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.
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- CAS No.: 1280738-47-7
- 화학식: C18H14N4O2
- 분자량:318.33
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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All Parasite Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| J774.A1 | CC50 |
>500 μM
Compound: 58
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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
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[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.
Chemical Information
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CAS No. 1280738-47-7
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분자량 318.33
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PT4 Related Classifications
HY-146166 Related Classifications
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