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  1. Neuronal Signaling
  2. Sigma Receptor
  3. PD 144418 oxalate

PD 144418 oxalate 是一種高親和力,強(qiáng)效和選擇性的 sigma 1 受體 (σ1 receptor) 配體 (對 σ1 和 σ2 的 Ki 值分別為 0.08 nM 和 1377 nM),對其他受體,離子通道和酶沒有任何顯著的親和力。PD 144418 oxalate 具有潛在的抗精神病活性。

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PD 144418 oxalate Chemical Structure

PD 144418 oxalate Chemical Structure

CAS No. : 1794760-28-3

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查看 Sigma Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows potential antipsychotic activity[1][2].

IC50 & Target

Ki: 0.08 nM (σ1 receptor) and 1377 nM (σ2 receptor)[1]

體外研究
(In Vitro)

In vitro, PD 144418 reverses the N-methyl-D-aspartate (NMDA)-induced increase in cyclic GMP (cGMP) in rat cerebellar slices without affecting the basal levels, suggesting that σ1 sites may be important in the regulation of glutamine-induced actions. PD 144418 potentiates the decrease in 5-hydroxytryptophan caused by Haloperidol in the mesolimbic region, but by itself has no effect in 5-HT and dopamine (DA) synthesis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

體內(nèi)研究
(In Vivo)

PD 144418 (10 mg/kg; intraperitoneal injection; male CD-1 mice) treatment antagonizes Mescaline-induced scratching at doses that did not alter spontaneous motor activity, with PD 144418 showing ED50 values of 7.0 mg/kg i.p.[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CD-1 mice induced with Mescaline[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; once
Result: Antagonized mescaline-induced scratching at doses that did not alter spontaneous motor activity.
分子量

372.41

Formula

C20H24N2O5

CAS 號
性狀

固體

顏色

Off-white to light yellow

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細(xì)胞實驗: 

DMSO 中的溶解度 : 25 mg/mL (67.13 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.6852 mL 13.4261 mL 26.8521 mL
5 mM 0.5370 mL 2.6852 mL 5.3704 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 98.65%

參考文獻(xiàn)

PD 144418 oxalate 相關(guān)分類

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6852 mL 13.4261 mL 26.8521 mL 67.1303 mL
5 mM 0.5370 mL 2.6852 mL 5.3704 mL 13.4261 mL
10 mM 0.2685 mL 1.3426 mL 2.6852 mL 6.7130 mL
15 mM 0.1790 mL 0.8951 mL 1.7901 mL 4.4754 mL
20 mM 0.1343 mL 0.6713 mL 1.3426 mL 3.3565 mL
25 mM 0.1074 mL 0.5370 mL 1.0741 mL 2.6852 mL
30 mM 0.0895 mL 0.4475 mL 0.8951 mL 2.2377 mL
40 mM 0.0671 mL 0.3357 mL 0.6713 mL 1.6783 mL
50 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3426 mL
60 mM 0.0448 mL 0.2238 mL 0.4475 mL 1.1188 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱:
PD 144418 oxalate
目錄號:
HY-108512A
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