ML 145 是选择性，竞争性的人 GPR35/CXCR8 拮抗剂，IC₅₀/EC₅₀ 为 20.1 nM。ML 145 对 GPR35 的选择性比 GPR55 (IC₅₀/EC₅₀=21.7 μM) 高超 1000 倍。 ML 145 对啮齿动物直系同源物的 GPR35 均无明显活性。

ML 145 is a selective and competitive human GPR35/CXCR8 antagonist with an IC 50 /EC 50 of 20.1 nM. ML 145 has over 1000-fold more selective for GPR35 compared to GPR55 (IC 50 /EC 50 =21.7 μM). ML 145 has no significant activity for GPR35 at either rodent ortholog.

Solid

IC50/EC50: 20.1 nM (GPR35), 21.7 μM (GPR55)

ML 145 (10 μM) also fully blocks internalization of human FLAG-GPR35-eYFP in response to varying concentrations of Zaprinast, Cromolyn disodium, and Pamoate.
ML 145 is either without effect (mouse) or displays only a small and apparently noncompetitive inhibitory effect (rat) at the rodent orthologs.
ML 145 acts as a competitive antagonist for a number of agonists at human GPR35 and has an IC50 value against EC80 concentrations of various GPR35 agonists in the region of 20 nM.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Heynen-Genel S, et al. Selective GPR35 Antagonists - Probes 1 & 2. National Center for Biotechnology Information (US); 2010-2010 Feb 28.
[2]. Laura Jenkins, et al. Antagonists of GPR35 display high species ortholog selectivity and varying modes of action. J Pharmacol Exp Ther. 2012 Dec;343(3):683-95.

In Vitro: DMSO : 50 mg/mL (103.61 mM; Need ultrasonic)配制储备液