CID 2745687

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

CID 2745687 是一种 GPR35 拮抗剂，可抑制色甘酸二钠和扎普司特（两种共享重叠结合位点的激动剂）对 GPR35 的作用。

CID 2745687 is a GPR35 antagonist that inhibited the effects at human GPR35 of cromolyn disodium and zaprinast, two agonists that share an overlapping binding site.

For ERK1/2 phosphorylation with 1 μM Pamoic acid as the agonist, the CID 2745687 (CID2745687) Ki is 18 nM. CID 2745687 (CID-2745687) is a potent antagonist in β-arrestin-2 interaction assays only at human GPR35.Using the BRET-based GPR35-β-arrestin-2 interaction assay and an EC80 concentration of Zaprinast (20 μM) as agonist, CID 2745687 behaved as a moderately potent, concentration-dependent antagonist at human GPR35 with pIC50=6.70±0.09.CID 2745687 (pIC50=6.27±0.08) fully reverses the agonist action of Cromolyn disodium .

CID 2745687 (CID2745687; 1 mg/kg; administrated orally every day for the last 4 weeks), a specific GPR35 antagonist, reverses Lodoxamide-mediated anti-fibrotic effects. Animal Model:Six-week-old male C57BL/6 miceDosage:1 mg/kgAdministration:Oral administration, every day for 4 weeks Result:Inhibited Lodoxamide-mediated protective effects.

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Cell Cycle/DNA Damage

GPR

GRP35

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264233-05-8

395.43

C17H19F2N5O2S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (316.11 mM)

O=C(C1=C(C=NNC(NC(C)(C)C)=S)N(C2=CC=C(F)C=C2F)N=C1)OC

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(-20℃)

With Ice Pack

≥ 2 years