Vidupiprant 是一种有效的 CRTH2 和前列腺素 D 受体双重拮抗剂,在人源血浆中的 IC50 分别为 8 nM 和 35 nM。 Vidupiprant 可用于治疗哮喘的研究。
产品描述
Vidupiprant is an effective dual antagonist of CRTH2 and prostanoid D receptor with IC50s of 8 nM and 35 nM in human plasma. Vidupiprant can be used in studies about the treatment of asthma.
体外活性
Vidupiprant inhibits prostaglandin D2-induced cAMP response in platelets in 80% human whole blood with a Kb of 4.7 nM. Vidupiprant inhibits the prostaglandin D2 -induced down-modulation of CRTH2 on CD16 negative granulocytes in human whole blood with a Kb of 0.2 nM. Vidupiprant demonstrates antagonist activity in an aequorin assay using CRTH2-transfected HEK 293 cells and an eosinophil shape change assay[1].
体内活性
In a guinea pig model of PGD2-induced airway constriction, airway resistance is measured in response to PGD2 challenge. Vidupiprant has a Kb of 5 nM[1].
Cas No.
1169483-24-2
分子式
C28H27Cl2FN2O6S
分子量
609.49
别名
AMG 853
储存和溶解度
DMSO:95 mg/mL (155.87 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years