DSM265
- Product Name
- DSM265
- CAS No.
- 1282041-94-4
- Chemical Name
- DSM265
- Synonyms
- DSM265;DSM265,DSM-265;DSM265;DSM265;DSM265;DSM265, 10 mM in DMSO;2-(1,1-Difluoroethyl)-5-methyl-N-[4-(pentafluoro-λ6-sulfanyl)phenyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine;2-(1,1-Difluoroethyl)-5-methyl-N-(4-(pentafluoro-l6-sulfaneyl)phenyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
- CBNumber
- CB73354231
- Molecular Formula
- C14H12F7N5S
- Formula Weight
- 415.33
- MOL File
- 1282041-94-4.mol
DSM265 Property
- storage temp.
- Store at -20°C
- solubility
- DMSO:50.0(Max Conc. mg/mL);120.39(Max Conc. mM)
- form
- A solid
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H360May damage fertility or the unborn child
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
N-Bromosuccinimide Price
- Product number
- D826535
- Product name
- DSM265
- Packaging
- 2.5mg
- Price
- $500
- Updated
- 2021/12/16
- Product number
- 447734
- Product name
- DSM265
- Packaging
- 1mg
- Price
- $602
- Updated
- 2021/12/16
- Product number
- CS-0018179
- Product name
- DSM265
- Purity
- 99.72%
- Packaging
- 5mg
- Price
- $80
- Updated
- 2021/12/16
- Product number
- CS-0018179
- Product name
- DSM265
- Purity
- 99.72%
- Packaging
- 10mg
- Price
- $110
- Updated
- 2021/12/16
- Product number
- CS-0018179
- Product name
- DSM265
- Purity
- 99.72%
- Packaging
- 25mg
- Price
- $150
- Updated
- 2021/12/16
DSM265 Chemical Properties,Usage,Production
Description
DSM265 belongs to a promising class of antimalarials that inhibit the plasmodium dihydroorotate dehydrogenase enzyme required for pyrimidine biosynthesis. Its good in-vitro efficacy, activity on blood and liver stages, pharmacokinetic profile suitable for single dosing, and good tolerability and safety profiles in phase 1 clinical assessments make it one of the most promising drug candidates in the global antimalarial portfolio.[1]
Uses
DSM265, inhibits the growth of P. falciparum 3D7 parasites with an EC50 of 4.3 nM. It is also a PfDHODH inhibitor with an IC50 of 8.9 nM.
Synthesis
DSM-265 has been synthesized by cyclocondensation of ethyl acetoacetate (I) with aminoguanidine hydrochloride (II) in the presence of NaOEt in refluxing EtOH to give 2,3- diamino-6-methylpyrimidin-4(3H)-one (III). Intermediate (III) upon cyclization with ethyl 2,2-difluoropropanoate (IV) using NaOEt in refluxing EtOH and subsequent treatment with HCl yields triazolopyrimidine derivative (V). Compound (V) reacts with POCl3 providing 7-chloro-2-(1,1-difluoroethyl)- 5-methyl[1,2,4]triazolo[1,5-a]pyrimidine (VI), which is finally condensed with 4-aminophenylsulfurpentafluoride (VII) in EtOH at 50 °C.[2]
in vivo
DSM265 (0.5 to 75 mg/kg; Oral administration; twice daily; for 4 days; NOD-scid IL-2Rγnull (NSG) mice) has potent in vivo antimalarial activity with 90% effective dose (ED90) of 3 mg/kg per day (1.5 mg/kg twice daily). The maximum rate of parasite killing occurred at and above a dose of 13 mg/kg per day (6.4 mg/kg twice daily).
DSM265 has moderate terminal elimination half-life (t1/2) of 2-4 hours for mice (0.5 to 75 mg/kg, oral) [2].
| Animal Model: | NOD-scid IL-2Rγnull (NSG) mice (23-36 g)[2] |
| Dosage: | 0.5 to 75 mg/kg |
| Administration: | Oral administration; twice daily; for 4 days |
| Result: | Had potent antimalarial activity with 90% effective dose (ED90) of 3 mg/kg per day (1.5 mg/kg twice daily). |
IC 50
Plasmodium
References
[1] SABINE BÉLARD Michael R. DSM265: a novel drug for single-dose cure of Plasmodium falciparum malaria.[J]. The Lancet. Infectious diseases, 2018: 819-820. DOI:10.1016/S1473-3099(18)30374-8.
[2] R. THAKARE. DSM-265. Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor, Treatment of malaria[J]. Drugs of The Future, 2019, 1 1. DOI:10.1358/DOF.2019.44.2.2941689.
DSM265 Preparation Products And Raw materials
Raw materials
Preparation Products
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