Primaquine Diphosphate

製品コードS4237 バッチS423701

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₅H₂₁N₃O.2H₃O₄P
	分子量	455.34	CAS No.	63-45-6
Solubility (25°C)*	体外	DMSO	91 mg/mL (199.85 mM)
		Water	91 mg/mL (199.85 mM)
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Primaquine Diphosphate is a transmission-blocking anti-malarial clinically available, displaying a marked activity against gametocytes of all species of human malaria.
in vitro	Primaquine is still the only transmission-blocking anti-malarial clinically available, displaying a marked activity against gametocytes of all species of human malaria, including multi-resistant Plasmodium falciparum strains. Primaquine is also effective against all exoerythrocytic forms of the parasite and is used in conjunction with other anti-malarials for the treatment of vivax and ovale malaria. The exact mechanism by which Primaquine so effectively eliminates Plasmodium falciparum and gametocytes is still unknown, but it is thought that metabolism at the parasites’ mitochondria is impaired, eventually by interference with the ubiquinone function as an electron carrier in the respiratory chain. Another potential mechanism of anti-malarial action by Primaquine is the production of highly reactive metabolites that generate intracellular oxidative potentials. Primaquine is found to be an inhibitor of vesicular transport and blocks the calcium-release-activated current in rat megakaryocytes. Primaquine also acts on cardiac Na⁺ channels in isolated rat ventricular muscle and myocytes. Primaquine inhibits protein transport with IC50 of 50 μM, and inhibits the budding of vesicles from the donor membranes. PQ has a strong inhibitory effect on the recycling of endocytosed proteins to the plasma membrane. Primaquine is able to inhibit the potassium current by blockade of muscarinic receptors. Primaquine also inhibit human erythrocyte membrane acetylcholinesterase (AChE) with IC33 of 30 μM. Primaquine is a nitrite-reacting mutagen precursor where the secondary amino group plays a key role. ^[1]

製品説明

Primaquine Diphosphate is a transmission-blocking anti-malarial clinically available, displaying a marked activity against gametocytes of all species of human malaria.

in vitro

Primaquine is still the only transmission-blocking anti-malarial clinically available, displaying a marked activity against gametocytes of all species of human malaria, including multi-resistant Plasmodium falciparum strains. Primaquine is also effective against all exoerythrocytic forms of the parasite and is used in conjunction with other anti-malarials for the treatment of vivax and ovale malaria. The exact mechanism by which Primaquine so effectively eliminates Plasmodium falciparum and gametocytes is still unknown, but it is thought that metabolism at the parasites’ mitochondria is impaired, eventually by interference with the ubiquinone function as an electron carrier in the respiratory chain. Another potential mechanism of anti-malarial action by Primaquine is the production of highly reactive metabolites that generate intracellular oxidative potentials. Primaquine is found to be an inhibitor of vesicular transport and blocks the calcium-release-activated current in rat megakaryocytes. Primaquine also acts on cardiac Na⁺ channels in isolated rat ventricular muscle and myocytes. Primaquine inhibits protein transport with IC50 of 50 μM, and inhibits the budding of vesicles from the donor membranes. PQ has a strong inhibitory effect on the recycling of endocytosed proteins to the plasma membrane. Primaquine is able to inhibit the potassium current by blockade of muscarinic receptors. Primaquine also inhibit human erythrocyte membrane acetylcholinesterase (AChE) with IC33 of 30 μM. Primaquine is a nitrite-reacting mutagen precursor where the secondary amino group plays a key role. ^[1]

プロトコル(参考用のみ)

参考

[1] Vale N, et al. Eur J Med Chem, 2009, 44(3), 937-953.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Primaquine Diphosphate, a Known Antimalarial Drug, Blocks Vascular Leakage Acting Through Junction Stabilization [ Front Pharmacol, 2021, 12:695009]	PubMed: 34149436
Quantifying Drug Combination Synergy along Potency and Efficacy Axes. [ Cell Syst, 2019, 8(2):97-108]	PubMed: 30797775

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。