| Bioactivity | 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[1]. | ||||||||||||
| Invitro | 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[1].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[1]. MK-0249 shows high intrinsic activity[1]. | ||||||||||||
| In Vivo | MK-0249 (Compound 1) (0-30 mg/kg; p.o.; once) elevates histamine levels in the rat brain in a dose-dependent manner[1].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[1].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[1]. Animal Model: | ||||||||||||
| Name | MK-0249 | ||||||||||||
| CAS | 862309-06-6 | ||||||||||||
| Formula | C23H24F3N3O2 | ||||||||||||
| Molar Mass | 431.45 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Nagase T, et al. Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists. J Med Chem. 2008 Aug 14;51(15):4780-9. |
MK-0249
CAS: 862309-06-6 F: C23H24F3N3O2 W: 431.45
MK-0249 (Compound 1) is a potent, selective and orally active histamine H3 receptor antagonist, with anIC50 of 1.7 nM fo
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.