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- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
862309-06-6
- 规格：
1 mg/5 mg
| 规格： | 1 mg | 产品价格： | ￥2000.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥5000.0 |
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MK-0249
CAS No. : 862309-06-6
MCE 国际站：MK-0249
产品活性：MK-0249 (Compound 1) 是一种有效的、选择性的、具有口服活性的 histamine H3 受体拮抗剂，对人体H3 受体的IC50 值为 1.7 nM。
研究领域：GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation
作用靶点：Histamine Receptor
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.
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.
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.
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.
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