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My CartCAS：500-92-5
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 500-92-5 |
| Name | Proguanil |
| Molecular Formula | C11H16ClN5 |
| Molecular Weight | 253.73 |
| Solubility | Soluble in DMSO(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 207-915-6 |
| MDL | MFCD00133609 |
| SMILES | CC(C)N=C(N)N=C(N)NC1=CC=C(C=C1)Cl |
| InChIKey | SSOLNOMRVKKSON-UHFFFAOYSA-N |
| InChI | InChI=1S/C11H16ClN5/c1-7(2)15-10(13)17-11(14)16-9-5-3-8(12)4-6-9/h3-7H，1-2H3，(H5，13，14，15，16，17) |
| PubChem CID | 6178111 |
| Target Point | Parasite |
| Passage | Anti-infection |
| Background | Proguanil inhibits the parasites dihydrofolate reductase, preventing the synthesis of purines and pyrimidines. |
| Biological Activity | Proguanil 是一种抗疟原药，经代谢可生成活性代谢物 Cycloguanil，也是一种二氢叶酸还原酶（DHFR）抑制剂。[1-2] |
| In Vitro | 氯胍本身在体外只有微弱的抗疟活性(IC50 2.4-19 微摩尔)，其有效性取决于活性代谢物环戊胍(IC50 0.5-2.5 毫微微摩尔)。阿托伐醌和氯胍的组合具有协同作用。这两种药物对配子细胞和疟原虫的红细胞前期(肝)也有活性。[1]阿托伐醌-氯胍复方制剂以选择性的方式作为寄生虫线粒体的特异性解偶联剂，原药形式的氯胍与阿托伐醌协同作用，降低了阿托伐醌使疟原虫体内 DeltaPsim 崩溃的有效浓度。[2]氯胍 5-HT3 受体有竞争性抑制作用，其 IC50 值为 1.81 μM。代谢物 4-氯苯基-1-双胍(CPB)和环戊胍(CG)对 5-HT3 受体具有类似的抑制作用。在较高浓度下，CPB 是一种部分激动剂(EC50 = 14.1 μM；I/Imax = 0.013)。[3]用 0.3 μM 至 10 μM 的氯胍处理 16 至 18 日龄大鼠的绒毛膜细胞 5 天，存活率和 DNA 完整性的降低。[4] |
| In Vivo | 十至十二周大的雄性大鼠每天注射氯胍(2.9 毫克/千克体重)，分别持续五天和六周，睾丸和附睾也出现了持续时间依赖性退化，在恢复实验中得以恢复。[4]研究评估了阿托伐醌(ATV)和氯胍(PG)联合疗法对未封闭的野生型和ATV抗性的 B.gibsoni 具有协同作用。对实验性 B.gibsoni 感染的两只慢性期狗和三只急性期狗服用马拉隆(阿托伐醌和氯胍)后，寄生虫血症下降，临床症状也有所改善。[5] |
| Data Literature Source | [1]. Pudney M，et al. Atovaquone and proguanil hydrochloride: a review of nonclinical studies. J Travel Med. 1999 May;6 Suppl 1:S8-12. [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. [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. [4]. Stephen AO，et al. Prolonged administration of proguanil induces reproductive toxicity in male rats. J Toxicol Sci. 2011 Oct;36(5):587-99. [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. |
| Unit | Bottle |
| Specification | 10mg 25mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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