Tandospirone citrate (Synonyms: 坦度螺酮柠檬酸盐; SM-3997 citrate)
目录号: PL05244 纯度: ≥99%
CAS No. :112457-95-1
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中文名称
Tandospirone citrate
中文别名
枸橼酸坦度螺酮;盐酸格拉司琼;坦度螺酮,柠檬酸D8;枸橼酸坦度螺酮杂质
英文名称
Tandospirone citrate
英文别名
Tandospirone Citrate;[14C]-Tandospirone citrate;4,7-Methano-1H-isoindole-1,3(2H)-dione, hexahydro-2-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-, (3aalpha,4beta,7beta,7aalpha)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1);SM-3997;SM 3997;Tandospirone citrate [USAN];metanopirone citrate;Sediel (TN);UNII-0R8E9BWM4J;tandospirone dihydrogen citrate;SureCN121034;AC1L1TH8;SM-3997 citrate;(3aR,4S,7R,7aS)-rel-Hexahydro-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-4,7-methano-1H-isoindole-1,3(2H)-dione 2-hydroxy-1,2,3-propanetricarboxylate (1:1);Sediel;Methanospirone;Tandopsirone citrate;(3aα,4β,7β,7aα)-Hexahydro-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-4,7-methano-1H-isoindole-1,3(2H)-dione·citric acid;3aalpha,4alpha,5,6,7alpha,7aalpha-Hexahydro-2-[4- [4-(2-pyriMidinyl)-1-piperazinyl]butyl]-4,7-Methano-1H-isoindole-1,3(2H)-dione dihydrogen citrate;4,7-Methano-1H-isoindole-1,3(2H)-dione, hexahydro-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-, (3aa,4b,7b,7aa)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1);4,7-Methano-1H-isoindole-1,3(2H)-dione, hexahydro-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-, (3aR,4S,7R,7aS)-rel-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) (9CI)
Cas No.
112457-95-1
分子式
C21H29N5O2.C6H8O7
分子量
575.61
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Tandospirone citrate (SM-3997 citrate) 是一种有效的,选择性5-HT1A 受体激动剂 (Ki = 27 nM) , 比作用于 SR-2, SR-1C, α1, α2, D1 和D2受体选择性高(Ki值为1300-41000 nM)。
生物活性
Tandospirone citrate is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM). IC50 Value: 27±5 nM(Ki) [1] Target: 5-HT1A in vitro: Tandospirone is most potent at the 5-HT1A receptor, displaying a Ki value of 27 +/- 5 nM. The agent is approximately two to three orders of magnitude less potent at 5-HT2, 5-HT1C, alpha 1-adrenergic, alpha 2-adrenergic, and dopamine D1 and D2 receptors (Ki values ranging from 1300 to 41000 nM). Tandospirone is essentially inactive at 5-HT1B receptors; 5-HT uptake sites; beta-adrenergic, muscarinic cholinergic, and benzodiazepine receptors [1]. 3H-SM-3997 bound rapidly, reversibly and in a saturable manner with high affinity to rat brain hippocampal membranes (Kd = 9.4 nM, Bmax = 213 fmol/mg protein) [2]. in vivo: Chronic treatment with tandospirone, at 0.2 and 1
性状
Solid
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. Hamik A, et al. Analysis of tandospirone (SM-3997) interactions with neurotransmitter receptor binding sites. Biol Psychiatry. 1990 Jul 15;28(2):99-109.
[2]. Shimizu H, et al. Characterization of the putative anxiolytic SM-3997 recognition sites in rat brain. Life Sci. 1988;42(24):2419-27.
[3]. Uehara T, et al.
溶解度数据
In Vitro: H2O : 10.4 mg/mL (18.07 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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