Vidupiprant

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Vidupiprant 是一种有效的 CRTH2 和前列腺素 D 受体双重拮抗剂，在人血浆中的 IC50 分别为 8 nM 和 35 nM。

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.(In Vitro):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.(In Vivo):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.

Vidupiprant (AMG 853, Compound 2) inhibits the prostaglandin D2 (PGD2)-induced down-modulation of CRTH2 on CD16 negative granulocytes (eosinophils) in human whole blood with a Kb of 0.2 nM. Vidupiprant also inhibits PGD2-induced cAMP response in platelets in 80% human whole blood with a Kb of 4.7 nM, which is significantly improved, as compared to the Kb of 148 nM of AMG 009. In addition, Vidupiprant demonstrates similar antagonist activity in an aequorin assay using CRTH2-transfected HEK 293 cells and an eosinophil shape change assay, as compared to the CRTH2 receptor down-modulation human whole blood assay.

The significant improvement of DP potency of Vidupiprant (AMG 853, Compound 2) over AMG 009 is also demonstrated in vivo in a guinea pig model of PGD2-induced airway constriction. In this model, airway resistance is measured in response to PGD2 challenge. The in vitro guinea pig DP potency is evaluated in guinea pig whole blood cAMP assay.Vidupiprant has a Kb of 5 nM, while the Kb of AMG 009 is 82 nM.

AMG 853

GPCR/G Protein

Prostaglandin Receptor

Androgen Receptor

——

——

1169483-24-2

609.49

C28H27Cl2FN2O6S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (164.07 mM)

CC(C)(C)NC(=O)c1ccc(Oc2cc(F)c(CC(O)=O)cc2Cl)c(NS(=O)(=O)c2ccc(cc2Cl)C2CC2)c1

——

(-20℃)

With Ice Pack

≥ 2 years