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  3. DSM265

DSM265 

製品番号: HY-100184 純度: 99.59%
取扱説明書

DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 of 8.9 nM. DSM265 can also inhibit the growth of Pf3D7 parasites with an EC50 of 4.3 nM.

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DSM265 構造式

DSM265 構造式

CAS 番号 : 1282041-94-4

容量 価格(税別) 在庫状況 数量
10 mM * 1  mL in DMSO USD 302 在庫あり
Estimated Time of Arrival: December 31
1 mg USD 110 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 330 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 500 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 1000 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1500 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 2100 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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製品説明

DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 of 8.9 nM. DSM265 can also inhibit the growth of Pf3D7 parasites with an EC50 of 4.3 nM[1][2].

IC50 & Target

IC50: 8.9 nM (PfDHODH)[1]
EC50: 4.3 nM (P. falciparum 3D7 parasites)[1]

体内実験

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).
臨床実験
分子量

415.33

分子式

C₁₄H₁₂F₇N₅S

CAS 番号

1282041-94-4

SMILES

CC1=NC2=NC(C(C)(F)F)=NN2C(NC3=CC=C(S(F)(F)(F)(F)F)C=C3)=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 50 mg/mL (120.39 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4077 mL 12.0386 mL 24.0772 mL
5 mM 0.4815 mL 2.4077 mL 4.8154 mL
10 mM 0.2408 mL 1.2039 mL 2.4077 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (6.62 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (6.62 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
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Keywords:

DSM265DSM 265DSM-265ParasiteInhibitorinhibitorinhibit

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製品名:
DSM265
製品番号:
HY-100184
数量:
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