公司官網(wǎng) http://www.staherb.com/ 資質(zhì):HALAL, KOSHER等認(rèn)證
?:19573130018 楊經(jīng)理(微信同號(hào))
中文簡介|Chinese Profile
產(chǎn)品名稱:蒿甲醚(Artemether)
品牌/供應(yīng)商:長沙上禾生物 Staherb
來源:青蒿素(Artemisinin,源自黃花蒿 Artemisia annua L.)半合成衍生物(二氫青蒿素甲基化產(chǎn)物,以 β-蒿甲醚為藥用活性構(gòu)型)
CAS:71963-77-4|分子式:C??H??O?|分子量:298.37
核心功效
高效抗瘧:對瘧原蟲紅細(xì)胞內(nèi)期裂殖體有強(qiáng)大、快速殺滅作用,抗瘧活性約為青蒿素的 6 倍。
主治各型瘧疾:惡性瘧、間日瘧,尤其適用于抗氯喹惡性瘧及兇險(xiǎn)型瘧疾(含腦型瘧)的搶救與聯(lián)合治療(ACTs,如蒿甲醚-苯芴醇)。
脂溶性優(yōu):比青蒿素親脂性更強(qiáng)(cLogP≈2.84),適合油懸肌注、口服制劑及復(fù)方配伍。
體內(nèi)轉(zhuǎn)化:經(jīng)肝臟 CYP3A4/CYP2B6 去甲基化為雙氫青蒿素(DHA),由 DHA 發(fā)揮最終抗瘧活性。
藥理作用
蒿甲醚保留青蒿素類 C12–C13 內(nèi)過氧橋(–O–O–)這一關(guān)鍵抗瘧藥效團(tuán)。進(jìn)入感染紅細(xì)胞后,在瘧原蟲酸性食物泡內(nèi)被血紅蛋白降解釋放的游離鐵/血紅素(Fe2?/FP-IX)激活,開環(huán)產(chǎn)生細(xì)胞毒性有機(jī)自由基/親電中間體,與瘧原蟲蛋白、膜系統(tǒng)形成共價(jià)加合物,破壞表膜-線粒體功能,迅速殺滅蟲體。

English Profile|英文簡介
Product: Artemether (β-Artemether predominant)
Brand/Supplier: Changsha Staherb Natural Ingredients Co., Ltd. (Staherb)
Nature: Semi-synthetic sesquiterpene-lactone derivative of artemisinin (from Artemisia annua L.) — dihydroartemisinin methyl ether.
CAS: 71963-77-4|Formula: C??H??O?|MW: 298.37
Key Benefits / Core Efficacy
Potent antimalarial: Rapid and strong schizonticidal activity against erythrocytic-stage Plasmodium; antimalarial potency ~6× that of artemisinin.
Broad malaria coverage: Effective for P. falciparum and P. vivax, especially chloroquine-resistant falciparum malaria and severe/complicated malaria (including cerebral malaria) when used in ACTs (e.g., artemether-lumefantrine).
Lipophilic pro-drug: Higher lipophilicity than artemisinin (cLogP≈2.84); suitable for oil-based IM injection, oral tablets/capsules, and fixed-dose combinations.
Metabolic activation: Demethylated in vivo by hepatic CYP3A4/CYP2B6 back to dihydroartemisinin (DHA), the true active moiety.
Pharmacological Action
Artemether retains the C12–C13 endoperoxide bridge, the essential antimalarial pharmacophore of artemisins. Inside the parasite-infected erythrocyte, hemoglobin digestion releases ferrous iron / heme (Fe2? / FP-IX), which cleaves the peroxide bridge to generate cytotoxic carbon-centered radicals and electrophiles. These intermediates alkylate parasite proteins and membranes, disrupt the parasitophorous vacuole / mitochondrial function, and cause rapid parasite death.
公司官網(wǎng) http://www.staherb.com/ 資質(zhì):HALAL, KOSHER等認(rèn)證
?:19573130018 楊經(jīng)理(微信同號(hào))