Name: MK-8318
Brand: TargetMol
SKU: T16097
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

25 mg

¥ 15,000

10-14周

50 mg

¥ 19,800

10-14周

100 mg

¥ 25,500

10-14周

生物活性

产品描述	MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).
靶点活性	CYP2C9:50 μM, CYP2D6:50 μM, β-arrestin:3.5 nM, CRTH2/DP2 receptor:5.0 nM (ki), CYP3A4:50 μM, cAMP:8.0 nM
体外活性	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).
体内活性	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.

化学信息

分子量	534.5
分子式	C₂₇H₂₆F₄N₂O₅
CAS No.	1416581-40-2
Smiles	N(C(CCC(O)=O)=O)([C@H]1C=2C(N(C(=O)C3=CC=C(OC(F)(F)F)C=C3)[C@@]4([C@]1(CCC4)[H])[H])=CC=C(F)C2)C5CC5
密度	no data available

储存&溶解度

存储	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准

MK-8318