Proguanil (Synonyms: 氯胍)

目录号: HY-B0806 纯度: 99.84%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Proguanil 是一种抗疟前体，被代谢为活性代谢物环鸟苷 (HY-12784)。Proguanil 是一种二氢叶酸还原酶 (DHFR) 抑制剂。

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Proguanil Chemical Structure

CAS No. : 500-92-5

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥550	In-stock
5 mg	￥312	In-stock
10 mg	￥500	In-stock
25 mg	￥1100	In-stock
50 mg	￥1800	In-stock
100 mg		询价
200 mg		询价

or 大包装询价

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Customer Review

Other Forms of Proguanil:

MCE 顾客使用本产品发表的 1 篇科研文献

•ACS Omega. 2024 Feb 28;9(10):11870-11882. [Abstract]

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor^[1]^[2].

IC₅₀ & Target

Plasmodium

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A2780	IC₅₀	13 μM Compound: Proguanil	Antiproliferative activity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31864776]
A549	IC₅₀	3.8 μM Compound: Proguanil	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31864776]
HCT-116	IC₅₀	8.4 μM Compound: Proguanil	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31864776]
HEK293	EC₅₀	> 10000 nM Compound: BIG22	Agonist activity at human TAAR1 expressed in HEK293 cells assessed as cAMP accumulation after 20 mins by BRET assay Agonist activity at human TAAR1 expressed in HEK293 cells assessed as cAMP accumulation after 20 mins by BRET assay	[PMID: 27823885]
HeLa	EC₅₀	> 100 μM Compound: 30	Antiviral activity against Respiratory syncytial virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against Respiratory syncytial virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
HeLa	EC₅₀	> 100 μM Compound: 30	Antiviral activity against coxsackie B4 virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against coxsackie B4 virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
HeLa	EC₅₀	> 100 μM Compound: 30	Antiviral activity against vesicular stomatitis virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis Antiviral activity against vesicular stomatitis virus infected in human HeLa cells assessed as inhibition of viral-induced cytopathic effect measured after 3 to 6 days post infection by microscopic analysis	[PMID: 28477572]
MDCK	CC₅₀	> 100 μM Compound: 30	Cytotoxicity against dog MDCK cells assessed as reduction in cell viability measured after 5 to 6 days by MTS assay Cytotoxicity against dog MDCK cells assessed as reduction in cell viability measured after 5 to 6 days by MTS assay	[PMID: 28477572]
T-24	IC₅₀	18.4 μM Compound: Proguanil	Antiproliferative activity against human T24 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human T24 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31864776]
UMUC3	IC₅₀	16.3 μM Compound: Proguanil	Antiproliferative activity against human UM-UC-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human UM-UC-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31864776]

体外研究
(In Vitro)

Proguanil 本身只有较弱的体外抗疟活性 (IC₅₀=2.4-19 μM)，其有效性取决于活性代谢物环胍 (IC₅₀=0.5-2.5 纳米)。Cycloguanil 是一种二氢叶酸还原酶 (DHFR) 抑制剂。Atovaquone 和 Proguanil 的组合在体外具有协同作用。这两种药物还对疟原虫的配子体和红细胞前 (肝脏) 阶段有活性^[1]。
Proguanil 作为双胍而非其代谢物环胍 (一种寄生虫二氢叶酸还原酶) 发挥作用[DHFR]抑制剂) 来增强 Atovaquone 的作用。Proguanil 介导的增强作用对 Atovaquone 具有特异性，因为其他线粒体电子传递抑制剂 (如粘噻唑和抗霉素) 的作用不会因加入 Proguanil 而改变^[2]。
5-HT ₃ 受体反应被 Proguanil 、代谢物 4-氯苯基-1-双胍 (CPB) 和活性代谢物环胍 (CG) 可逆抑制，IC₅₀ 为 1.81，1.48 和 4.36 μM^[3]。

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

体内研究
(In Vivo)

Proguanil (口服2.9 mg/kg 体重；每天一次，分别给药 5 天和 6 周) 在 wistar 品系白化大鼠中显示轻度退行性变化 5 天，而在 6 周内显示严重退行性变化^[4]。
Proguanil 处理大鼠的血清睾酮水平显著降低^[4]。
给予马拉隆 (atovaquone 和 Proguanil) 实验B. gibsoni 感染两只慢性期犬和三只急性期犬导致寄生虫血症减少，并观察到临床改善^[5]。

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

Clinical Trial

分子量

253.73

Formula

C₁₁H₁₆ClN₅

CAS 号

500-92-5

性状

固体

颜色

White to off-white

中文名称

氯胍

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 130 mg/mL (512.36 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.9412 mL	19.7060 mL	39.4120 mL
5 mM	0.7882 mL	3.9412 mL	7.8824 mL
10 mM	0.3941 mL	1.9706 mL	3.9412 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制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

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.17 mg/mL (8.55 mM); 澄清溶液

此方案可获得 ≥ 2.17 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.17 mg/mL (8.55 mM); 澄清溶液

此方案可获得 ≥ 2.17 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.17 mg/mL (8.55 mM); 澄清溶液

此方案可获得 ≥ 2.17 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.84%

选择批次：

Data Sheet (649 KB) SDS (392 KB)

COA (188 KB) LCMS (267 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Pudney M, et al. Atovaquone and proguanil hydrochloride: a review of nonclinical studies. J Travel Med. 1999 May;6 Suppl 1:S8-12. [Content Brief]

[2]. Srivastava IK, et al. A mechanism for the synergistic antimalarial action of atovaquone and proguanil. Antimicrob Agents Chemother. 1999 Jun;43(6):1334-9. [Content Brief]

[3]. Lochner M, et al. The antimalarial drug proguanil is an antagonist at 5-HT3 receptors. J Pharmacol Exp Ther. 2014 Dec;351(3):674-84. [Content Brief]

[4]. Stephen AO, et al. Prolonged administration of proguanil induces reproductive toxicity in male rats. J Toxicol Sci. 2011 Oct;36(5):587-99. [Content Brief]

[5]. Iguchi A, et al. The in vitro interactions and in vivo efficacy of atovaquone and proguanil against Babesia gibsoni infection in dogs. Vet Parasitol. 2013 Nov 8;197(3-4):527-33. [Content Brief]

Cell Assay ^[4]	Sertoli cells obtained from sixteen to eighteen day-old-rats are cultured and treated with 0.3 μM to 10 μM of proguanil for 5 days after which Sertoli cell viability and nuclei integrity are determined. Also, the genetic expressions of transferrin and Glial cell line-derived neurotrophic factor are assessed^[4]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[4]	Rats: Groups of ten to twelve-week-old rats are administered proguanil (2.9 mg/kg body weight) daily for 5 days and 6 weeks respectively. Thereafter, body and reproductive organ weights are taken, sperm parameters are analyzed, while the histology of the testis and epididymis are carried out. Also, serum levels of testosterone, luteinizing hormone and follicle stimulating hormone are determined^[4]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Pudney M, et al. Atovaquone and proguanil hydrochloride: a review of nonclinical studies. J Travel Med. 1999 May;6 Suppl 1:S8-12. [Content Brief] [2]. Srivastava IK, et al. A mechanism for the synergistic antimalarial action of atovaquone and proguanil. Antimicrob Agents Chemother. 1999 Jun;43(6):1334-9. [Content Brief] [3]. Lochner M, et al. The antimalarial drug proguanil is an antagonist at 5-HT3 receptors. J Pharmacol Exp Ther. 2014 Dec;351(3):674-84. [Content Brief] [4]. Stephen AO, et al. Prolonged administration of proguanil induces reproductive toxicity in male rats. J Toxicol Sci. 2011 Oct;36(5):587-99. [Content Brief] [5]. Iguchi A, et al. The in vitro interactions and in vivo efficacy of atovaquone and proguanil against Babesia gibsoni infection in dogs. Vet Parasitol. 2013 Nov 8;197(3-4):527-33. [Content Brief]

Proguanil 相关分类

Infection

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.9412 mL	19.7060 mL	39.4120 mL	98.5299 mL
	5 mM	0.7882 mL	3.9412 mL	7.8824 mL	19.7060 mL
	10 mM	0.3941 mL	1.9706 mL	3.9412 mL	9.8530 mL
	15 mM	0.2627 mL	1.3137 mL	2.6275 mL	6.5687 mL
	20 mM	0.1971 mL	0.9853 mL	1.9706 mL	4.9265 mL
	25 mM	0.1576 mL	0.7882 mL	1.5765 mL	3.9412 mL
	30 mM	0.1314 mL	0.6569 mL	1.3137 mL	3.2843 mL
	40 mM	0.0985 mL	0.4926 mL	0.9853 mL	2.4632 mL
	50 mM	0.0788 mL	0.3941 mL	0.7882 mL	1.9706 mL
	60 mM	0.0657 mL	0.3284 mL	0.6569 mL	1.6422 mL
	80 mM	0.0493 mL	0.2463 mL	0.4926 mL	1.2316 mL
	100 mM	0.0394 mL	0.1971 mL	0.3941 mL	0.9853 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:

Proguanil500-92-5氯胍ParasiteAntifolateantimalarialinfectionembryotoxicitytoxicitybiguanidereproductiveInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

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上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Proguanil (Synonyms: 氯胍)

Customer Review

Other Forms of Proguanil:

MCE 顾客使用本产品发表的 1 篇科研文献