Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
25 mg | 約10-14 週間 | ¥ 521,000 |
50 mg | 約10-14 週間 | ¥ 684,000 |
100 mg | 約10-14 週間 | ¥ 918,000 |
説明 | MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM). |
ターゲット&IC50 | CYP2C9:50 μM, β-arrestin:3.5 nM, CYP2D6:50 μM, CYP3A4:50 μM, cAMP:8.0 nM, CRTH2/DP2 receptor:5.0 nM (ki) |
In vitro | MK-8318 suppresses β-arrestin, cAMP, CYP3A4, CYP2C9, and CYP2D6 (IC50s: 3.5±2.1 nM, 8.0±6.8 nM, 50 μM, 50 μM and 50 μM). |
In vivo | MK-8318 displays 76% LAR efficacy and 114% AHR efficacy. MK-8318 blocks late airway response (LAR) and airway hyperresponsiveness (AHR) after i.v. infusion at 1 mg/kg, in a sheep model. MK-8318 also shows good efficacy on BAL cells/pulmonary function from ovalbumin sensitized and challenged Brown Norway rats at 3, 10, and 30 mg/kg oral dosing. |
分子量 | 534.5 |
分子式 | C27H26F4N2O5 |
CAS No. | 1416581-40-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
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MK-8318 1416581-40-2 Others MK 8318 MK8318 Inhibitor inhibitor inhibit