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首页-小分子抑制剂&激动剂-GPCR-Proton-sensing GPCRs-BRD5075
BRD5075

Chemical Structure : BRD5075

CAS No.:

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BRD5075 (BRD 5075)

货号: PC-22775Not For Human Use, Lab Use Only.

BRD5075 is a potent, specific activator / positive allosteric modulator (PAM) of GPR65, induces GPR65-dependent cAMP production with EC50 of 3.8 and 6.9 uM for WT GPR65 and GPR65 I231L respectively, regulates GPR65-dependent inflammatory cytokine and chemokine expression.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BRD5075 is a potent, specific activator / positive allosteric modulator (PAM) of GPR65, induces GPR65-dependent cAMP production with EC50 of 3.8 and 6.9 uM for WT GPR65 and GPR65 I231L respectively, regulates GPR65-dependent inflammatory cytokine and chemokine expression.
BRD5075 demonstrates the highest activity for hGPR65 and mGPR65 at 1.56 μM.
BRD5075 exhibits robust induction of cAMP activity and recruited G protein for the WT and variant hGPR65 as well as for the mouse ortholog.
BRD5075 is able to recruit G protein in cells expressing the variant hGPR65 I231L.
BRD5075 (5 uM, 20 uM) shows strong inhibitory effect of low pH on TNF secretion and further TNF suppression in MDDCs stimulated with lipopolysaccharide (LPS).
BRD5075 can potentiate GPR65 and the risk variant I231L to rebalance inflammatory responses.
GPR65 is a proton-activated heterotrimeric GTP-binding protein (G protein)–coupled receptor (GPCR) expressed primarily on myeloid and lymphoid immune cells that has been implicated through genetics in multiple autoimmune and inflammatory diseases.

物理化学性质&存储条件

分子量 417.47
分子式 C23H23N5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

5-(4-(isopropoxymethyl)phenyl)-N-(5-methylpyridin-2-yl)-7-oxo-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carboxamide

参考文献

1. Neale I, et al. Sci Adv. 2024 Jul 19;10(29):eadn2339.

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