DM-1157
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1239953-66-2
- 分子式: C28H31ClN6
- 分子量:487.04
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
DM-1157 (Compound 22) (0.9-1.8 nM; 72 h) potently inhibits growth of chloroquine-sensitive D6, chloroquine-resistant Dd2, and chloroquine-resistant 7G8 Plasmodium falciparum strains in vitro with normalized IC50 values of 0.9 nM, 1.6 nM, and 1.8 nM, respectively[1].
DM-1157 (6500 nM) has a low in vitro cytotoxicity against murine spleenic lymphocytes, with a cytotoxicity IC50 of 6500 nM and a therapeutic index of 4060 relative to its antimalarial activity against Dd2 Plasmodium falciparum[1].
DM-1157 (10-50 nM; 24 h) potently inhibits hemozoin production in synchronized chloroquine-sensitive D6 and chloroquine-resistant Dd2 Plasmodium falciparum strains in vitro, with near-complete inhibition at 10 nM and complete inhibition at 50 nM, while inducing digestive vacuole enlargement[1].
DM-1157 (72 h) potently inhibits in vitro growth of chloroquine-sensitive P. falciparum D6 (IC50 = 0.2 nM) and chloroquine-resistant P. falciparum Dd2 (IC50 = 2.2 nM) and 7G8 (IC50 = 1.8 nM) strains, and shows cytotoxicity against mouse spleen lymphocytes with an LC50 of 6500 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NMRI (female)[1]
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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)
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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)
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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.
化学情報
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CAS 番号 1239953-66-2
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分子量 487.04
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分子式 C28H31ClN6
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SMILES
ClC1=CC2=NC=CC(NCCCN3CCC(CC3)NC(C4=NC=CC=C4)C5=NC=CC=C5)=C2C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Burgess SJ, et al. Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. J Med Chem. 2010;53(17):6477-6489. [Content Brief]
[2].
Liebman KM, et al. Unsymmetrical Bisquinolines with High Potency against P. falciparum Malaria. Molecules. 2020 May 10;25(9):2251.
[Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
DM-1157 関連分類
HY-182394 関連分類
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