Pimavanserin hemitartrate | ACP-103 | 5-HT Receptor Inhibitor

Pimavanserin hemitartrate {[allProObj[0].p_purity_real_show]}

货号：A244461 同义名： ACP-103; Pimavanserin tartrate

Pimavanserin hemitartrate 是一种 5-HT2 受体拮抗剂，常用于帕金森病相关幻觉和精神病症状机制的研究。

Pimavanserin hemitartrate 化学结构
CAS号：706782-28-7

Pimavanserin hemitartrate 3D分子结构
CAS号：706782-28-7

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Pimavanserin hemitartrate 质控信息

5-羟色胺受体亚型比较

产品名称	5-HT ↓ ↑	5-HT1 ↓ ↑	5-HT2 ↓ ↑	5-HT3 ↓ ↑	5-HT5 ↓ ↑	5-HT6 ↓ ↑	5-HT7 ↓ ↑	其他靶点	纯度
Desvenlafaxine	++ 5-HT, Ki: 40.2 nM								98%
Lamotrigine	+ 5-HT (rat brain synaptosomes), IC50: 474 μM 5-HT (human platelets), IC50: 240 μM								98%
Venlafaxine	✔								99%
Fluvoxamine maleate	✔								99%
Iloperidone	✔								99%
Ziprasidone HCl	✔								98+%
Atomoxetine HCI	+ 5-HT, Ki: 77 nM								98%
Dapoxetine HCl	✔								97%
Trazodone	✔								98+%
Clomipramine HCl	✔								98%
Mirtazapine	✔								99+%
Escitalopram oxalate	+++ 5-HT, Ki: 0.89 nM								97%
Duloxetine	✔								97%
Sertraline HCl	++ 5-HT, Ki: 13 nM								98%
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								98%
Latrepirdine 2HCl	✔							GluR	99%
Fluoxetine HCl	✔								99.5%
Paroxetine HCl	✔							AChR	99%
BMY 7378		++ 5-HT1A, pIC50: 6.4 5-HT1D, pIC50: 5.9	+ 5-HT2, pIC50: 5.5						97%
Flibanserin		+++ 5-HT1A, Ki: 1 nM	+ 5-HT2A, Ki: 49 nM						95%
LY310762		+ 5-HT1D, Ki: 249 nM							99%+
Cyclobenzaprine HCI			✔						99%
Blonanserin			+++ 5-HT2, Ki: 3.98 nM						99%
Cyproheptadine HCl			++++ 5-HT2, IC50: 0.6 nM						99+%
Olanzapine			✔						99+%
Pimavanserin hemitartrate			+++ 5-HT2A, pIC50: 8.7						99%
Ketanserin			+++ 5-HT2C (Human), Ki: 2.5 nM 5-HT2C (Rat), Ki: 50 nM						99%+
Loxapine succinate			++ 5-HT2 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 nM						98%
Agomelatine			✔						98%
Clozapine			✔						98%
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	99%
PRX-08066 maleate			+++ 5-HT2B, IC50: 3.4 nM						98+%
RS-127445			++++ 5-HT2B, pKi: 9.5 5-HT2B, pIC50: 10.4						99%+
Sarpogrelate HCl			++++ 5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM						98%
Tropisetron				✔					99%
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					98%
Ondansetron				✔					99%
Granisetron				✔					98%
Alosetron HCl				✔					98%
Ondansetron HCl dihydrate				✔					98%
VUF10166				++++ 5-HT3AB, Ki: 22 nM 5-HT3A, Ki: 0.04 nM					99%+
Azasetron HCl				++++ 5-HT3, IC50: 0.33 nM					99%
Asenapine maleate		+++ 5-HT1A, pKi: 8.6 5-HT1B, pKi: 8.4	++++ 5-HT2A, pKi: 9.75 5-HT2C, pKi: 10.46		+++ 5-HT5A, pKi: 8.84	++++ 5-HT6, pKi: 9.6	++++ 5-HT7, pKi: 9.94		97%
Risperidone		++ 5-HT1B, Ki: 14.9 nM 5-HT1D, Ki: 84.6 nM	++++ 5-HT2A, Ki: 61.9 nM 5-HT2C, Ki: 12 nM		+ 5-HT5A, Ki: 206 nM		++ 5-HT7, Ki: 6.6 nM		98%
SB 271046 HCl						+++ 5-HT6, pKi: 8.92			99%+
Intepirdine						++++ 5-HT6, pKi: 9.63			99%+
SB-269970 HCl							++ 5-HT7, pKi: 8.3		98+%
BRL 15572		++ 5-HT1D, pKi: 6 5-HT1B, pKi: 6.1	++ 5-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2			+ 5-HT6, pKi: 5.9	+ 5-HT7, pKi: 6.3		95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Pimavanserin hemitartrate 生物活性

靶点

5-HT2

5-HT2A, pIC50:8.7

描述

Pimavanserin is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson's disease.

Pimavanserin hemitartrate 细胞实验

Cell Line MRC5 HPDE-6 PO2 PANC1 MIAPaCa2 BxPC3 AsPC1 PO2 MIAPaCa2 L3.6pl BxPC3 AsPC1 Brain bEND.3 endothelial cells 3D human liver spheroids	Concentration	Treated Time	Description	References
MRC5	5 μM	48 hours	PVT had minimal effects on normal cells	Mol Ther Oncolytics. 2020 Sep 2;19:19-32.
HPDE-6	5 μM	48 hours	PVT had minimal effects on normal cells	Mol Ther Oncolytics. 2020 Sep 2;19:19-32.
PO2	3-9 μM	24, 48, 72 hours	PVT significantly suppressed the proliferation of pancreatic cancer cells with IC50 ranging from 3 to 9 μM	Mol Ther Oncolytics. 2020 Sep 2;19:19-32.
PANC1	3-9 μM	24, 48, 72 hours	PVT significantly suppressed the proliferation of pancreatic cancer cells with IC50 ranging from 3 to 9 μM	Mol Ther Oncolytics. 2020 Sep 2;19:19-32.
MIAPaCa2	3-9 μM	24, 48, 72 hours	PVT significantly suppressed the proliferation of pancreatic cancer cells with IC50 ranging from 3 to 9 μM	Mol Ther Oncolytics. 2020 Sep 2;19:19-32.
BxPC3	3-9 μM	24, 48, 72 hours	PVT significantly suppressed the proliferation of pancreatic cancer cells with IC50 ranging from 3 to 9 μM	Mol Ther Oncolytics. 2020 Sep 2;19:19-32.
AsPC1	3-9 μM	24, 48, 72 hours	PVT significantly suppressed the proliferation of pancreatic cancer cells with IC50 ranging from 3 to 9 μM	Mol Ther Oncolytics. 2020 Sep 2;19:19-32.
PO2	7.5 µM	24 h	PVT significantly increased autophagy, as shown by a 2.5–5.0 fold increase in AO staining	Cancers (Basel). 2021 Nov 12;13(22):5661.
MIAPaCa2	7.5 µM	24 h	PVT significantly increased autophagy, as shown by a 2.5–5.0 fold increase in AO staining	Cancers (Basel). 2021 Nov 12;13(22):5661.
L3.6pl	7.5 µM	24 h	PVT significantly increased autophagy, as shown by a 2.5–5.0 fold increase in AO staining	Cancers (Basel). 2021 Nov 12;13(22):5661.
BxPC3	7.5 µM	24 h	PVT significantly increased autophagy, as shown by a 3.0 fold increase in AO staining	Cancers (Basel). 2021 Nov 12;13(22):5661.
AsPC1	7.5 µM	24 h	PVT significantly increased autophagy, as shown by a 3.0 fold increase in AO staining	Cancers (Basel). 2021 Nov 12;13(22):5661.
Brain bEND.3 endothelial cells	1 and 2 μM	6 hours	Pimavanserin significantly reversed the increased lactate dehydrogenase (LDH) release, declined cell viability, increased endothelial permeability, and downregulated Claudin 5 and Krüppel-like factors 6 (KLF6) observed in the OGD/R group.	Bioengineered. 2021 Dec;12(1):7481-7494.
3D human liver spheroids	1 μM	7 days	Pimavanserin reduced FFA-induced COL1A1 deposition, but its effect was less pronounced than that of ketanserin.	Sci Rep. 2024 Jan 16;14(1):1396.

Cell Line

Concentration

Treated Time

Description

References

MRC5

5 μM

48 hours

PVT had minimal effects on normal cells

Mol Ther Oncolytics. 2020 Sep 2;19:19-32.

HPDE-6

5 μM

48 hours

PVT had minimal effects on normal cells

Mol Ther Oncolytics. 2020 Sep 2;19:19-32.

PO2

3-9 μM

24, 48, 72 hours

PVT significantly suppressed the proliferation of pancreatic cancer cells with IC50 ranging from 3 to 9 μM

Mol Ther Oncolytics. 2020 Sep 2;19:19-32.

PANC1

3-9 μM

24, 48, 72 hours

PVT significantly suppressed the proliferation of pancreatic cancer cells with IC50 ranging from 3 to 9 μM

Mol Ther Oncolytics. 2020 Sep 2;19:19-32.

MIAPaCa2

3-9 μM

24, 48, 72 hours

PVT significantly suppressed the proliferation of pancreatic cancer cells with IC50 ranging from 3 to 9 μM

Mol Ther Oncolytics. 2020 Sep 2;19:19-32.

BxPC3

3-9 μM

24, 48, 72 hours

PVT significantly suppressed the proliferation of pancreatic cancer cells with IC50 ranging from 3 to 9 μM

Mol Ther Oncolytics. 2020 Sep 2;19:19-32.

AsPC1

3-9 μM

24, 48, 72 hours

PVT significantly suppressed the proliferation of pancreatic cancer cells with IC50 ranging from 3 to 9 μM

Mol Ther Oncolytics. 2020 Sep 2;19:19-32.

PO2

7.5 µM

24 h

PVT significantly increased autophagy, as shown by a 2.5–5.0 fold increase in AO staining

Cancers (Basel). 2021 Nov 12;13(22):5661.

MIAPaCa2

7.5 µM

24 h

PVT significantly increased autophagy, as shown by a 2.5–5.0 fold increase in AO staining

Cancers (Basel). 2021 Nov 12;13(22):5661.

L3.6pl

7.5 µM

24 h

PVT significantly increased autophagy, as shown by a 2.5–5.0 fold increase in AO staining

Cancers (Basel). 2021 Nov 12;13(22):5661.

BxPC3

7.5 µM

24 h

PVT significantly increased autophagy, as shown by a 3.0 fold increase in AO staining

Cancers (Basel). 2021 Nov 12;13(22):5661.

AsPC1

7.5 µM

24 h

PVT significantly increased autophagy, as shown by a 3.0 fold increase in AO staining

Cancers (Basel). 2021 Nov 12;13(22):5661.

Brain bEND.3 endothelial cells

1 and 2 μM

6 hours

Pimavanserin significantly reversed the increased lactate dehydrogenase (LDH) release, declined cell viability, increased endothelial permeability, and downregulated Claudin 5 and Krüppel-like factors 6 (KLF6) observed in the OGD/R group.

Bioengineered. 2021 Dec;12(1):7481-7494.

3D human liver spheroids

1 μM

7 days

Pimavanserin reduced FFA-induced COL1A1 deposition, but its effect was less pronounced than that of ketanserin.

Sci Rep. 2024 Jan 16;14(1):1396.

Pimavanserin hemitartrate 动物实验

Species Female athymic nude mice Female athymic nude mice Mice C57BL/6 mice Mice Mice	Animal Model Subcutaneous and orthotopic pancreatic tumor xenografts BxPC3 subcutaneous xenograft model P301L/COMT– and rTg(P301L)4510 mouse models Forced swim test (FST) APP/PS1 transgenic mice Middle cerebral artery occlusion (MCAO) model	Administration	Dosage	Frequency	Description	References
Female athymic nude mice	Subcutaneous and orthotopic pancreatic tumor xenografts	Oral	10 mg/kg	Every day for 28 days	PVT significantly suppressed the growth of subcutaneous and orthotopic pancreatic tumors by 51%-77% without any general signs of toxicity or changes in behavioral activity	Mol Ther Oncolytics. 2020 Sep 2;19:19-32.
Female athymic nude mice	BxPC3 subcutaneous xenograft model	Oral gavage	10 mg/kg	Daily for 33 days	PVT significantly suppressed tumor growth, reducing tumor volume by 64% and tumor weight by 73%	Cancers (Basel). 2021 Nov 12;13(22):5661.
Mice	P301L/COMT– and rTg(P301L)4510 mouse models	Intraperitoneal injection	3 mg/kg	Single dose	Pimavanserin ameliorated the hyperkinetic phenotype in both P301L/COMT– and rTg(P301L)4510 mouse models but had no significant impact on sensorimotor gating.	Alzheimers Dement (N Y). 2022 Feb 1;8(1):e12247
C57BL/6 mice	Forced swim test (FST)	Intraperitoneal injection	10 or 15 mg/kg	Single dose, tested 30-45 minutes after administration	Evaluate the antidepressant-like effects of ST-2300	Biomolecules. 2022 May 10;12(5):683
Mice	APP/PS1 transgenic mice	Subcutaneous injection	0.1, 0.3, 1 mg/kg	Every 24 hours for 80 hours	To assess the effect of Pimavanserin on brain interstitial fluid Aβ levels. Results showed a dose-dependent decrease in ISF Aβ40 levels, with a maximal reduction of 47.1±4.4% at the highest dose.	J Neurochem. 2021 Mar;156(5):658-673
Mice	Middle cerebral artery occlusion (MCAO) model		1 mg/kg	Pretreated before MCAO modeling	Pimavanserin significantly reversed the elevated neurological deficit score, increased brain water content, increased production of inflammatory factors, increased BBB permeability, and downregulated Claudin 5 expression observed in the MCAO group.	Bioengineered. 2021 Dec;12(1):7481-7494.

Species

Female athymic nude mice Female athymic nude mice Mice C57BL/6 mice Mice Mice

Animal Model

Subcutaneous and orthotopic pancreatic tumor xenografts BxPC3 subcutaneous xenograft model P301L/COMT– and rTg(P301L)4510 mouse models Forced swim test (FST) APP/PS1 transgenic mice Middle cerebral artery occlusion (MCAO) model

Administration

Dosage

Frequency

Description

References

Female athymic nude mice

Subcutaneous and orthotopic pancreatic tumor xenografts

Oral

10 mg/kg

Every day for 28 days

PVT significantly suppressed the growth of subcutaneous and orthotopic pancreatic tumors by 51%-77% without any general signs of toxicity or changes in behavioral activity

Mol Ther Oncolytics. 2020 Sep 2;19:19-32.

Female athymic nude mice

BxPC3 subcutaneous xenograft model

Oral gavage

10 mg/kg

Daily for 33 days

PVT significantly suppressed tumor growth, reducing tumor volume by 64% and tumor weight by 73%

Cancers (Basel). 2021 Nov 12;13(22):5661.

Mice

P301L/COMT– and rTg(P301L)4510 mouse models

Intraperitoneal injection

3 mg/kg

Single dose

Pimavanserin ameliorated the hyperkinetic phenotype in both P301L/COMT– and rTg(P301L)4510 mouse models but had no significant impact on sensorimotor gating.

Alzheimers Dement (N Y). 2022 Feb 1;8(1):e12247

C57BL/6 mice

Forced swim test (FST)

Intraperitoneal injection

10 or 15 mg/kg

Single dose, tested 30-45 minutes after administration

Evaluate the antidepressant-like effects of ST-2300

Biomolecules. 2022 May 10;12(5):683

Mice

APP/PS1 transgenic mice

Subcutaneous injection

0.1, 0.3, 1 mg/kg

Every 24 hours for 80 hours

To assess the effect of Pimavanserin on brain interstitial fluid Aβ levels. Results showed a dose-dependent decrease in ISF Aβ40 levels, with a maximal reduction of 47.1±4.4% at the highest dose.

J Neurochem. 2021 Mar;156(5):658-673

Mice

Middle cerebral artery occlusion (MCAO) model

1 mg/kg

Pretreated before MCAO modeling

Pimavanserin significantly reversed the elevated neurological deficit score, increased brain water content, increased production of inflammatory factors, increased BBB permeability, and downregulated Claudin 5 expression observed in the MCAO group.

Bioengineered. 2021 Dec;12(1):7481-7494.

Pimavanserin hemitartrate 参考文献

Pimavanserin hemitartrate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

0.99mL

0.20mL

0.10mL

4.97mL

0.99mL

0.50mL

9.95mL

1.99mL

0.99mL

Pimavanserin hemitartrate 技术信息

CAS号	706782-28-7
分子式	C₅₄H₇₄F₂N₆O₁₀
分子量	1005.2
SMILES Code	O=C(NCC1=CC=C(OCC(C)C)C=C1)N(CC2=CC=C(F)C=C2)C3CCN(C)CC3.O=C(O)[C@H](O)[C@@H](O)C(O)=O.O=C(NCC4=CC=C(OCC(C)C)C=C4)N(CC5=CC=C(F)C=C5)C6CCN(C)CC6
MDL No.	MFCD09970919

别名	ACP-103; Pimavanserin tartrate; ACP-103 hemitartrate
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

细胞实验：

DMSO: 80 mg/mL(79.59 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H₂O: 50 mg/mL(49.74 mM)，配合低频超声助溶

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

方案三

Pimavanserin hemitartrate {[allProObj[0].p_purity_real_show]}

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Pimavanserin hemitartrate 质控信息

Pimavanserin hemitartrate 生物活性

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Pimavanserin hemitartrate 动物实验

Pimavanserin hemitartrate 参考文献

Pimavanserin hemitartrate 实验方案

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