Formoterol-13C-d3 (hemifumarate)
目录号 : GC47369
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
Formoterol-13C-d3 is intended for use as an internal standard for the quantification of formoterol by GC- or LC-MS. Formoterol is a selective agonist of the β2-adrenergic receptor (β2-AR; Kis = 7.58 and 2,630 nM for β2- and β1-ARs, respectively).1 It is selective for β-ARs in isolated guinea pig trachea over those in atrial tissue (pD2s = 9.29 and 6.98, respectively) and has a long duration of action.2,1 Aerosolized formoterol (10 µg/ml, inhaled) prevents the late asthmatic response and eosinophil and macrophage infiltration in bronchoalveolar lavage fluid (BALF), and as well as reduces bronchial reactivity in a guinea pig model of allergic asthma induced by ovalbumin.3 Formulations containing formoterol have been used, alone and in combination with other compounds, in the treatment of chronic obstructive pulmonary disease and asthma.4,5,6
1.Anderson, G.P.Formoterol: Pharmacology, molecular basis of agonism, and mechanism of long duration of a highly potent and selective β2-adrenoceptor agonist bronchodilatorLife Sciences52(26)2145-2160(1993) 2.Decker, N., Quennedey, M.C., Rouot, B., et al.Effects of N-aralkyl substitution of β-agonists on α- and β-adrenoceptor subtypes: Pharmacological studies and binding assaysJ. Pharm. Pharmacol.34(2)107-112(1982) 3.Sugiyama, H., Okada, C., Bewtra, A.K., et al.The effect of formoterol on the late asthmatic phenomena in guinea pigsJ. Allergy Clin. Immunol.89(4)858-866(1992) 4.Decramer, M.L., Hanania, N.A., LÖtvall, J.O., et al.The safety of long-acting β2-agonists in the treatment of stable chronic obstructive pulmonary diseaseInt. J. Chron. Obstruct. Pulmon. Dis.853-64(2013) 5.Tashkin, D.P., and Ferguson, G.T.Combination bronchodilator therapy in the management of chronic obstructive pulmonary diseaseRespir. Res.14(1)49(2013) 6.Bush, A., and Saglani, S.Management of severe asthma in childrenLancet376(9743)814-825(2010)
| Cas No. | N/A | SDF | |
| Canonical SMILES | OC(C=C1)=C(NC([H])=O)C=C1[C@H](O)CN[C@@H](C)CC2=CC=C(O[13C]([2H])([2H])[2H])C=C2.OC(/C=C/C(O)=O)=O | ||
| 分子式 | C18[13C]H21D3N2O4.1/2C4H4O4 | 分子量 | 406.5 |
| 溶解度 | DMSO: 20 mg/ml,Methanol: 1 mg/ml,Water: Slightly 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.46 mL | 12.3001 mL | 24.6002 mL |
| 5 mM | 0.492 mL | 2.46 mL | 4.92 mL |
| 10 mM | 0.246 mL | 1.23 mL | 2.46 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。
[Aliskiren hemifumarate]
Dtsch Med Wochenschr 2008 Jun;133(24):1308-12.PMID:18465684DOI:10.1055/s-2008-1077232.
Aliskiren, a renin inhibitor, is the first in a new class of drugs interfering with the renin angiotensin system. Aliskiren was approved by the US Food and Drug Administration (FDA) in March 2007, and in Europe in August 2007 for the treatment of hypertension (marketed as Tekturna and Rasilez, respectively). Several clinical trials demonstrated effective blood pressure reduction due to aliskiren treatment. Whether aliskiren exhibits morbidity and mortality benefits for patients beyond its blood pressure reduction capability, can only be judged after realization of comparative long-term clinical trials. Furthermore, it remains to be seen, whether the use of aliskiren will be indicated for treatment of additional diseases, as it was the case for other inhibitors of the renin angiotensin system. In fact, recent and ongoing clinical trials regarding heart failure and diabetic nephropathy demonstrated first beneficial effects of aliskiren in these conditions (reduction of urinary albumin/creatinine-ratio and NTproBNP, respectively).
rac-4-[4-Cyano-2-(hy-droxy-meth-yl)phen-yl]-4-(4-fluoro-phen-yl)-4-hy-droxy-N,N-dimethyl-butanaminium hemifumarate
Acta Crystallogr Sect E Struct Rep Online 2011 Jan 8;67(Pt 2):o284.PMID:21522976DOI:10.1107/S1600536810054346.
In the title salt, C(20)H(24)FN(2)O(2) (+)·0.5C(4)H(2)O(4) (2-), the fumarate anion is located on an inversion centre. In the cation, the two benzene rings are nearly perpendicular to each other, making a dihedral angle of 87.41 (10)°. The cation is linked to the anion by a bifurcated N-H⋯O hydrogen bond. Classical O-H⋯O and weak C-H⋯F hydrogen bonding is also present in the crystal structure. Three C atoms of the N,N-dimethyl-butanaminium moiety are disordered over two sites with refined site occupancies of 0.466 (14) and 0.534 (14).
Aseptic gingivitis related to quetiapine hemifumarate
Pharmacopsychiatry 2013 Jan;46(1):39-40.PMID:22915485DOI:10.1055/s-0032-1321906.
Quetiapine hemifumarate (QF) is widely used in psychiatry and is associated with regularly occurring side effects such as dizziness and metabolic problems. Apart from these typical adverse events the agent has attracted attention for several rare phenomena (priapism, cholestasis, rhabdomyolysis) that indeed feature anecdotal character, but are nevertheless indispensable for a comprehensive understanding of the factual risk profile of quetiapine. We present the first report of aseptic gingivitis associated with QF in a patient with mental retardation.
Synthesis and characterization of high-purity N,N-dimethyltryptamine hemifumarate for human clinical trials
Drug Test Anal 2020 Oct;12(10):1483-1493.PMID:32608093DOI:10.1002/dta.2889.
Since 2006, there has been a resurgent interest in the pharmacology and therapeutics of psychedelic drugs. Psilocybin, the 4-phosphoryl ester of N,N-dimethyltryptamine (DMT), has been studied most often, but DMT itself is also appealing because of its brief but profound psychological effects and its presence as an endogenous substance in mammalian brain. Although there have been a few studies of ayahuasca, a DMT-containing water infusion, only one human study with pure DMT has been reported since the early 2000s. Newly planned clinical trials to assess the safety and efficacy of DMT in humans with major depressive disorders require high-purity water-soluble DMT for intravenous administration. Accordingly, we synthesized and characterized DMT hemifumarate for these upcoming studies. The synthetic approach of Speeter and Anthony was slightly modified to gain some efficiency in time. In particular, this is the first known report to use aluminum hydride, generated in situ from lithium aluminum hydride, to reduce the intermediate 2-(1H-indol-3-yl)-N,N-dimethyl-2-oxoacetamide to DMT. A quench protocol was developed to produce a good yield of exceptionally pure free base DMT upon workup, which was then converted to the hemifumarate salt. Analysis of the final product included differential scanning calorimetry, thermogravimetric analysis, gas chromatography-mass spectrometry (GC-MS), 1 H and 13 C nuclear magnetic resonance spectroscopy, high-performance liquid chromatography, residual solvent analysis by GC headspace sampling, X-ray powder diffraction analysis, and residual lithium analysis by inductively coupled plasma-mass spectrometry. The DMT hemifumarate was minimally 99.9% pure, with no significant impurities or residual solvents, thus meeting regulatory standards for administration to humans.
Discovery of the hemifumarate and (alpha-L-alanyloxy)methyl ether as prodrugs of an antirheumatic oxindole: prodrugs for the enolic OH group
J Med Chem 1996 Jan 5;39(1):10-8.PMID:8568796DOI:10.1021/jm950575k.
Ether, ester, and carbonate derivatives of the antirheumatic oxindole 1 were prepared and screened as potential prodrugs of 1. This effort led to the discovery of the (alpha-L-alanyloxy)-methyl ether and hemifumarate derivatives of 1 which deliver the drug efficiently into the circulation of test animals, are stable in the solid state, and possess good stability in solution at low pH as required to ensure gastric stability. Success in achieving acceptable bioavailabilities of 1 across species (rats, dogs, and monkeys) followed the inclusion of ionizable functionality within the promoiety to compensate for masking the polar enolic OH group of the free drug. However, the introduction of ionizable functionality was often associated with decreased stability, as demonstrated by the hemisuccinate, hemiadipate, hemisuberate, and alpha-amino ester derivatives of 1 which could not be isolated. A clear exception was the hemifumarate derivative of 1 which was not only isolable but actually more stable at neutral pH than the nonionizable ester analogues. The solution and solid state stability of the hemifumarate, together with its activity as a prodrug of 1, suggests that hemifumarate be considered as an alternative to hemisuccinate as a prodrug derivative for alcohols, particularly in situations where solution state stability is an issue.