Pimavanserin hemitartrate

(Synonyms: ACP-103 hemitartrate)
目录号: PL04099 纯度: ≥99%
Pimavanserin (ACP-103) hemitartrate 是一种有效的 5-HT 2A 受体反向激动剂,pIC50 和 pKi 值分别为8.73和9.3。
CAS No. :706782-28-7
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中文名称
Pimavanserin hemitartrate
中文别名
酒石酸匹莫范色林;哌马色林;匹莫范色林 L-酒石酸盐;匹莫范色林酒石酸盐;头孢噻呋
英文名称
Pimavanserin hemitartrate
英文别名
Pimavanserin Tartrate;Unii-na83F1sjsr;Pimavanserin hemitartrate
Cas No.
706782-28-7
分子式
C54H74F2N6O10
分子量
1005.20
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)
详情描述
Pimavanserin (ACP-103) hemitartrate 是一种有效的 5-HT 2A 受体反向激动剂,pIC50 和 pKi 值分别为8.73和9.3。
产品详情
Pimavanserin (ACP-103) hemitartrate 是一种有效的 5-HT 2A 受体反向激动剂,pIC50 和 pKi 值分别为8.73和9.3。
生物活性
Pimavanserin (ACP-103) hemitartrate is a potent 5-HT 2A receptor inverse agonist with pIC 50 and pK i of 8.73 and 9.3, respectively.
性状
Solid
IC50 & Target[1][2]
5-HT2A Receptor 8.73 (pIC50) 5-HT2A Receptor
体外研究(In Vitro)
Pimavanserin hemitartrate competitively antagonizes the binding of [H]ketanserin to heterologously expressed human 5-HT 2A receptors with a mean pKi of 9.3 in membranes and 9.70 in whole cells. Pimavanserin hemitartrate displays potent inverse agonist activity in the cell-based functional assay receptor selection and amplification technology (R-SAT), with a mean pIC50 of 8.7. Pimavanserin hemitartrate demonstrates lesser affinity (mean pKi of 8.80 in membranes and 8.00 in whole cells, as determined by radioligand binding) and potency as an inverse agonist (mean pIC50 7.1 in R-SAT) at human 5-HT 2C receptors, and lacks affinity and functional activity at 5-HT 2B receptors, dopamine D2 receptors, and other human monoaminergic receptors. has not independently confirmed the accura
体内研究(In Vivo)
Pimavanserin hemitartrate attenuates head-twitch behavior (3 mg/kg p.o.), and prepulse inhibition deficits (1-10 mg/kg s.c.) induced by the 5-HT2A receptor agonist in rats and reduces the hyperactivity induced in mice by the N-methyl-D-aspartate receptor noncompetitive antagonist, consistent with a 5-HT 2A receptor mechanism of action in vivo and antipsychotic-like efficacy. Pimavanserin hemitartrate demonstrates 42.6% oral bioavailability in rats. has not independently confirmed the accuracy of these methods. They are for reference only.
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]. Vanover KE, et al. Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP- 103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist. J Pharmacol Exp Ther. 2006 May;317(2):910-8.
溶解度数据
In Vitro: DMSO : ≥ 75 mg/mL (149.23 mM)H2O : 50 mg/mL (99.48 mM; Need ultrasonic)
搜索质检报告(COA)
[1]. Vanover KE, et al. Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP- 103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist. J Pharmacol Exp Ther. 2006 May;317(2):910-8.

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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