2. GPCR/G Protein
  3. LPL Receptor
  4. S1P1 agonist 7

S1P1 agonist 7 是一种强效、具备口服活性的 β-抑制蛋白偏向型 S1P1 激动剂 (EC50(G‑protein) = 12.7 nM，EC50(β‑arrestin) = 3.23 nM)，具有强效的免疫调节活性和良好的安全性。S1P1 agonist 7 具备优异的代谢稳定性、微弱至中度的 CYP 抑制能力，以及不作用于 S1P3 受体的高选择性。S1P1 agonist 7 在实验性自身免疫性脑脊髓炎小鼠模型中展现出良好的药代动力学特性，能够有效降低循环淋巴细胞数量，并显著减轻疾病的严重程度。S1P1 agonist 7 可用于多发性硬化症研究。

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S1P1 agonist 7

S1P1 agonist 7 Chemical Structure

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S1P1 agonist 7 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

S1P1 agonist 7 is a potent, orally active, and β-arrestin-biased S1P1 agonist (EC50(G‑protein) = 12.7 nM and EC50(β‑arrestin) = 3.23 nM). S1P1 agonist 7 demonstrates potent immunomodulatory activity and a favorable safety profile. S1P1 agonist 7 exhibits excellent metabolic stability, minimal to moderate CYP inhibition, and S1P3-sparing selectivity. S1P1 agonist 7 shows pharmacokinetics, effectively reduces circulating lymphocytes, and significantly alleviates disease severity in experimental autoimmune encephalomyelitis (EAE) mouse models under both prophylactic and therapeutic regimens. S1P1 agonist 7 can be used for multiple sclerosis (MS) research[1].

体外研究
(In Vitro)

S1P1 agonist 7 (compound 28) 的分子对接研究表明，其相对于芬戈莫德 (HY-11063) 表现出 4.51 倍的 β-抑制蛋白偏向性，其 G 蛋白信号通路 EC50 为 12.7 nM，β-抑制蛋白招募 EC50 为 3.23 nM[1]。
S1P1 agonist 7 (1-10 µM，15-60分钟) 在所有的人、大鼠和小鼠的肝微粒体中均表现出高度稳定性，且在 10 µM 浓度下对大多数 CYP 同工酶无显著抑制作用[1]。
S1P1 agonist 7 (从100 μM起始浓度进行梯度稀释，90 分钟) 在 Chem-4/G15 和 CHO-K1 EDG1 细胞模型中显示出对 S1P1 受体的高选择性，其 G 蛋白信号通路的 EC50 值为0.014 μM，β-抑制蛋白招募的 EC50 值为0.0023 μM，且仅对 S1P5 受体表现出微弱活性[1]。
S1P1 agonist 7 (0.041-10 μM，2 分钟) 即使在最高测试浓度下，也未在人类 iPSC 来源的心肌细胞中引起任何可观察到的峰值频率或搏动速率的变化[1]。

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

S1P1 agonist 7 相关抗体:
体内研究
(In Vivo)

S1P1 agonist 7 (1、3 和 10 mg/kg，灌胃，单次给药) 可降低 C57BL/6N 小鼠的外周血淋巴细胞计数[1]。
S1P1 agonist 7 (10 mg/kg，灌胃，每日一次，连续 23 天) 在 MOG35-55 (HY-P1240) 诱导的 EAE 小鼠模型中表现出强大的保护作用，能够减缓其疾病发作、抑制病情进展并减轻相关的病理损伤[1]。

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

Animal Model: Female C57BL/6N mice (8 weeks old) immunized with MOG/CFA emulsion and received PTX on two consecutive days to induce EAE[1]
Dosage: 10 mg/kg
Administration: i.g., daily for 23 days
Result: Delayed disease onset and reduced symptom severity, as indicated by lower cumulative and mean maximum clinical scores.
Maintained its prophylactic effect until the peak of disease severity, which occurred around 17 dpi.
Prevented body weight loss and lowered disease incidence in EAE mice, indicating a protective effect.
Moderated disease progression, and led to a steady reduction in symptom severity until 34 dpi, demonstrating a moderate therapeutic effect comparable to that of Siponimod (HY-12355).
Significantly reduced the cumulative clinical score from 19 dpi (the peak of EAE) to 34 dpi.
Prevented body weight loss compared to the vehicle-treated group.
Markedly reduced demyelination in the spinal cord's dorsal column and ventral white matter.
Reduce immune cell infiltration and partially preserved myelin integrity.
Animal Model: Female C57BL/6N mice (8 weeks old)[1]
Dosage: 1, 3, and 10 mg/kg
Administration: i.g., once
Result: Reduced PLC to 24.4% of baseline at 4 h post administration, outperforming Fingolimod (36.3%).
Promoted a rapid recovery of PLCs to 70.8% of baseline within 28 hours, in contrast to Fingolimod (HY-11063), which causes prolonged lymphopenia.
Produced a rapid reduction in lymphocyte counts to approximately 40% of baseline at 3 h post administration and achieved maximal suppression at the 3 and 10 mg/kg doses by 6 h post administration, while triggering an early rebound in the 1 mg/kg group by the same time, suggesting the onset of recovery.
Elicited a stronger pharmacodynamic response at 3 and 10 mg/kg, and permitted full lymphocyte recovery in all groups within 24 hours.
分子量

406.43

Formula

C23H22N2O5
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

S1P1 agonist 7 相关分类

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  • 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:

S1P1 agonist 7LPL ReceptorLysophospholipid Receptorβ-arrestin-biasedS1P1immunomodulatory activitymetabolic stabilityCYP inhibitionEAE mouse modelMSiPSC-derived cardiomyocytesmicrosomalPLCInhibitorinhibitorinhibit

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