DHFR-IN-5
Based on 1 Customer Validation
DHFR-IN-5 is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 shows anti-malaria activity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.27%
- CAS 番号: 1142407-81-5
- 分子式: C18H24N4O4
- 分子量:360.41
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero | IC50 |
>100 μM
Compound: P218
|
Cytotoxicity against African green monkey Vero cells assessed as cell growth inhibition incubated for 72 hrs by sulforhodamine B assay
Cytotoxicity against African green monkey Vero cells assessed as cell growth inhibition incubated for 72 hrs by sulforhodamine B assay
|
[PMID: 37731689] |
| Vero | IC50 |
>100 μM
Compound: P218
|
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability
|
[PMID: 39026651] |
体外実験
DHFR-IN-5 (compound p218) shows highly active against PYR-resistant P. falciparum with IC50s of 4.6, 56 nM for wild-type P. falciparum (TM4), quadruple mutant P. falciparum (V1/S), respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1]
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Dosage:30 mg/kg
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Administration:P.o.
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Result:Showed good oral bioavailability (46.3%), a reasonable half-life (7.3 h), and minimal distribution into the brain.
化学情報
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CAS 番号 1142407-81-5
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性状 Solid
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分子量 360.41
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分子式 C18H24N4O4
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Color Off-white to gray
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SMILES
O=C(CCC1=C(OCCCOC2=C(CC)N=C(N)N=C2N)C=CC=C1)O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (277.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7746 mL | 13.8731 mL | 27.7462 mL | 69.3654 mL |
| 5 mM | 0.5549 mL | 2.7746 mL | 5.5492 mL | 13.8731 mL | |
| 10 mM | 0.2775 mL | 1.3873 mL | 2.7746 mL | 6.9365 mL | |
| 15 mM | 0.1850 mL | 0.9249 mL | 1.8497 mL | 4.6244 mL | |
| 20 mM | 0.1387 mL | 0.6937 mL | 1.3873 mL | 3.4683 mL | |
| 25 mM | 0.1110 mL | 0.5549 mL | 1.1098 mL | 2.7746 mL | |
| 30 mM | 0.0925 mL | 0.4624 mL | 0.9249 mL | 2.3122 mL | |
| 40 mM | 0.0694 mL | 0.3468 mL | 0.6937 mL | 1.7341 mL | |
| 50 mM | 0.0555 mL | 0.2775 mL | 0.5549 mL | 1.3873 mL | |
| 60 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1561 mL | |
| 80 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8671 mL | |
| 100 mM | 0.0277 mL | 0.1387 mL | 0.2775 mL | 0.6937 mL |