2. GPCR/G Protein Apoptosis Immunology/Inflammation
  3. GPR68 TNF Receptor Interleukin Related
  4. GPR68 antagonist 1

GPR68 antagonist 1 是一种 GPR68 拮抗剂，其 IC50 为 81 nM。GPR68 antagonist 1 抑制小鼠 GPR68 介导的 cAMP 信号通路，其 IC50 为 179 nM。GPR68 antagonist 1 可缓解葡聚糖硫酸钠 (DSS) (HY-116282C) 诱导的小鼠炎症性肠病模型的疾病症状。GPR68 antagonist 1 可用于炎症性肠病的相关研究。

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GPR68 antagonist 1

GPR68 antagonist 1 Chemical Structure

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GPR68 antagonist 1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GPR68 antagonist 1 is a GPR68 antagonist with an IC50 of 81 nM. GPR68 antagonist 1 inhibits the mouse GPR68-mediated cAMP signaling pathway with an IC50 of 179 nM. GPR68 antagonist 1 alleviates disease symptoms in a dextran sulfate sodium (DSS) (HY-116282C)-induced mouse model of inflammatory bowel disease. GPR68 antagonist 1 is applicable to research related to inflammatory bowel disease[1].

IC50 & Target[1]

IL-6

 

IL-1β

 

药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax T1/2 CLz/F Vz/F AUC0-t Bioavailability
Mice[1] 30 mg/kg i.p. 1889.06 ng/mL 2.00 h 3.21 h 2.45 mL/min/kg 11.40 L/kg 12243.55 ng·h/mL /
Mice[1] 30 mg/kg p.o. 182.91 ng/mL 0.50 h 2.73 h 51.20 mL/min/kg 203.18 L/kg 552.49 ng·h/mL 2.36 %
Mice[1] 10 mg/kg i.v. 1774.50 ng/mL 0.08 h 2.51 h 1.28 mL/min/kg 4.63 L/kg 7808.94 ng·h/mL /
体内研究
(In Vivo)

GPR68 antagonist 1 (Compound 18l) (10-30 mg/kg; i.p.; daily; 10 days) 可显著缓解 C57BL/6 小鼠中 DSS 诱导的 IBD 症状，包括减轻体重下降、结肠缩短和促炎细胞因子产生，同时改善小鼠的存活率和结肠组织组织学特征[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (6-8 weeks old; DSS-induced IBD model)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: i.p.; daily; 10 days (day 0 to day 9)
Result: Delayed weight loss in DSS-exposed mice, with weight recovery observed after switching to normal water.
Reduced colonic shortening.
Prolonged mouse survival.
Mitigated colon tissue damage as shown by H&E staining.
Reduced infiltration of S100A9-positive inflammatory cells in colon tissues.
Significantly decreased serum levels of pro-inflammatory cytokines IL-6, IL-1β, and TNF-α.
Significantly reduced mRNA expression of Il-6, Il-1β, and Tnf-α in colon tissues.
分子量

430.49

Formula

C28H24F2O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GPR68 antagonist 1 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GPR68 antagonist 1GPR68TNF ReceptorInterleukin RelatedG Protein-Coupled Receptor 68Tumor Necrosis Factor ReceptorTNFRILBEAS-2B cellsinflammatory bowel diseasecAMP signalingHEK293T cellsAC16 cellsHK-2 cellsdextran sulfate sodiumC57BL/6 micepro-inflammatory cytokinesInhibitorinhibitorinhibit

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GPR68 antagonist 1
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HY-181485
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