DSM705


Catalog No. Size PriceQuantity
M16956-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

DSM705 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 exhibits nanomolar potency against Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs. DSM705 is a potent antimalarial compound.

Product information

Molecular Weight: 404.39

Formula: C19H19F3N6O

Chemical Name: 3-methyl-N-[(1R)-1-(1H-1, 2, 4-triazol-5-yl)ethyl]-4-[1-[6-(trifluoromethyl)pyridin-3-yl]cyclopropyl]-1H-pyrrole-2-carboxamide

Smiles: CC1C(=CNC=1C(=O)N[C@H](C)C1NN=CN=1)C1(CC1)C1=CC=C(N=C1)C(F)(F)F

InChiKey: JUBPRXDFKLPILK-LLVKDONJSA-N

InChi: InChI=1S/C19H19F3N6O/c1-10-13(8-24-15(10)17(29)27-11(2)16-25-9-26-28-16)18(5-6-18)12-3-4-14(23-7-12)19(20,21)22/h3-4,7-9,11,24H,5-6H2,1-2H3,(H,27,29)(H,25,26,28)/t11-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

DSM705 shows inhibitory activity against P. falciparum DHODH (PfDHODH, IC50=95 nM), P. vivax DHODH (PvDHODH, IC50=52 nM) and Pf3D7 cells (EC50=12 nM), with no inhibition of the human enzyme.

In Vivo:

DSM705 (3-200 mg/kg; p.o. twice a day for 6 days) provides the maximum rate of parasite killing at the dose of 50 mg/kg and fully suppresses parasitemia by days 7-8. DSM705 (2.6 and 24 mg/kg; a single p.o.) exhibits high oral bioavailability (74%, 70%), apparent t1/2 (3.4, 4.5 h) and Cmax (2.6, 20 μM) in Swiss outbred mice. DSM705 (2.3 mg/kg; a single i.v.) exhibits plasma clearance (CL=2.8 mL/min/kg) and Vss (1.3 L/kg) in mice.

Products are for research use only. Not for human use.

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