CID 16020046

A selective GPR55 inverse agonist

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库存: 现货

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10mg

￥1612.00

1290.00

- +
50mg

￥6712.00

5370.00

- +
100mg

￥0.00

0.00

- +
200mg

￥0.00

0.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajce55630
CAS: 834903-43-4
别名: 4-[4,6-二氢-4-(3-羟基苯基)-3-(4-甲基苯基)-6-氧代吡咯并[3,4-C]吡唑-5(1H)-基]苯甲酸
分子式: C25H19N3O4
分子量: 425.44
纯度: >98%
溶解度: DMSO: 100 mg/mL (235.05 mM)
储存: Store at -20°C
库存: 现货

Background

CID16020046 is a GPR55 inverse agonist that antagonizes GPR55 constitutive activity with an IC₅₀ value of 15 μM.¹ It inhibits GPR55-mediated ERK1/2 phosphorylation, LPI-induced Ca²⁺ signaling (IC₅₀ = 0.21 μM in HEK-GPR55 cells), and GPR55-mediated transcription factor activation.¹ It does not affect ERK1/2 phosphorylation or transcription factor activation in CB receptor expressing cells and demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptors.¹ This compound has been shown to block GPR55-mediated endothelial wound healing and reverse LPI-inhibited platelet aggregation.¹

1.Kargl, J., Brown, A.J., Andersen, L., et al.A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell functionJ. Pharmacol. Exp. Ther.346(1)54-66(2013)