2. Anti-infection Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Parasite Reactive Oxygen Species
  4. PT4

PT4 是一种抗皮肤利什曼病 (CL) 的化合物。PT4 对两种 Leishmania 均有效，对 L. amazonensis 和 L. braziliensis 的 IC50 分别为 125.18 和 233.18 μM。PT4 降低线粒体膜电位且提高活性氧产生，导致寄生虫死亡。PT4 具有有效的体内抗炎活性。

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PT4 Chemical Structure

PT4 Chemical Structure

CAS No. : 1280738-47-7

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PT4 相关抗体

Top Publications Citing Use of Products

查看 Parasite 亚型特异性产品:

查看所有亚型
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

细胞效力
(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]
体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PT4 相关抗体:

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.
体内研究
(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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

318.33

Formula

C18H14N4O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PT4 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

PT41280738-47-7PT 4PT-4ParasiteReactive Oxygen SpeciesAntileishmanial activityCutaneous leishmaniasisLeishmaniaanti-inflammatoryInhibitorinhibitorinhibit

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