2. Anti-infection
  3. Parasite
  4. DM-1157

DM-1157 是一种口服有效的非对称双喹啉类血红素抑制剂，其 IC50 为 1.6 μM，Kd 为 1.7 μM。DM-1157 可与溶液中的血红素二聚体结合，抑制 β-血晶素形成，抑制恶性疟原虫消化泡中疟色素的形成，在恶性疟原虫消化泡中累积，诱导恶性疟原虫消化泡增大，抑制氯喹 (Chloroquine) (HY-17589A) 敏感型和耐药型恶性疟原虫株的生长。DM-1157 可用于疟疾及恶性疟原虫型疟疾的研究。

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DM-1157

DM-1157 Chemical Structure

CAS No. : 1239953-66-2

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DM-1157 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DM-1157 is an orally active asymmetric bisquinoline heme inhibitor with a IC50 of 1.6 μM and a Kd of 1.7 μM. DM-1157 binds to heme dimers in solution, inhibits β-hematin formation, suppresses hemozoin formation in the digestive vacuole of Plasmodium falciparum, accumulates in the digestive vacuole of Plasmodium falciparum, induces enlargement of the digestive vacuole of Plasmodium falciparum, and inhibits the growth of Chloroquine (HY-17589A)-sensitive and resistant Plasmodium falciparum strains. DM-1157 can be used for the research of malaria and Plasmodium falciparum-type malaria[1][2].

体外研究
(In Vitro)

DM-1157 (Compound 22) (72 h) 可在体外强效抑制氯喹敏感株 D6、氯喹耐药株 Dd2 和氯喹耐药株 7G8 这三种恶性疟原虫菌株的生长，其标准化 IC50 值分别为 0.9 nM、1.6 nM 和 1.8 nM[1]。
DM-1157 对小鼠脾淋巴细胞的体外细胞毒性较低，其细胞毒性 IC50 为 6500 nM，针对 Dd2 恶性疟原虫的抗疟活性相对治疗指数为 4060[1]。
DM-1157(10-50 nM; 24 h) 可在体外强效抑制同步化的氯喹敏感株 D6 和氯喹耐药株 Dd2 恶性疟原虫的疟色素生成，在 10 nM 时抑制作用接近完全，在 50 nM 时则完全抑制，同时会诱导消化泡膨大[1]。
DM-1157 (72 h) 可强效抑制体外培养的氯喹敏感型恶性疟原虫 (P. falciparum) D6 株 (IC50 = 0.2 nM)、氯喹耐药型恶性疟原虫 (P. falciparum) Dd2 株 (IC50 = 2.2 nM) 和 7G8 株 (IC50 = 1.8 nM) 的生长，且对小鼠脾淋巴细胞具有细胞毒性，其 LC50 为 6500 nM[2]。

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

DM-1157 相关抗体:
体内研究
(In Vivo)

DM-1157 (Compound 22) (30-46 mg/kg；口服、皮下注射；单次给药、连续 4 天给药；感染后 24 小时，自感染后第 0 天开始) 在感染 P. berghei 的 NMRI 小鼠中展现出强效的口服及皮下抗疟活性[1]。

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

Animal Model: NMRI (female)[1]
Dosage: 30 mg/kg (single oral dose); 30 mg/kg (single subcutaneous dose); 30 mg/kg (4 consecutive oral doses); 46 mg/kg (4 consecutive oral doses)
Administration: p.o. (single dose, 24h post-infection); s.c. (single dose, 24h post-infection); p.o. (4 consecutive daily doses, starting day 0 post-infection)
Result: Achieved 94% anti-malarial activity and a mean mouse survival time of 7 days.
Achieved 99.3% anti-malarial activity and a mean mouse survival time of 9 days.
Achieved >99.9% anti-malarial activity, with 2 out of 3 mice cured (parasite-free at 30 days post-infection).
Achieved >99.9% anti-malarial activity, with 9 out of 10 mice cured (parasite-free at 30 days post-infection), and the 10th mouse surviving to 29 days post-infection.
分子量

487.04

Formula

C28H31ClN6
CAS 号
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DM-1157 相关分类

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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.

Keywords:

DM-11571239953-66-2DM1157DM 1157ParasiteDd2hemozoinβ-hematinPlasmodium bergheimurine spleenic lymphocyteshemePlasmodium falciparum digestive vacuolesPlasmodium falciparummalariaD6Inhibitorinhibitorinhibit

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