DSM265 - 99%, high purity , CAS No.1282041-94-4

  • ≥99%
Item Number
D649991
Grouped product items
SKUSizeAvailabilityPrice Qty
D649991-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$80.90
D649991-10mg
10mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$110.90
D649991-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$150.90
D649991-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$250.90
D649991-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$450.90
D649991-250mg
250mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$1,000.90
D649991-500mg
500mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$1,850.90

Basic Description

SynonymsA17069 | SCHEMBL14053411 | UNII-0Q42P4YI6B | BCP17584 | HY-100184 | 1282041-94-4 | DB12397 | 2-(1,1-difluoroethyl)-5-methyl-N-[4-(pentafluoro-$l^{6}-sulfanyl)phenyl]-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine | CS-0018179 | SB17069 | 0Q42P4YI6B | 2-(1,1-DIFL
Specifications & Purity≥99%
Biochemical and Physiological MechanismsDSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase ( Pf DHODH ) with an IC 50 of 8.9 nM. DSM265 can also inhibit the growth of Pf 3D7 parasites with an EC 50 of 4.3 nM.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Product Description

DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase ( Pf DHODH ) with an IC 50 of 8.9 nM. DSM265 can also inhibit the growth of Pf 3D7 parasites with an EC 50 of 4.3 nM

In Vivo

DSM265 (0.5 to 75 mg/kg; Oral administration; twice daily; for 4 days; NOD- scid IL-2Rγ (NSG) mice) has potent in vivo antimalarial activity with 90% effective dose ( ED 90 ) 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 (t 1/2 ) of 2-4 hours for mice (0.5 to 75 mg/kg, oral). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NOD- scid IL-2Rγ (NSG) mice (23-36 g)Dosage: 0.5 to 75 mg/kg Administration: Oral administration; twice daily; for 4 days Result: Had potent antimalarial activity with 90% effective dose ( ED 90 ) of 3 mg/kg per day (1.5 mg/kg twice daily).

Form:Solid

IC50& Target:IC50: 8.9 nM ( Pf DHODH), EC50: 4.3 nM ( P. falciparum 3D7 parasites)

Product Properties

ALogP6.5

Associated Targets(Human)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
DHODH Tclin Dihydroorotate dehydrogenase (2737 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KCNH2 Tclin HERG (29587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CACNA1C Tclin Voltage-gated L-type calcium channel alpha-1C subunit (766 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KCNA5 Tclin Voltage-gated potassium channel subunit Kv1.5 (1353 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ALB Tchem Serum albumin (2651 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SCN5A Tclin Sodium channel protein type V alpha subunit (3462 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HepG2 (196354 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver microsomes (16955 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver (3974 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Plasmodium falciparum (966862 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
L1210 (27553 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Plasmodium cynomolgi (553 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Plasmodium vivax (152 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Plasma (328 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
8238086 Cytochrome P450 (0 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 2-(1,1-difluoroethyl)-5-methyl-N-[4-(pentafluoro-λ6-sulfanyl)phenyl]-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
INCHI InChI=1S/C14H12F7N5S/c1-8-7-11(26-13(22-8)24-12(25-26)14(2,15)16)23-9-3-5-10(6-4-9)27(17,18,19,20)21/h3-7,23H,1-2H3
InChi Key OIZSVTOIBNSVOS-UHFFFAOYSA-N
Canonical SMILES CC1=NC2=NC(=NN2C(=C1)NC3=CC=C(C=C3)S(F)(F)(F)(F)F)C(C)(F)F
Isomeric SMILES CC1=NC2=NC(=NN2C(=C1)NC3=CC=C(C=C3)S(F)(F)(F)(F)F)C(C)(F)F
PubChem CID 51347395
Molecular Weight 415.33

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilityDMSO : 50 mg/mL (120.39 mM; Need ultrasonic) Ethanol : 11.11 mg/mL (26.75 mM; Need ultrasonic)

Safety and Hazards(GHS)

Pictogram(s) GHS08,   GHS07
Signal Danger
Hazard Statements

H315:Causes skin irritation

H319:Causes serious eye irritation

H360:May damage fertility or the unborn child

Precautionary Statements

P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

P280:Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352:IF ON SKIN: wash with plenty of water.

P321:Specific treatment (see ... on this label).

P405:Store locked up.

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P362+P364:Take off contaminated clothing and wash it before reuse.

P203:Obtain, read and follow all safety instructions before use.

P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes.

P318:if exposed or concerned, get medical advice.

P337+P317:If eye irritation persists: Get medical help.

P332+P317:If skin irritation occurs: Get medical help.

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Solution Calculators