产品
编 号：F485244
分子式：C23H24F3N3O2
分子量：431.45
分子式：C23H24F3N3O2
分子量：431.45
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 862309-06-6
产品详情
生物活性：
MK-0249 (Compound 1) is a potent, selective and orally active histamine H3 receptor antagonist, with an IC50 of 1.7 nM for human H3.
体内研究：
MK-0249 (Compound 1) (0-30 mg/kg; p.o.; once) elevates histamine levels in the rat brain in a dose-dependent manner.MK-0249 (10 mg/kg; p.o.; once) shows markedly higher brain penetrability and a lower plasma Occ90 value in mdr1a (-/-) mice than in mdr1a (+/+) mice.MK-0249 shows rodent brain permeability and is significantly limited by P-gp mediated efflux in rodents, whereas the extent of P-gp mediated efflux in humans should be very small or negligible.Animal Model:SD rats
Dosage:3, 10 and 30 mg/kg
Administration:Oral administration, once
Result:Showed a statistically significant increase in tele-methylhistamine levels at 30 mg/kg.
Animal Model:P-gp-deficient mdr1a (-/-) and wild type mdr1a (+/+) CF-1 mice
Dosage:10 mg/kg
Administration:Oral administration, once
Result:The brain-to-plasma ratio in mdr1a (-/-) mice (b/p = 14) was remarkably higher than that in SD rats (b/p = 1.1) and mdr1a (+/+) mice (b/p = 0.8).
Animal Model:Male Sprague-Dawley rats, male Beagle dogs, and male rhesus monkeys
Dosage:1 or 3 mg/kg
Administration:IV or PO (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of 1 in Rats, Dogs, and Rhesus Monkeysa iv (1 mg/kg)po (3 mg/kg)
CLp (mL/min/kg)Vdss(L/kg)t1/2(h)Cmax(μM)AUC0-∞(μM h)Fb(%)
rat124.45.51.016.3565
dog199.79.91.811.8>100
体外研究：
MK-0249 (Compound 1) shows very good hepatic clearance values (CLh e 11 mL/min/kg), and is a substrate for rat P-gp but not for human P-gp.MK-0249 displays potent binding affinity to human, rat, and rhesus H3 receptors with Ki values of 6.8 ± 1.3 nM, 33 ± 3 nM, and 4.3 ± 1.2 nM, respectively. MK-0249 shows high intrinsic activity.
MK-0249 (Compound 1) is a potent, selective and orally active histamine H3 receptor antagonist, with an IC50 of 1.7 nM for human H3.
体内研究：
MK-0249 (Compound 1) (0-30 mg/kg; p.o.; once) elevates histamine levels in the rat brain in a dose-dependent manner.MK-0249 (10 mg/kg; p.o.; once) shows markedly higher brain penetrability and a lower plasma Occ90 value in mdr1a (-/-) mice than in mdr1a (+/+) mice.MK-0249 shows rodent brain permeability and is significantly limited by P-gp mediated efflux in rodents, whereas the extent of P-gp mediated efflux in humans should be very small or negligible.Animal Model:SD rats
Dosage:3, 10 and 30 mg/kg
Administration:Oral administration, once
Result:Showed a statistically significant increase in tele-methylhistamine levels at 30 mg/kg.
Animal Model:P-gp-deficient mdr1a (-/-) and wild type mdr1a (+/+) CF-1 mice
Dosage:10 mg/kg
Administration:Oral administration, once
Result:The brain-to-plasma ratio in mdr1a (-/-) mice (b/p = 14) was remarkably higher than that in SD rats (b/p = 1.1) and mdr1a (+/+) mice (b/p = 0.8).
Animal Model:Male Sprague-Dawley rats, male Beagle dogs, and male rhesus monkeys
Dosage:1 or 3 mg/kg
Administration:IV or PO (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of 1 in Rats, Dogs, and Rhesus Monkeysa iv (1 mg/kg)po (3 mg/kg)
CLp (mL/min/kg)Vdss(L/kg)t1/2(h)Cmax(μM)AUC0-∞(μM h)Fb(%)
rat124.45.51.016.3565
dog199.79.91.811.8>100
体外研究：
MK-0249 (Compound 1) shows very good hepatic clearance values (CLh e 11 mL/min/kg), and is a substrate for rat P-gp but not for human P-gp.MK-0249 displays potent binding affinity to human, rat, and rhesus H3 receptors with Ki values of 6.8 ± 1.3 nM, 33 ± 3 nM, and 4.3 ± 1.2 nM, respectively. MK-0249 shows high intrinsic activity.
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