C3=CC=CC=C3)C4=CC=CC=C4)C[C@H]1CC2.OS(C)(=O)=O | ||
| 分子式 | C20[13C]H22D3NO • CH3SO3H | 分子量 | 407.6 |
| 溶解度 | DMSO: soluble,Methanol: soluble | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4534 mL | 12.2669 mL | 24.5339 mL |
| 5 mM | 0.4907 mL | 2.4534 mL | 4.9068 mL |
| 10 mM | 0.2453 mL | 1.2267 mL | 2.4534 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。
Eribulin mesylate
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Eribulin mesylate, a nontaxane, completely synthetic microtubule inhibitor, has recently been approved by the U.S. Food and Drug Administration as third-line treatment of metastatic breast cancer refractory to anthracyclines and taxanes. Eribulin is a synthetic analogue of halichondrin B, which inhibits microtubule polymerization by a mechanism distinct from other available antitubulin agents. Eribulin significantly increased overall survival (OS; median OS for the eribulin-treated group was 13.1 months versus 10.6 months for the group treated by investigator's choice) in a heavily pretreated metastatic breast cancer population. Eribulin has a manageable side-effect profile, notably neutropenia and fatigue, and a relatively low incidence of peripheral neuropathy. The mechanism of action, pharmacokinetics, preclinical antitumor activity, and clinical trials of eribulin in the metastatic breast cancer setting are reviewed here.
A concise synthesis of l-gulose and its C-6 derivatives
Bioorg Med Chem 2022 Nov 1;73:117029.PMID:36174449DOI:10.1016/j.bmc.2022.117029.
A convenient route for the preparation of l-gulose and its C-6 derivatives starting from commercially available 2,3:5,6-diisopropylidene-d-mannofuranose via C-5 epimerization as the key step was developed. 1-O-Benzylation followed by regioselective hydrolysis of the 5,6-isopropylidene group furnished benzyl 2,3-isopropylidene-α-d-mannofuranoside, which was subjected upon regioselective one-pot 6-O-benzoylation and 5-O-mesylation, providing the corresponding 5-OMs-6-OBz derivative in excellent selectivity. Treatment of this mesylate compound with potassium t-butoxide to remove the benzoyl group followed by intramolecular SN2 inversion led to benzyl 5,6-anhydro-2,3-isopropylidene-β-l-gulofuranoside, which could undergo not only nucleophilic substitutions to open the epoxide ring to give various C-6 derivatives, but also acidic hydrolysis to yield 1,6-anhydro-β-l-gulopyranose for further transformation into l-gulopyranosyl pentaacetate.
Delivery of Dihydroergotamine mesylate to the Upper Nasal Space for the Acute Treatment of Migraine: Technology in Action
J Aerosol Med Pulm Drug Deliv 2022 Dec;35(6):321-332.PMID:36108289DOI:10.1089/jamp.2022.0005.
Oral tablets account for the majority of medications used to acutely treat migraine, but relief can be limited by their rates of dissolution and absorption. The nose is an attractive alternative route of drug delivery since it provides patient convenience of at-home use, gastrointestinal (GI) avoidance, and rapid absorption of drugs into systemic circulation because of its large surface area. However, the site of drug deposition within the nasal cavity should be considered since it can influence drug absorption. Traditional nasal devices have been shown to target drug delivery to the lower nasal space where epithelium is not best-suited for drug absorption and where there is an increased likelihood of drug clearance due to nasal drip, swallowing, or mucociliary clearance, potentially resulting in variable absorption and suboptimal efficacy. Alternatively, the upper nasal space (UNS) offers a permeable, richly vascularized epithelium with a decreased likelihood of drug loss or clearance due to the anatomy of this area. Traditional nasal pumps deposit <5% of active drug into the UNS because of the nasal cavity's complex architecture. A new technology, Precision Olfactory Delivery (POD®), is a handheld, manually actuated, propellant-powered, administration device that delivers drug specifically to the UNS. A dihydroergotamine (DHE) mesylate product, INP104, utilizes POD technology to deliver drug to the UNS for the acute treatment of migraine. Results from clinical studies of INP104 demonstrate a favorable pharmacokinetic profile, consistent and predictable dosing, rapid systemic levels known to be effective (similar to other DHE mesylate clinical programs), safety and tolerability on the upper nasal mucosa, and high patient acceptance. POD technology may have the potential to overcome the limitations of traditional nasal delivery systems, while utilizing the nasal delivery benefits of GI tract avoidance, rapid onset, patient convenience, and ease of use.
Eribulin mesylate (Halaven) for breast cancer
Med Lett Drugs Ther 2011 Apr 18;53(1362):30-1.PMID:21502935doi
Eribulin mesylate (Halaven-Eisai) has been approved by the FDA for treatment of patients with metastatic breast cancer who have previously received at least 2 chemotherapy regimens for metastatic cancer. Prior therapy should have included an anthracycline and a taxane in either an adjuvant or metastatic setting. Other drugs used to treat anthracycline- and taxane-refractory metastatic breast cancer include capecitabine (Xeloda), gemcitabine (Gemzar, and others) and vinorelbine (Navelbine, and others).
Determination of Methyl Methanesulfonate and Ethyl Methylsulfonate in New Drug for the Treatment of Fatty Liver Using Derivatization Followed by High-Performance Liquid Chromatography with Ultraviolet Detection
Molecules 2022 Mar 17;27(6):1950.PMID:35335314DOI:10.3390/molecules27061950.
A new derivatization high-performance liquid chromatography method with ultraviolet detection was developed and validated for the quantitative analysis of methanesulfonate genotoxic impurities in an innovative drug for the treatment of non-alcoholic fatty liver disease. In this study, sodium dibenzyldithiocarbamate was used as a derivatization reagent for the first time to enhance the sensitivity of the analysis, and NaOH aqueous solution was chosen as a pH regulator to avoid the interference of the drug matrix. Several key experimental parameters of the derivatization reaction were investigated and optimized. In addition, specificity, linearity, precision, stability, and accuracy were validated. The determined results of the samples were consistent with those obtained from the derivatization gas chromatography-mass spectrometry analysis. Thus, the proposed method is a reliable and practical protocol for the determination of trace methanesulfonate genotoxic impurities in drugs containing mesylate groups.