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[CAS NO. 862309-06-6] MK-0249
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-U00076 |
| Brand: | MCE |
| CAS: | 862309-06-6 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 431.45 |
| Molecular Formula | C23H24F3N3O2 |
| SMILES | - |
Summary
MK-0249 (Compound 1) is a potent, selective and orally active histamine H 3 receptor antagonist, with an IC 50 of 1.7 nM for human H3 [1] .
IC50 & Target
|
human H 3 receptor 1.7 nM (IC 50 ) |
rhesus H 3 receptor 4.3 nM (Ki) |
human H 3 receptor 6.8 nM (Ki) |
rat H 3 receptor 33 nM (Ki) |
In Vitro
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 H
3
receptors with K
i
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | SD rats [1] |
| 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 [1] |
| 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 [1] | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Dosage: | 1 or 3 mg/kg | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Administration: | IV or PO (Pharmacokinetic Analysis) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Result: |
Pharmacokinetic Parameters of 1 in Rats, Dogs, and Rhesus Monkeys
a
[1]
The molarity calculator equationMass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) The dilution calculator equationConcentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C 1 V 1 = C 2 V 2 Keywords:MK-0249 862309-06-6 MK0249 MK 0249 Histamine Receptor CNS dysfunction Inhibitor inhibitor inhibit Your Recently Viewed Products:Inquiry Online Your information is safe with us. * Required Fields. Bulk Inquiry
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