1. Anti-infection NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. Parasite Reactive Oxygen Species
  3. 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.

For research use only. We do not sell to patients.

PT4 Chemical Structure

PT4 Chemical Structure

CAS No. : 1280738-47-7

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Description

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[1].

Cellular Effect
Cell Line 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]
In Vitro

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.

Cell Cytotoxicity Assay[1]

Cell Line: Balb/c mice peritoneal exudate (mPEC), J774A.1 macrophages, Fibroblasts
Concentration: 0-1256.5 µM
Incubation Time: 48 hours
Result: Inhibited mPEC, J774A.1 and fibroblasts with CC50 value of 981.37 μM, 521.47 μM and 895.17 μM, respectively.

Cell Proliferation Assay[1]

Cell Line: L. amazonensis, L. braziliensis promastigotes
Concentration: 314.1-19.6 μM
Incubation Time: 48 hours
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.
In Vivo

The pharmacokinetic and toxicological parameters of PT4

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.

Molecular Weight

318.33

Formula

C18H14N4O2

CAS No.
SMILES

O=C1N(CCN2N=NC(C3=CC=CC=C3)=C2)C(C4=C1C=CC=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PT4
Cat. No.:
HY-146166
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