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  2. Metabolic Enzyme/Protease GPCR/G Protein
  3. Phosphodiesterase (PDE) GPR35
  4. Zaprinast

Zaprinast  (Synonyms: 扎普司特; M&B 22948)

目錄號: HY-B1816 純度: 99.95%
COA 產(chǎn)品使用指南

Zaprinast (M&B 22948) 是 cGMP 選擇性磷酸二酯酶 (PDE5) 的選擇性抑制劑。Zaprinast 導(dǎo)致肌細胞中的 cGMP 水平顯著增加。Zaprinast 是一種 G 蛋白偶聯(lián)受體 35 (GPR35) 激動劑，可強烈激活大鼠 GPR35，并中度激活人 GPR35。Zaprinast 通過抗增殖和促凋亡作用減少血管重塑。

MCE 的所有產(chǎn)品僅用作科學研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)

Zaprinast Chemical Structure

Zaprinast Chemical Structure

CAS No. : 37762-06-4

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥500
In-stock
5 mg ￥420
In-stock
10 mg ￥700
In-stock
25 mg ￥1296
In-stock
50 mg ￥2100
In-stock
100 mg ￥3400
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻

查看 Phosphodiesterase (PDE) 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects[1][2][3].

IC50 & Target[1][2]

PDE5

 

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
0.0611 μM
Compound: 3
Agonist activity at rat GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
Agonist activity at rat GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
[PMID: 23713606]
CHO EC50
0.98 μM
Compound: 3
Agonist activity at mouse GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
Agonist activity at mouse GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
[PMID: 23713606]
CHO EC50
1.96 μM
Compound: 3
Agonist activity at human GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
Agonist activity at human GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
[PMID: 23713606]
CHO EC50
2.24 μM
Compound: 3
Agonist activity at human GPR35b expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
Agonist activity at human GPR35b expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay
[PMID: 23713606]
HT-29 EC50
0.11 μM
Compound: Zaprinast
Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis
Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis
10.1039/C2MD20210G
HT-29 EC50
0.14 μM
Compound: Zaprinast
Agonist activity at GPR35 in human HT-29 cells measured after 10 mins by dynamic mass redistribution assay
Agonist activity at GPR35 in human HT-29 cells measured after 10 mins by dynamic mass redistribution assay
[PMID: 24900508]
HT-29 EC50
0.16 μM
Compound: zaprinast
Agonist activity at GPR35 in human HT-29 cells after 1 hr by dynamic mass redistribution assay
Agonist activity at GPR35 in human HT-29 cells after 1 hr by dynamic mass redistribution assay
[PMID: 21950657]
HT-29 EC50
0.16 μM
Compound: Zaprinast
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
[PMID: 24900447]
HT-29 EC50
0.16 μM
Compound: Zaprinast
Agonist activity at GPR35 in human HT-29 cells by dynamic mass redistribution assay
Agonist activity at GPR35 in human HT-29 cells by dynamic mass redistribution assay
[PMID: 22572579]
HT-29 IC50
1.22 μM
Compound: zaprinast
Agonist activity at GPR35 in human HT-29 cells assessed as desensitization of 1 uM zaprinast-induced DMR after 1 hr by dynamic mass redistribution assay
Agonist activity at GPR35 in human HT-29 cells assessed as desensitization of 1 uM zaprinast-induced DMR after 1 hr by dynamic mass redistribution assay
[PMID: 21950657]
HT-29 IC50
1.22 μM
Compound: Zaprinast
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
[PMID: 24900447]
HT-29 IC50
10.5 μM
Compound: zaprinast
Antagonist activity at GPR35 in human HT-29 cells assessed as inhibition of zaprinast-induced DMR by dynamic mass redistribution assay
Antagonist activity at GPR35 in human HT-29 cells assessed as inhibition of zaprinast-induced DMR by dynamic mass redistribution assay
[PMID: 21950657]
U2OS EC50
3.25 μM
Compound: Zaprinast
Agonist activity at GPR35 in human U2OS cells assessed as induction of beta-arrestin translocation after 5 hrs by beta-lactamase reporter gene assay
Agonist activity at GPR35 in human U2OS cells assessed as induction of beta-arrestin translocation after 5 hrs by beta-lactamase reporter gene assay
10.1039/C2MD20210G
U2OS EC50
4.2 μM
Compound: zaprinast
Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and GPR35-GA14-VP16 transcription factor fusion protein assessed as transcriptional activation after 5 hrs by tango beta-arrestin translocation reporter assay
Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and GPR35-GA14-VP16 transcription factor fusion protein assessed as transcriptional activation after 5 hrs by tango beta-arrestin translocation reporter assay
[PMID: 21950657]
U2OS EC50
5.3 μM
Compound: Zaprinast
Agonist activity at human GPR35 expressed in U2OS cells coexpressing Gal4-VP16/beta-arrestin fusion protein after 5 hrs by tango beta-arrestin translocation reporter gene assay
Agonist activity at human GPR35 expressed in U2OS cells coexpressing Gal4-VP16/beta-arrestin fusion protein after 5 hrs by tango beta-arrestin translocation reporter gene assay
[PMID: 24900508]
U2OS EC50
6.1 μM
Compound: Zaprinast
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
[PMID: 24900447]
U2OS EC50
6.2 μM
Compound: Zaprinast
Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and Gal4-VP16 transcription factor assessed as beta arrestin translocation after 5 hrs by Tango assay
Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and Gal4-VP16 transcription factor assessed as beta arrestin translocation after 5 hrs by Tango assay
[PMID: 22572579]
體外研究
(In Vitro)

Zaprinast (0.1, 0.3, 1, 3, 10, 30 μM) 在 HEK293 細胞中以濃度依賴性方式誘導(dǎo)共表達 FLAG-hGPR35 和四種外源 Gα 蛋白的轉(zhuǎn)染子中的細胞內(nèi)鈣動員[2]。
Zaprinast (100 μM；5 分鐘) 可促進 HEK293T 細胞中人 GPR35a C 末端尾部 5 個不同氨基酸的磷酸化[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Zaprinast (3 和 10 mg/kg；腹腔注射) 可增強高架十字迷宮 (EPM) 中的空間記憶，并減少 Hughes 盒測試中的探索活動[5]。

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

Animal Model: Male inbred BALB/c ByJ mice aged 7 weeks[5]
Dosage: 3 and 10 mg/kg
Administration: IP; 60 min before the first session
Result: Significantly decreased second-day latency compared to the control group in the EPM test with 10 mg/kg.
Significantly shortened the time spent in the novel side in the Hughes box with 10 mg/kg.
分子量

271.27

Formula

C13H13N5O2
CAS 號
性狀

固體

顏色

Off-white to pink

中文名稱

扎普司特
運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 62.5 mg/mL (230.40 mM; 超聲助溶; 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 3.6864 mL 18.4318 mL 36.8636 mL
5 mM 0.7373 mL 3.6864 mL 7.3727 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 (protect from light, stored under nitrogen)。-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

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (7.67 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (7.67 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
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

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.95%

參考文獻

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 (protect from light, stored under nitrogen)。-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 3.6864 mL 18.4318 mL 36.8636 mL 92.1591 mL
5 mM 0.7373 mL 3.6864 mL 7.3727 mL 18.4318 mL
10 mM 0.3686 mL 1.8432 mL 3.6864 mL 9.2159 mL
15 mM 0.2458 mL 1.2288 mL 2.4576 mL 6.1439 mL
20 mM 0.1843 mL 0.9216 mL 1.8432 mL 4.6080 mL
25 mM 0.1475 mL 0.7373 mL 1.4745 mL 3.6864 mL
30 mM 0.1229 mL 0.6144 mL 1.2288 mL 3.0720 mL
40 mM 0.0922 mL 0.4608 mL 0.9216 mL 2.3040 mL
50 mM 0.0737 mL 0.3686 mL 0.7373 mL 1.8432 mL
60 mM 0.0614 mL 0.3072 mL 0.6144 mL 1.5360 mL
80 mM 0.0461 mL 0.2304 mL 0.4608 mL 1.1520 mL
100 mM 0.0369 mL 0.1843 mL 0.3686 mL 0.9216 mL
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產(chǎn)品名稱：
Zaprinast
目錄號：
HY-B1816
需求量：