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  2. Anti-infection
  3. Parasite
  4. Primaquine

Primaquine 是一種有效的抗瘧疾劑，也是一種有效的惡性瘧原蟲殺配子體。Primaquine 可防止間日瘧和卵形瘧復(fù)發(fā)。

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)

Primaquine Chemical Structure

Primaquine Chemical Structure

CAS No. : 90-34-6

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥440
In-stock
50 mg ￥400
In-stock
100 mg   詢價(jià)  
200 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Primaquine:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Primaquine is a potent antimalaria agent and a potent gametocytocide in falciparum malaria. Primaquine prevents relapse in vivax and ovale malaria[1][2].

IC50 & Target

Plasmodium

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 100 μM
Compound: 1, PQ
Cytotoxicity against human A549 cells after 72 hrs
Cytotoxicity against human A549 cells after 72 hrs
[PMID: 19799426]
Caco-2 IC50
48 μM
Compound: 1
Antitumor activity against human Caco-2 cells after 48 hours hrs by SRB assay
Antitumor activity against human Caco-2 cells after 48 hours hrs by SRB assay
[PMID: 19896373]
Hepatocyte IC50
0.64 μM
Compound: Primaquine
Antimalarial activity against Plasmodium yoelii 265 sporozoites in primary mice (Mus musculus) hepatocytes after 48 hrs
Antimalarial activity against Plasmodium yoelii 265 sporozoites in primary mice (Mus musculus) hepatocytes after 48 hrs
[PMID: 18456502]
Hepatocyte CC50
54 μM
Compound: PQ
Cytotoxicity against human primary hepatocytes after 48 hrs by MTT assay
Cytotoxicity against human primary hepatocytes after 48 hrs by MTT assay
[PMID: 29754074]
Hepatocyte CC50
54.21 μM
Compound: PQ
Cytotoxicity against human primary hepatocytes assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human primary hepatocytes assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 30199706]
Hepatocyte IC50
75.7 nM
Compound: Primaquine
Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs
Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs
[PMID: 18212104]
HepG2 IC50
< 1 μM
Compound: Primaquine
Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin
Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin
[PMID: 23927658]
HepG2 IC50
101 μM
Compound: PQ
Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay
Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay
[PMID: 28939120]
HepG2 IC50
1160 nM
Compound: Primaquine
Antiplasmodial activity against liver stage of Plasmodium yoelii 17X NL sporozoites infected in human HepG2 cells expressing CD81 after 48 hrs by DAPI staining-based immunofluorescence analysis
Antiplasmodial activity against liver stage of Plasmodium yoelii 17X NL sporozoites infected in human HepG2 cells expressing CD81 after 48 hrs by DAPI staining-based immunofluorescence analysis
[PMID: 25791675]
HepG2 CC50
120.03 μM
Compound: PQ
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 30199706]
HepG2 CC50
6.1 μM
Compound: Primaquine
Cytotoxicity against human HepG2 cells expressing CD81 assessed as cell viability after 72 hrs by CellTiter-glo assay
Cytotoxicity against human HepG2 cells expressing CD81 assessed as cell viability after 72 hrs by CellTiter-glo assay
[PMID: 25791675]
HepG2 CC50
69.8 μM
Compound: PQ
Cytotoxicity against human HepG2 cells expressing CD81 assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells expressing CD81 assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 30199706]
HT-29 IC50
69.7 μM
Compound: 1
Antitumor activity against human HT-29 cells after 48 hours hrs by SRB assay
Antitumor activity against human HT-29 cells after 48 hours hrs by SRB assay
[PMID: 19896373]
Huh-7 IC50
2 μM
Compound: 1, PQ
Antiplasmodial activity against liver-stage GFP expressing Plasmodium berghei sporozoites infected in human HuH7 cells assessed as inhibition of parasite schizonts development after 48 hrs by FACS analysis
Antiplasmodial activity against liver-stage GFP expressing Plasmodium berghei sporozoites infected in human HuH7 cells assessed as inhibition of parasite schizonts development after 48 hrs by FACS analysis
[PMID: 19799426]
Huh-7 IC50
2.4 μM
Compound: 12; PQ
Antimalarial activity against liver stage Plasmodium berghei infected in human Huh-7 cells assessed as inhibition by bioluminescence assay
Antimalarial activity against liver stage Plasmodium berghei infected in human Huh-7 cells assessed as inhibition by bioluminescence assay
[PMID: 34242031]
Huh-7 IC50
3.4 μg/mL
Compound: Primaquine
Antimalarial activity against liver stage of Plasmodium berghei infected in human Huh7 cells assessed as reduction in parasite load treated after 2 hrs of infection for 46 hrs by luciferase assay
Antimalarial activity against liver stage of Plasmodium berghei infected in human Huh7 cells assessed as reduction in parasite load treated after 2 hrs of infection for 46 hrs by luciferase assay
[PMID: 25103602]
Huh-7 IC50
7.5 μM
Compound: Primaquine
Antiplasmodial activity against liver sporozoite stage of Plasmodium berghei expressing luciferase and GFP infected in human HuH7 cells assessed as inhibition of parasite development incubated for 1 hr prior to parasite infection measured after 48 hrs by
Antiplasmodial activity against liver sporozoite stage of Plasmodium berghei expressing luciferase and GFP infected in human HuH7 cells assessed as inhibition of parasite development incubated for 1 hr prior to parasite infection measured after 48 hrs by
[PMID: 24125849]
Huh-7 IC50
7.5 μM
Compound: 1, PQ
Antiplasmodial activity against liver stage Plasmodium berghei infected in human HuH7 cells co-expressing GFP-Luccon treated for 1 hr prior to infection followed by 24 hrs after compound washout measured after 48 hrs post-infection by Alamar Blue assay
Antiplasmodial activity against liver stage Plasmodium berghei infected in human HuH7 cells co-expressing GFP-Luccon treated for 1 hr prior to infection followed by 24 hrs after compound washout measured after 48 hrs post-infection by Alamar Blue assay
[PMID: 23701465]
Huh-7 IC50
7.5 μM
Compound: 3, PQ
Antiplasmodial activity against Plasmodium berghei liver stage form transfected in human Huh-7 cells assessed as cell viability after 48 hrs by luciferase reporter gene assay
Antiplasmodial activity against Plasmodium berghei liver stage form transfected in human Huh-7 cells assessed as cell viability after 48 hrs by luciferase reporter gene assay
[PMID: 23273038]
Huh-7 IC50
7.5 μM
Compound: 1, PQ
Antiplasmodial activity against liver stage of Plasmodium berghei sporozoites expressing firefly luciferase infected in human Huh7 cells assessed as inhibition of parasite development treated 1 hr prior to infection followed by compound replenisment at 24
Antiplasmodial activity against liver stage of Plasmodium berghei sporozoites expressing firefly luciferase infected in human Huh7 cells assessed as inhibition of parasite development treated 1 hr prior to infection followed by compound replenisment at 24
10.1039/C2MD20113E
Huh-7 IC50
7.5 μM
Compound: Primaquine
Antiplasmodial activity against liver stage of Plasmodium berghei expressing GFP infected in human Huh7 cells by luminescence assay
Antiplasmodial activity against liver stage of Plasmodium berghei expressing GFP infected in human Huh7 cells by luminescence assay
[PMID: 23806111]
Huh-7 IC50
7500 nM
Compound: 2, PQ
Antimalarial activity against liver stage of Plasmodium berghei infected in human Huh7 cells after 48 hrs by luciferase assay
Antimalarial activity against liver stage of Plasmodium berghei infected in human Huh7 cells after 48 hrs by luciferase assay
[PMID: 24900781]
Huh-7 IC50
7500 nM
Compound: PQ
Antiplasmodial activity against liver stage of Plasmodium berghei infected in human HuH7 cells assessed as parasite growth inhibition incubated for 1 hr prior to parasite infection measured after 48 hrs
Antiplasmodial activity against liver stage of Plasmodium berghei infected in human HuH7 cells assessed as parasite growth inhibition incubated for 1 hr prior to parasite infection measured after 48 hrs
[PMID: 24020770]
Huh-7 IC50
8 μM
Compound: PQ
Antiplasmodial activity against liver stage of Plasmodium berghei expressing GFP-Luc infected in HuH7 cells incubated at 1 hr prior to infection followed by compound replenisment at 24 hrs post-infection measured after 48 hrs by Alamar blue assay
Antiplasmodial activity against liver stage of Plasmodium berghei expressing GFP-Luc infected in HuH7 cells incubated at 1 hr prior to infection followed by compound replenisment at 24 hrs post-infection measured after 48 hrs by Alamar blue assay
[PMID: 23290049]
Huh-7 IC50
8.428 μM
Compound: PQ
Antiplasmodial activity against liver-stage of Plasmodium berghei expressing firefly luciferase infected in human Huh-7 cells after 48 hrs by bioluminescence assay
Antiplasmodial activity against liver-stage of Plasmodium berghei expressing firefly luciferase infected in human Huh-7 cells after 48 hrs by bioluminescence assay
[PMID: 26142491]
Huh-7 IC50
9.5 μM
Compound: 1
Antiplasmodial activity against liver stage Plasmodium berghei infected in Huh7 cells assessed as inhibition of parasite infection incubated for 1 hr prior to infection measured at 24 hrs by luciferase reporter gene assay
Antiplasmodial activity against liver stage Plasmodium berghei infected in Huh7 cells assessed as inhibition of parasite infection incubated for 1 hr prior to infection measured at 24 hrs by luciferase reporter gene assay
[PMID: 26968650]
MCF7 IC50
6.9 μM
Compound: 1
Antitumor activity against human MCF7 cells after 48 hours hrs by SRB assay
Antitumor activity against human MCF7 cells after 48 hours hrs by SRB assay
[PMID: 19896373]
RAW264.7 IC50
38.7 μg/mL
Compound: 2, PQ
Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay
[PMID: 21141892]
Vero IC50
≤ 23.8 μg/mL
Compound: 1, PQ
Cytotoxicity against African green monkey Vero cells by neutral red uptake assay
Cytotoxicity against African green monkey Vero cells by neutral red uptake assay
10.1039/C0MD00267D
Vero IC50
339.7 μM
Compound: PQ, primaquine
Cytotoxicity against african green monkey Vero cells assessed as [3H]hypoxanthine incorporation after 48 hrs
Cytotoxicity against african green monkey Vero cells assessed as [3H]hypoxanthine incorporation after 48 hrs
[PMID: 18653332]
體外研究
(In Vitro)

Primaquine 顯著降低活乳腺癌細(xì)胞的增殖，對 MCF-7 (ER+) 和 MDA-MB-453 (HER2+) 細(xì)胞的增殖沒有抑制作用。Primaquine 在體外抑制乳腺癌細(xì)胞的生長、遷移和集落形成[3]。

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

Cell Viability Assay[3]

Cell Line: MDA-MB-231, HCC1937 cells, MCF-7, and MDA-MB-453 cells
Concentration: 5 μM, 10 μM, 20 μM, 40 μM, 80 μM, 100 μM, 120 μM, and 150 μM
Incubation Time: 24 h
Result: Decreases breast cancer cell viability.
體內(nèi)研究
(In Vivo)

Primaquine （5-25 mg/kg；口服；每日；持續(xù) 3 天）沒有顯示肝臟生物發(fā)光信號，也沒有血液階段寄生蟲血癥[2]。

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

Animal Model: Male 6-week-old C57BL/6 albino mice with sporozoite inoculation[2]
Dosage: 5 mg/kg, 10 mg/kg, 15 mg/kg, 20 mg/kg, and 25 mg/kg
Administration: p.o; daily; for 3 days
Result: No blood stage parasitaemia was observed.
Clinical Trial
分子量

259.35

Formula

C15H21N3O
CAS 號
性狀

<25°C 固體,>25°C 液體

顏色

Light brown to yellow

運(yùn)輸條件

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

4°C, protect from light

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

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 250 mg/mL (963.95 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 3.8558 mL 19.2790 mL 38.5579 mL
5 mM 0.7712 mL 3.8558 mL 7.7116 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)。-80°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲存時(shí)，請?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)

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(dòng)物實(shí)驗(yàn)：

請根據(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(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (8.02 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    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(dòng)物溶解方案計(jì)算器
請輸入動(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

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請輸入您的動(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 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(jì)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)

您所需的儲備液濃度超過該產(chǎn)品的實(shí)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(dòng)物實(shí)驗(yàn)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(jǐn)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: 98.85%

參考文獻(xiàn)

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)。-80°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲存時(shí)，請?jiān)?個(gè)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 3.8558 mL 19.2790 mL 38.5579 mL 96.3948 mL
5 mM 0.7712 mL 3.8558 mL 7.7116 mL 19.2790 mL
10 mM 0.3856 mL 1.9279 mL 3.8558 mL 9.6395 mL
15 mM 0.2571 mL 1.2853 mL 2.5705 mL 6.4263 mL
20 mM 0.1928 mL 0.9639 mL 1.9279 mL 4.8197 mL
25 mM 0.1542 mL 0.7712 mL 1.5423 mL 3.8558 mL
30 mM 0.1285 mL 0.6426 mL 1.2853 mL 3.2132 mL
40 mM 0.0964 mL 0.4820 mL 0.9639 mL 2.4099 mL
50 mM 0.0771 mL 0.3856 mL 0.7712 mL 1.9279 mL
60 mM 0.0643 mL 0.3213 mL 0.6426 mL 1.6066 mL
80 mM 0.0482 mL 0.2410 mL 0.4820 mL 1.2049 mL
100 mM 0.0386 mL 0.1928 mL 0.3856 mL 0.9639 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：
Primaquine
目錄號：
HY-12651A
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