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My CartCAS：5355-16-8
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 | 5355-16-8 |
| Name | Diaveridine |
| Molecular Formula | C13H16N4O2 |
| Molecular Weight | 260.29 |
| Solubility | Soluble in DMSO ≥2mg/mL(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 226-333-3 |
| MDL | MFCD00057349 |
| SMILES | NC1=NC=C(CC2=CC=C(OC)C(OC)=C2)C(N)=N1 |
| InChIKey | LDBTVAXGKYIFHO-UHFFFAOYSA-N |
| InChI | InChI=1S/C13H16N4O2/c1-18-10-4-3-8(6-11(10)19-2)5-9-7-16-13(15)17-12(9)14/h3-4,6-7H,5H2,1-2H3,(H4,14,15,16,17) |
| PubChem CID | 21453 |
| Target Point | Parasite;DHFR |
| Passage | Anti-infection |
| Background | Diaveridine is a coccidiostatic compound with antiparasitic activity and is a dihydrofolate reductase (DHFR) inhibitor. |
| Biological Activity | Diaveridine (EGIS-5645) 是二氢叶酸还原酶 (DHFR) 的抑制剂，对于野生型 DHFR 的 Ki 值为 11.5 nM，Diaveridine 也是一种抗菌剂。[1-3] |
| In Vitro | Diaveridine是一种二氢叶酸还原酶(DHFR)抑制剂，野生型DHFR的Ki为11.5 nM，也是一种抗菌剂[1]。用Diaveridine处理90分钟对鼠伤寒沙门氏菌TA1535具有强烈的杀菌作用，并且在10μg/ mL或更高时未观察到细菌生长。没有代谢活化，用替尼定治疗48小时，但不是24小时，导致异常中期的频率呈剂量依赖性，显著增加。在100μg/ mL时，60％的中期细胞含有染色体畸变[2]。 |
| In Vivo | 所有剂量水平的替尼定(DVD)治疗组的精子异常(Diaveridine，128至512mg / kg)显示与阴性对照组相比没有显著差异。阴性对照组和Diaveridine治疗组(Diaveridine，128至512mg / kg)之间的微核没有显著差异。所有剂量水平的双乙酰定处理组和阴性对照组的染色体畸变均显著低于用环磷酰胺处理的阳性对照组(P <0.05)，表明所研究剂量的Diaveridine不会引起异常的染色体畸变。结果表明，与研究结束时期的阴性对照组相比，替维尼定给药不会引起器官与体重比值的显著变化[3]。 |
| Cell Experiment | 将细胞在37℃，5％CO 2的空气湿润气氛中培养。生长培养基是Eagle's MEM，补充有10％胎牛血清。在没有代谢活化的实验中，将细胞连续处理24或48小时而不改变培养基。在代谢活化的实验中，用不同剂量的测试化合物(包括Diaveridine)脉冲处理细胞6小时，并在新鲜培养基中孵育18小时。破碎型染色单体畸变，交换型染色单体畸变，破损型染色体畸变和交换型染色体畸变评分。差距也计算在内。有丝分裂指数由2000个细胞评分确定[2]。 |
| Animal Experiment | 将50只体重25至35g的雄性ICR小鼠随机分成5组，每组10只小鼠。实验组中的小鼠分别通过IG以128mg / kg(低剂量)，256mg / kg(中剂量)和512mg / kg(高剂量)体重接受Diaveridine(DVD)连续5天。阴性和阳性对照组中的小鼠分别接受IG 1％CMC-Na溶剂和40mg / kg体重的环磷酰胺。给予试验组0.2mL / 10g双乙脒(与1％CMC-Na混合，得到2mg / mL的浓度)，体重，每天一次，共5天。行为变化每天记录[3]。 |
| Data Literature Source | [1]. Sirichaiwat C et al. Target guided synthesis of 5-benzyl-2，4-diamonopyrimidines: their antimalarial activities and binding affinities to wild type and mutant dihydrofolate reductases from Plasmodium falciparum. J Med Chem 47:345-54 (2004). [2]. Ono T，et al. The genotoxicity of diaveridine and trimethoprim. Environ Toxicol Pharmacol. 1997 Sep;3(4):297-306. [3]. Wang J，et al. Acute，mutagenicity，teratogenicity and subchronic oral toxicity studies of diaveridine in rodents. Environ Toxicol Pharmacol. 2015 Sep;40(2):660-70 |
| Unit | Bottle |
| Specification | 250mg 500mg 1g |
Diaveridine是一种球虫抑制化合物，具有抗寄生虫活性，是dihydrofolate reductase (DHFR)抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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