Zaprinast (Synonyms: 扎普司特; M&B 22948)

目錄號(hào): HY-B1816 純度: 99.95%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南

摩爾計(jì)算器

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(xì)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(dòng)劑，可強(qiáng)烈激活大鼠 GPR35，并中度激活人 GPR35。Zaprinast 通過(guò)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(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Zaprinast Chemical Structure

CAS No. : 37762-06-4

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可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3. 試用裝只面向終端客戶。

規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in DMSO	￥500	In-stock
5 mg	￥420	In-stock
10 mg	￥700	In-stock
50 mg	￥2100	In-stock
100 mg	￥3400	In-stock
200 mg		詢價(jià)
500 mg		詢價(jià)

or 大包裝詢價(jià)

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

•Mol Neurobiol. 2024 Jun 15. [Abstract]

Zaprinast 相關(guān)產(chǎn)品

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

生物活性
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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(xì)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(xì)胞中以濃度依賴性方式誘導(dǎo)共表達(dá) FLAG-hGPR35 和四種外源 Gα 蛋白的轉(zhuǎn)染子中的細(xì)胞內(nèi)鈣動(dòng)員^[2]。
Zaprinast (100 μM；5 分鐘) 可促進(jìn) HEK293T 細(xì)胞中人 GPR35a C 末端尾部 5 個(gè)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(qiáng)高架十字迷宮 (EPM) 中的空間記憶，并減少 Hughes 盒測(cè)試中的探索活動(dòng)^[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(hào)

37762-06-4

性狀

固體

顏色

Off-white to pink

中文名稱

扎普司特

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : 62.5 mg/mL (230.40 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)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
10 mM	0.3686 mL	1.8432 mL	3.6864 mL

查看完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)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(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

請(qǐng)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(chǔ)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(qǐng)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(chǔ)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。
方案三

請(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
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，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)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(guò) 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購(gòu)。，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)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(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)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%

選擇批次：

Data Sheet (643 KB) SDS (393 KB)

COA (269 KB) HNMR (275 KB) LCMS (265 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Choi SH , et al. Zaprinast, an inhibitor of cGMP-selective phosphodiesterases, enhances the secretion of TNF-alpha and IL-1beta and the expression of iNOS and MHC class II molecules in rat microglial cells. J Neurosci Res. 2002 Feb 1;67(3):411-21. [Content Brief]

[2]. Taniguchi Y, et al. Zaprinast, a well-known cyclic guanosine monophosphate-specific phosphodiesterase inhibitor, is an agonist for GPR35. FEBS Lett. 2006 Sep 18;580(21):5003-8. Epub 2006 Aug 17. [Content Brief]

[3]. Keswani AN , et al The cyclic GMP modulators YC-1 and zaprinast reduce vessel remodeling through antiproliferative and proapoptotic effects. J Cardiovasc Pharmacol Ther. 2009 Jun;14(2):116-24. [Content Brief]

[4]. Nina Divorty, et al. Agonist-induced phosphorylation of orthologues of the orphan receptor GPR35 functions as an activation sensor. J Biol Chem. 2022 Mar;298(3):101655. [Content Brief]

[5]. Furuzan Akar, et al. Zaprinast and rolipram enhances spatial and emotional memory in the elevated plus maze and passive avoidance tests and diminishes exploratory activity in naive mice. Med Sci Monit Basic Res. 2014 Jul 24:20:105-11. [Content Brief]

Zaprinast 相關(guān)分類

Neurological Disease Endocrinology Cardiovascular Disease

完整儲(chǔ)備液配制表

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

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.

Keywords:

Zaprinast37762-06-4M&B 22948扎普司特Phosphodiesterase (PDE)GPR35G Protein-Coupled Receptor 35cGMPPhosphodiesterasePDE5vessel remodelingantiproliferativeproapoptoticInhibitorinhibitorinhibit

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營(yíng)業(yè)執(zhí)照（三證合一）

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Zaprinast (Synonyms: 扎普司特; M&B 22948)

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