PT4
PT4 is a therapeutic agent against Cutaneous leishmaniasis (CL). PT4 is effective against both species of Leishmania, with IC50s of 125.18 and 233.18 μM for L. amazonensis and L. braziliensis, respectively. PT4 decreases of mitochondrial membrane potential and increases production of reactive oxygen species, which leads to parasite death. PT4 has a potent in vivo anti-inflammatory 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。
- CAS 番号: 1280738-47-7
- 分子式: C18H14N4O2
- 分子量:318.33
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Parasite アイソフォーム固有の製品をすべて表示
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| J774.A1 | CC50 |
>500 μM
Compound: 58
|
Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 34171661] |
PT4 (0-1256.5 µM, 48 hours) can inhibit mammalian cells viability[1]. PT4 (314.1-19.6 μM, 48 hours) inhibits the growth of promastigote and amastigote of L. amazonensis and L. braziliensis promastigotes[1]. PT4 causes depolarization of the mitochondrial membrane of L. amazonensis and L. braziliensis promastigotes and increasing ROS in mitochondria[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Balb/c mice peritoneal exudate (mPEC), J774A.1 macrophages, Fibroblasts
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Concentration:0-1256.5 µM
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Incubation Time:48 hours
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Result:Inhibited mPEC, J774A.1 and fibroblasts with CC50 value of 981.37 μM, 521.47 μM and 895.17 μM, respectively.
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Cell Line:L. amazonensis, L. braziliensis promastigotes
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Concentration:314.1-19.6 μM
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Incubation Time:48 hours
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Result:Inhibited promastigote of L. amazonensis and L. braziliensis promastigotes with IC50 value of 70.46 μM and 181.73 μM, respectively. Inhibited amastigote of them with IC50 value of 125.18 μM and 233.18 μM, respectively.
| Parameter | |
| HBA (≤10) | 4 |
| HBD (≤5) | 0 |
| LogP (≤5) | 2.23 |
| MW (≤500) g/mol | 318.33 |
| n-ROTB (≤10) | 4 |
| TPSA (A2) | 68.09 |
| BBB | Yes |
| GIA | High |
| P-GP substrate | No |
| Skin permeability (cm/s) | -6.85 |
| CYP450 2C9 inhibitor | Yes |
| CYP450 2D6 inhibitor | No |
| CYP450 2C19 inhibitor | Yes |
| CYP450 3A4 inhibitor | No |
| CYP450 1A2 inhibitor | Yes |
| Total Clearance (log ml/min/kg) | 0.117 |
| Renal OCT2 substrate | No |
| LD50 (mg/Kg) | 4700 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1280738-47-7
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分子量 318.33
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分子式 C18H14N4O2
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SMILES
O=C1N(CCN2N=NC(C3=CC=CC=C3)=C2)C(C4=C1C=CC=C4)=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
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)