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rac-Tolterodine-d14 (tartrate) Sale

(Synonyms: (rac)-PNU-200583-d14 tartrate) 目录号 : GC48478

An internal standard for the quantification of tolterodine

rac-Tolterodine-d14 (tartrate) Chemical Structure

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1mg
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产品描述

rac-Tolterodine-d14 is intended for use as an internal standard for the quantification of tolterodine by GC- or LC-MS. Tolterodine is an antagonist of muscarinic acetylcholine receptors (Kis = 1.4, 2.7, 3.6, 3.1, and 2.2 nM for M1-5 receptors, respectively).1 It reduces intracellular calcium mobilization induced by carbachol in bladder smooth muscle cells and submandibular gland cells isolated from cynomolgus monkeys (Kis = 3.16 and 2 nM, respectively).2 Tolterodine inhibits volume-induced bladder contractions and oxotremorine-induced salivation in rats (ID50s = 0.025 and 0.12 mg/kg, respectively).3 Formulations containing tolterodine have been used in the treatment of overactive bladder.

1.Jones, L.H., Randall, A., Napier, C., et al.Design and synthesis of a fluorescent muscarinic antagonistBioorg. Med. Chem. Lett.18(2)825-827(2008) 2.Kobayashi, S., Ikeda, K., and Miyata, K.Comparison of in vitro selectivity profiles of solifenacin succinate (YM905) and current antimuscarinic drugs in bladder and salivary glands: A Ca2+ mobilization study in monkey cellsLife Sci.74(7)843-853(2004) 3.McNamara, A., Pulido-Rios, M.T., Sweazey, S., et al.Pharmacological properties of TD-6301, a novel bladder selective muscarinic receptor antagonistEur. J. Pharmacol.605(1-3)145-152(2009)

Chemical Properties

Cas No. SDF
别名 (rac)-PNU-200583-d14 tartrate
Canonical SMILES [2H]C([2H])([2H])C(C([2H])([2H])[2H])([2H])N(C(C([2H])([2H])[2H])([2H])C([2H])([2H])[2H])CCC(C1=CC=CC=C1)C2=C(C=CC(C)=C2)O.OC(C(C(O)=O)O)C(O)=O
分子式 C22H17D14NO•C4H6O6 分子量 489.7
溶解度 DMSO: soluble,Methanol: soluble 储存条件 -20°C
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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。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.0421 mL 10.2103 mL 20.4207 mL
5 mM 0.4084 mL 2.0421 mL 4.0841 mL
10 mM 0.2042 mL 1.021 mL 2.0421 mL
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Research Update

Calcium tartrate gel

Anal Biochem 1989 May 15;179(1):86-9.PMID:2757203DOI:10.1016/0003-2697(89)90205-4.

A method for preparation of a gel for chromatography has been developed. The adsorbent is calcium tartrate treated with potassium phosphate. By changing the temperature of synthesis (10-65 degrees C) and concentration of the salts (calcium chloride and sodium potassium tartrate) from 0.3 to 3.0 M, we have been able to prepare adsorbent crystals of definite sizes in the range 35-200 microns. In all cases, for synthesis of adsorbent, the Ca2+/K+Na+ ratio was greater than 1. After treatment of calcium tartrate crystals with 0.075-1.5 M potassium phosphate at 80-100 degrees C and pH 8.5-9.0, an appropriate chromatographic adsorbent was prepared. The chromatographic properties of calcium tartrate gel have been studied. The adsorbent permits flow rates of 25-150 ml/h, depending on the particle size. The capacity of calcium tartrate gel for binding BSA, RNA, and DNA was similar to that of Tiselius' hydroxyapatite (A. Tiselius, S. Hjerten, O. Levin (1956) Arch. Biochem. Biophys. 65, 132-155). The spheric shape of gel particles permits uniform and compact packing of adsorbent under the conditions of column chromatography.

Investigation of radiation sensitivity of some tartrate compounds

Radiat Prot Dosimetry 2014 Jun;159(1-4):199-202.PMID:24736299DOI:10.1093/rpd/ncu119.

Potential electron spin resonance (ESR) dosimetric application of different compounds of sodium tartrate, such as sodium tartrate dihydrate, sodium bitartrate monohydrate and potassium sodium tartrate tetrahydrate, was investigated in the range of 0.74-25 Gy. While the radiation-induced intermediates produced in these compounds are similar, their radiation yields are different. It is found that the radiation yield of sodium tartrate dihydrate is higher than other compounds of sodium tartrates. Comparison of the radiation yields were also made between well-known samples of ammonium tartrate, alanine and lithium formate. It is found that the radiation yields of sodium tartrate dihydrate, sodium bitartrate monohydrate and potassium sodium tartrate tetrahydrate have the values of 1.22, 0.18 and 0.13, respectively.

Inhibitory effect of tartrate against phosphate-induced DJ-1 aggregation

Int J Biol Macromol 2018 Feb;107(Pt B):1650-1658.PMID:29030185DOI:10.1016/j.ijbiomac.2017.10.022.

The DJ-1 protein engages in diverse cellular and pathological processes, including tumorigenesis, apoptosis, sperm fertilization, and the progression of Parkinson's disease (PD). The functional dimeric form of DJ-1 transforms into non-functional filamentous aggregates in an inorganic phosphate (Pi)-dependent manner in vitro. Here, we demonstrated that Pi and reactive oxygen species (ROS) induce DJ-1 aggregation in Neuro2A and SH-SY5Y cells. Remarkably, tartrate treatment significantly reduced Pi- and ROS-induced DJ-1 aggregation and restored Pi- and ROS-provoked cell death using quantitative data as mean±standard deviation, and statistics. Mechanistically, tartrate prevented DJ-1 aggregation via occupying the Pi-binding site. These findings revealed an unexpected physiological role of tartrate in the maintenance of DJ-1 function, and thus, a potential use as an inhibitor of DJ-1 aggregation.

The L-tartrate/succinate antiporter TtdT (YgjE) of L-tartrate fermentation in Escherichia coli

J Bacteriol 2007 Mar;189(5):1597-603.PMID:17172328DOI:10.1128/JB.01402-06.

Escherichia coli ferments L-tartrate under anaerobic conditions in the presence of an additional electron donor to succinate. The carrier for L-tartrate uptake and succinate export and its relation to the general C(4)-dicarboxylate carriers DcuA, DcuB, and DcuC were studied. The secondary carrier TtdT, encoded by the ttdT (previously called ygjE) gene, is required for the uptake of L-tartrate. The ttdT gene is located downstream of the ttdA and ttdB genes, encoding the L-tartrate dehydratase TtdAB. Analysis of mRNA by reverse transcription-PCR showed that ttdA, ttdB, and ttdT are cotranscribed. Deletion of ttdT abolished growth by L-tartrate and degradation of L-tartrate completely. Bacteria containing TtdT catalyze L-tartrate or succinate uptake and specific heterologous L-tartrate/succinate antiporting. D-Tartrate is not a substrate for TtdT. TtdT operates preferentially in the direction of tartrate uptake and succinate excretion. The Dcu carriers do not support anaerobic growth on L-tartrate or L-tartrate transport. TtdT is related in sequence and function to CitT, which catalyzes heterologous citrate/succinate antiporting in citrate fermentation.

Anion composition of açaı́ extracts

J Agric Food Chem 2013 Jun 26;61(25):5928-35.PMID:23772604DOI:10.1021/jf4014185.

Many products labeled açaı́ are presently marketed as natural supplements with various claimed health benefits. Authentic açaı́ is expensive; as a result, numerous products labeled as containing açaı́ are being sold that actually contain little or no açaı́. Authentic açaı́ samples from Brazil and Florida as well as several reputed açaı́ products were analyzed by suppressed conductometric anion chromatography. Columns with different selectivities were used to obtain a complete separation of all anions. Tandem mass spectrometry was used for confirmation of the less common ions. Quinate, lactate, acetate, formate, galacturonate, chloride, sulfate, malate, oxalate, phosphate, citrate, isocitrate, and myo-inositol hexakisphosphate (phytate) were found. Only the Florida açaı́ had detectable levels of hexanoate. No açaı́ sample had any detectable levels of tartrate, which is present in abundance in grape juice, the most common adulterant. The highly characteristic anion profile and in particular the absence of tartrate can readily be used to identify authentic açaı́ products. Açaı́ from Florida had a 6 times greater level of phytate. The present analytical approach for phytate may be superior to extant methods.