产品
编 号：F743777
分子式：C18H14N4O2
分子量：318.33
分子式：C18H14N4O2
分子量：318.33
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CAS No: 1280738-47-7
产品详情
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.
体内研究：
The pharmacokinetic and toxicological parameters of PT4 Parameter
HBA (≤10)4
HBD (≤5)0
LogP (≤5)2.23
MW (≤500) g/mol318.33
n-ROTB (≤10)4
TPSA (A2)68.09
BBBYes
GIAHigh
P-GP substrateNo
Skin permeability (cm/s)-6.85
CYP450 2C9 inhibitorYes
CYP450 2D6 inhibitorNo
CYP450 2C19 inhibitorYes
CYP450 3A4 inhibitorNo
CYP450 1A2 inhibitorYes
Total Clearance (log ml/min/kg)0.117
Renal OCT2 substrateNo
LD50 (mg/Kg)4700
体外研究：
PT4 (0-1256.5 μM, 48 hours) can inhibit mammalian cells viability.PT4 (314.1-19.6 μM, 48 hours) inhibits the growth of promastigote and amastigote of L. amazonensis and L. braziliensis promastigotes.PT4 causes depolarization of the mitochondrial membrane of L. amazonensis and L. braziliensis promastigotes and increasing ROS in mitochondria.
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.
体内研究：
The pharmacokinetic and toxicological parameters of PT4 Parameter
HBA (≤10)4
HBD (≤5)0
LogP (≤5)2.23
MW (≤500) g/mol318.33
n-ROTB (≤10)4
TPSA (A2)68.09
BBBYes
GIAHigh
P-GP substrateNo
Skin permeability (cm/s)-6.85
CYP450 2C9 inhibitorYes
CYP450 2D6 inhibitorNo
CYP450 2C19 inhibitorYes
CYP450 3A4 inhibitorNo
CYP450 1A2 inhibitorYes
Total Clearance (log ml/min/kg)0.117
Renal OCT2 substrateNo
LD50 (mg/Kg)4700
体外研究：
PT4 (0-1256.5 μM, 48 hours) can inhibit mammalian cells viability.PT4 (314.1-19.6 μM, 48 hours) inhibits the growth of promastigote and amastigote of L. amazonensis and L. braziliensis promastigotes.PT4 causes depolarization of the mitochondrial membrane of L. amazonensis and L. braziliensis promastigotes and increasing ROS in mitochondria.
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