2. GPCR/G Protein
  3. LPL Receptor
  4. S1PR1/S1PR5 agonist-1

S1PR1/S1PR5 agonist-1 (Compound 19) 是一种口服有效的 S1PR1 和 S1PR5 激动剂，EC50 为 40.0 和 22.9 nM。S1PR1/S1PR5 agonist-1 可结合 S1PR1 的关键残基以介导激动活性。S1PR1/S1PR5 agonist-1 可缓解 DSS 诱导的小鼠模型中的结肠炎病理改变，且对小鼠心率影响极小。S1PR1/S1PR5 agonist-1 可用于炎症性肠病的研究。

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S1PR1/S1PR5 agonist-1

S1PR1/S1PR5 agonist-1 Chemical Structure

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S1PR1/S1PR5 agonist-1 相关抗体

Top Publications Citing Use of Products

查看 LPL Receptor 亚型特异性产品:

查看所有亚型
LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

S1PR1/S1PR5 agonist-1 (Compound 19) is an orally active S1PR1 and S1PR5 agonist with EC50 values of 40.0 and 22.9 nM, respectively. S1PR1/S1PR5 agonist-1 binds to key residues of S1PR1 to mediate agonistic activity. S1PR1/S1PR5 agonist-1 alleviates colitis pathological changes in DSS-induced mouse models and exerts minimal effects on mouse heart rate. S1PR1/S1PR5 agonist-1 can be used for the research of inflammatory bowel disease[1].

IC50 & Target[1]

S1PR1

40.0 nM (EC50)

S1PR5

22.9 nM (EC50)

体外研究
(In Vitro)

S1PR1/S1PR5 agonist-1 可在稳定表达 S1PR1/Gα16 的 CHO-K1 细胞中强效激动 S1PR1，其 EC50 为 40.0 ± 2.5 nM[1]。
S1PR1/S1PR5 agonist-1 可在稳定表达 S1PR5/Gα16/CHO-K1 的细胞中强效激动 S1PR5，其 EC50 为 22.9 ± 0.5 nM[1]。

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

S1PR1/S1PR5 agonist-1 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 AUClast Tmax Cmax Bioavailability
Mice[1] 20 mg/kg p.o. 2.2 ± 0.1 h 79634.0 ± 16163.0 ng·h/mL 1.3 ± 0.6 h 13458.0 ± 4056.0 ng/mL 105.0 %
Mice[1] 2 mg/kg i.v. 1.1 h 7573.0 ± 1385.0 ng·h/mL / / /
体内研究
(In Vivo)

S1PR1/S1PR5 agonist-1 (3 mg/kg；口服) 可在雄性 C57BL/6J 小鼠中维持心脏功能，且无明显负性变时作用[1]。
S1PR1/S1PR5 agonist-1 (3 mg/kg；口服；每日 1 次；连续 10 天) 可显著减轻葡聚糖硫酸钠诱导的雄性 C57BL/6J 小鼠结肠炎，其效果优于 50 mg/kg 5-ASA[1]。

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

Animal Model: C57BL/6J mice (male, 10 weeks old, SPF grade)[1]
Dosage: 3 mg/kg
Administration: p.o.
Result: Preserved cardiac function, maintaining both ejection fraction and fractional shortening throughout the 72-hour evaluation period.
Showed no significant negative chronotropic effects.
Induced a transient increase in basal heart rate by day 3 that partially subsided after the third dose.
Animal Model: C57BL/6J mice (male, DSS-induced colitis model)[1]
Dosage: 3 mg/kg
Administration: p.o.; once daily; 10 days
Result: Significantly ameliorated acute colitis compared to the vehicle group, reducing body weight loss, lowering disease activity index scores, and increasing colon length.
Demonstrated efficacy superior to 50 mg/kg 5-ASA.
Improved epithelial architecture, reduced ulceration, and diminished inflammatory infiltrate via histopathological analysis.
Decreased F4/80-positive macrophage infiltration via immunofluorescence staining.
Reduced Ly-6G-positive neutrophil recruitment via immunohistochemistry.
Reduced peripheral lymphocyte counts via hematological analysis, consistent with on-target S1PR1-mediated lymphocyte sequestration.
分子量

496.56

Formula

C29H28N4O4
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

S1PR1/S1PR5 agonist-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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:

S1PR1/S1PR5 agonist-1LPL ReceptorLysophospholipid ReceptorS1PR3dextran sodium sulfate-induced mouse modelinflammatory bowel diseaseS1PR5CHO-K1 cellsT cell migrationS1PR2S1PR1S1PR4colitisInhibitorinhibitorinhibit

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