Company Name: |
Changzhou Chenhong Biotechnology Co., Ltd.
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Tel: |
0519-85788828 13775037613 |
Email: |
sales@chemrenpharm.com |
Products Intro: |
Product Name:DSM502 CAS:2426616-55-7 Purity:99% Package:50mg;100mg;250mg;500mg;1g;5g
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Company Name: |
Nantong QuanYi Biotechnology Co., Ltd
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Tel: |
0513-66337626 18051384581 |
Email: |
sales@chemhifuture.com |
Products Intro: |
Product Name:DSM502 CAS:2426616-55-7 Purity:98%+ HPLC Package:10mg,500mg,1g,2g,5g,10g,more
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| 1H-Pyrrole-2-carboxamide, N-cyclopropyl-3-methyl-4-[[6-(trifluoromethyl)-3-pyridinyl]methyl]- Basic information |
| 1H-Pyrrole-2-carboxamide, N-cyclopropyl-3-methyl-4-[[6-(trifluoromethyl)-3-pyridinyl]methyl]- Chemical Properties |
Boiling point | 447.6±45.0 °C(Predicted) | density | 1.35±0.1 g/cm3(Predicted) | storage temp. | Store at -20°C | solubility | DMSO : 250 mg/mL (773.25 mM; Need ultrasonic) | pka | 15.60±0.50(Predicted) | form | Solid | color | White to off-white |
| 1H-Pyrrole-2-carboxamide, N-cyclopropyl-3-methyl-4-[[6-(trifluoromethyl)-3-pyridinyl]methyl]- Usage And Synthesis |
Biological Activity | DSM502 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM502 exhibits nanomolar potency againsts Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs[1].
DSM502 shows inhibitory activity against P. falciparum DHODH (PfDHODH, IC50=20 nM), P. vivax DHODH (PvDHODH, IC50=14 nM) and Pf3D7 cells (EC50=14 nM), with no inhibition of the human enzyme[1].
DSM502 (10 and 50 mg/kg; p.o. once daily for 4 days) results in 97% parasite clearance in confirmatory SCID study compared to 85% clearance in the GSK study[1].DSM502 (18.3 and 50 mg/kg; a single p.o.) exhibits high oral bioavailability (>100%, >100%), apparent t1/2 (2.6, 3.6 h) and Cmax (8.4, 42.3 μM) in mice[1].DSM502 (2.8 mg/kg; a single i.v.) exhibits apparent t1/2 (2.8 h), plasma clearance (26.1 mL/min/kg), and Vss (1.2 L/kg) in mice[1]. | References | [1]. Kokkonda S, et, al. Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria. J Med Chem. 2020 May 14;63(9):4929-4956. [2]. Palmer MJ, et, al. Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series. J Med Chem. 2021 May 13;64(9):6085-6136. |
| 1H-Pyrrole-2-carboxamide, N-cyclopropyl-3-methyl-4-[[6-(trifluoromethyl)-3-pyridinyl]methyl]- Preparation Products And Raw materials |
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