产品
编 号：F753154
分子式：C22H24ClN7O2
分子量：453.92
分子式：C22H24ClN7O2
分子量：453.92
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CAS No: 2482998-35-4
产品详情
生物活性：
HDAC1-IN-3 is a potent Pf HDAC1 inhibitor. HDAC1-IN-3 shows antimalarial activity in wild-type and multidrug-resistant parasite strains. HDAC1-IN-3 shows a significant in vivo killing effect against all life cycles of parasites.
体内研究：
HDAC1-IN-3 (30, 60, 90 mg/kg; i.p.; once daily for 5 days) shows acceptable therapeutic efficacy and safety.HDAC1-IN-3 (5 mg/kg; i.p.) shows good pharmacokinetic properties.Pharmacokinetic Parameters of HDAC1-IN-3 in Female BALB/c mice.parameter JX35
Cmax (ng/mL)539
Tmax (h)0.25
AUC last (h·ng/mL)638
AUC inf (h·ng/mL)640
t1/2 (h)0.91
CLZ/F (L/h/kg)7.81
VZ/F (L/kg)10.20
Female BALB/c mice; 5 mg/kg; i.p.Animal Model:6-8 weeks, BALB/c female mice
Dosage:30, 60, 90 mg/kg
Administration:I.p., once daily for 5 days
Result:Showed acceptable therapeutic efficacy and safety.
Animal Model: 6-8 weeks, female BALB/c mice
Dosage:5 mg/kg
Administration:I.p.
Result:Showed good pharmacokinetic properties.
体外研究：
HDAC1-IN-3 (compound JX35) shows antimalarial activity with IC50s of 1.26 nM and 1.61 nM for wild-type Plasmodium falciparum (P. falciparum) parasite 3D7 and chloroquine-resistant P. falciparum parasite Dd2, respectively.HDAC1-IN-3 (10 μM; 72 h) shows low cytotoxicity with IC50s of 1.02 μM and 1.21 μM for HepG2, 293T cells, respectively.HDAC1-IN-3 (72 h) shows no cross-resistance with clinical antimalarial drugs with IC50s of 3.06, 2.18, 5.85 nM for GB4, C2A, CP286, respectively.HDAC1-IN-3 (10, 30, 60, 100 nM; 3, 6, 12, 24 h) shows antimalarial activity in a time- and dose-dependent manner with asynchronous 3D7 parasites.HDAC1-IN-3 (40 nM, 4 days; P. falciparum 3D7 cells) shows the killing effects of JX35 on P. falciparum parasites during asexual reproduction stages might be related to the inhibition of schizont growth and reinvasion of RBCs (red blood cells).HDAC1-IN-3 (5, 20 nM; 4 h) inhibits the expression of Pf HDAC against ART (artemisinin)-resistant parasite strains.HDAC1-IN-3 reduces the inhibition of hHDACs with IC50s of 2.2, 5.1, 5.2, 85.5, 29.9 nM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively.
HDAC1-IN-3 is a potent Pf HDAC1 inhibitor. HDAC1-IN-3 shows antimalarial activity in wild-type and multidrug-resistant parasite strains. HDAC1-IN-3 shows a significant in vivo killing effect against all life cycles of parasites.
体内研究：
HDAC1-IN-3 (30, 60, 90 mg/kg; i.p.; once daily for 5 days) shows acceptable therapeutic efficacy and safety.HDAC1-IN-3 (5 mg/kg; i.p.) shows good pharmacokinetic properties.Pharmacokinetic Parameters of HDAC1-IN-3 in Female BALB/c mice.parameter JX35
Cmax (ng/mL)539
Tmax (h)0.25
AUC last (h·ng/mL)638
AUC inf (h·ng/mL)640
t1/2 (h)0.91
CLZ/F (L/h/kg)7.81
VZ/F (L/kg)10.20
Female BALB/c mice; 5 mg/kg; i.p.Animal Model:6-8 weeks, BALB/c female mice
Dosage:30, 60, 90 mg/kg
Administration:I.p., once daily for 5 days
Result:Showed acceptable therapeutic efficacy and safety.
Animal Model: 6-8 weeks, female BALB/c mice
Dosage:5 mg/kg
Administration:I.p.
Result:Showed good pharmacokinetic properties.
体外研究：
HDAC1-IN-3 (compound JX35) shows antimalarial activity with IC50s of 1.26 nM and 1.61 nM for wild-type Plasmodium falciparum (P. falciparum) parasite 3D7 and chloroquine-resistant P. falciparum parasite Dd2, respectively.HDAC1-IN-3 (10 μM; 72 h) shows low cytotoxicity with IC50s of 1.02 μM and 1.21 μM for HepG2, 293T cells, respectively.HDAC1-IN-3 (72 h) shows no cross-resistance with clinical antimalarial drugs with IC50s of 3.06, 2.18, 5.85 nM for GB4, C2A, CP286, respectively.HDAC1-IN-3 (10, 30, 60, 100 nM; 3, 6, 12, 24 h) shows antimalarial activity in a time- and dose-dependent manner with asynchronous 3D7 parasites.HDAC1-IN-3 (40 nM, 4 days; P. falciparum 3D7 cells) shows the killing effects of JX35 on P. falciparum parasites during asexual reproduction stages might be related to the inhibition of schizont growth and reinvasion of RBCs (red blood cells).HDAC1-IN-3 (5, 20 nM; 4 h) inhibits the expression of Pf HDAC against ART (artemisinin)-resistant parasite strains.HDAC1-IN-3 reduces the inhibition of hHDACs with IC50s of 2.2, 5.1, 5.2, 85.5, 29.9 nM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively.
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