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G蛋白偶联受体/G蛋白
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/ 5-羟色胺受体 / Sarpogrelate HCl/盐酸沙格雷酯

Sarpogrelate HCl/盐酸沙格雷酯 {[allProObj[0].p_purity_real_show]}

货号：A166685 同义名： MCI-9042; Sarpogrelate (hydrochloride)

Sarpogrelate HCl是一种 5-HT2A 和 5-HT2B 受体的拮抗剂，能够阻断血清素诱导的血小板聚集，用于治疗糖尿病、Buerger 病、雷诺病、冠状动脉病、心绞痛和动脉粥样硬化。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Sarpogrelate HCl/盐酸沙格雷酯 化学结构 CAS号：135159-51-2
Sarpogrelate HCl/盐酸沙格雷酯 化学结构
CAS号：135159-51-2
Sarpogrelate HCl/盐酸沙格雷酯 3D分子结构
CAS号：135159-51-2
Sarpogrelate HCl/盐酸沙格雷酯 化学结构 CAS号：135159-51-2
Sarpogrelate HCl/盐酸沙格雷酯 3D分子结构 CAS号：135159-51-2
规格 价格 会员价 库存 数量
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Sarpogrelate HCl/盐酸沙格雷酯 纯度/质量文件 产品仅供科研

货号：A166685 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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-HT1D, pIC50: 5.9

5-HT1A, pIC50: 6.4

 		+

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 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 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-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 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-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 nM

 		++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 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-HT1B, pKi: 6.1

5-HT1D, pKi: 6

 		++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

 		+

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。

Sarpogrelate HCl/盐酸沙格雷酯 生物活性

靶点

  • 5-HT2

    5-HT2A, Kd:2.1 nM

    5-HT2C, Kd:1.1 nM
描述 Sarpogrelate Hydrochloride is a highly selective serotonin (5-hydroxytryptamine, 5-HT2A) receptor antagonist used as an antiplatelet agent for the treatment of peripheral artery disease. Sarpogrelate hydrochloride might be a weak inhibitor of CYP (cytochrome P450 ) 2D6[3]. Moreover, Sarpogrelate Hydrochloride ameliorates diabetic nephropathy not only by suppressing macrophage infiltration, but also by anti-inflammatory and anti-fibrotic effects[4]. A 5- or 1-day treatment with 50 mg/kg sarpogrelate can completely protect the retina of BALB/c mice from light-induced retinopathy[5].

Sarpogrelate HCl/盐酸沙格雷酯 参考文献

[1]Nishio H, Inoue A, et al. Binding affinity of sarpogrelate, a new antiplatelet agent, and its metabolite for serotonin receptor subtypes. Arch Int Pharmacodyn Ther. 1996 Mar-Apr;331(2):189-202.

[2]Pertz H, Elz S. In-vitro pharmacology of sarpogrelate and the enantiomers of its major metabolite: 5-HT2A receptor specificity, stereoselectivity and modulation of ritanserin-induced depression of 5-HT contractions in rat tail artery. J Pharm Pharmacol. 1995 Apr;47(4):310-6.

[3]Min JS, Kim D, Park JB, Heo H, Bae SH, Seo JH, Oh E, Bae SK. Application of physiologically based pharmacokinetic modeling in predicting drug-drug interactions for sarpogrelate hydrochloride in humans. Drug Des Devel Ther. 2016 Sep 14;10:2959-2972. doi: 10.2147/DDDT.S109141. PMID: 27695293; PMCID: PMC5028085.

[4]Lee ES, Lee MY, Kwon MH, Kim HM, Kang JS, Kim YM, Lee EY, Chung CH. Sarpogrelate hydrochloride ameliorates diabetic nephropathy associated with inhibition of macrophage activity and inflammatory reaction in db/db mice. PLoS One. 2017 Jun 22;12(6):e0179221. doi: 10.1371/journal.pone.0179221. PMID: 28640832; PMCID: PMC5480859.

[5]Tullis BE, Ryals RC, Coyner AS, Gale MJ, Nicholson A, Ku C, Regis D, Sinha W, Datta S, Wen Y, Yang P, Pennesi ME. Sarpogrelate, a 5-HT2A Receptor Antagonist, Protects the Retina From Light-Induced Retinopathy. Invest Ophthalmol Vis Sci. 2015 Jul;56(8):4560-9. doi: 10.1167/iovs.15-16378. PMID: 26200496; PMCID: PMC4515947.

Sarpogrelate HCl/盐酸沙格雷酯 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.21mL

10.73mL

2.15mL

1.07mL

21.46mL

4.29mL

2.15mL

Sarpogrelate HCl/盐酸沙格雷酯 技术信息

CAS号135159-51-2
分子式C24H32ClNO6
分子量 465.97
SMILES Code O=C(OC(COC1=CC=CC=C1CCC2=CC=CC(OC)=C2)CN(C)C)CCC(O)=O.[H]Cl
MDL No. MFCD00887582
别名 MCI-9042; Sarpogrelate (hydrochloride); Sarpogrelate hydrochloride
运输蓝冰
InChI Key POQBIDFFYCYHOB-UHFFFAOYSA-N
Pubchem ID 444005
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C
溶解方案

DMSO: 60 mg/mL(128.76 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: 30 mg/mL(64.38 mM)，配合低频超声助溶

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
配制的工作液建议现用现配，短期内尽快用完。 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

Tags: Sarpogrelate | 135159-51-2 | MCI-9042 | MCI9042 | MCI 9042 | 5-HT2R Antagonist | GPCR/G Protein | Neuronal Signaling | 5-HT Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Sarpogrelate HCl/盐酸沙格雷酯 纯度/质量文件 | Sarpogrelate HCl/盐酸沙格雷酯 亚型比较 | Sarpogrelate HCl/盐酸沙格雷酯 生物活性 | Sarpogrelate HCl/盐酸沙格雷酯 参考文献 | Sarpogrelate HCl/盐酸沙格雷酯 实验方案 | Sarpogrelate HCl/盐酸沙格雷酯 技术信息

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