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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- No. CAS: 1239953-66-2
- Fòrmula: C28H31ClN6
- Peso molecular:487.04
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
In Vitro
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.
In Vivo
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.
Chemical Information
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No. CAS 1239953-66-2
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Peso molecular 487.04
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DM-1157 Related Classifications
HY-182394 Related Classifications
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