2. GPCR/G Protein
  3. LPL Receptor
  4. TYY-31

TYY-31 是一种具有口服活性的、选择性的 S1PR1 激动剂，EC50 为 1.13 pM。TYY-31 可促进 ERK1/2 磷酸化。TYY-31 具有抗炎和免疫抑制作用，可改善 DSS 诱导的小鼠结肠炎，并呈剂量依赖性降低小鼠外周血淋巴细胞计数。TYY-31 可用于溃疡性结肠炎的研究。

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TYY-31

TYY-31 Chemical Structure

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TYY-31 相关抗体

Top Publications Citing Use of Products

查看 LPL Receptor 亚型特异性产品:

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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

TYY-31 is an orally active, selective S1PR1 agonist with an EC50 of 1.13 pM. TYY-31 promotes the phosphorylation of ERK1/2. TYY-31 exerts anti-inflammatory and immunosuppressive effects, ameliorates DSS-induced colitis in mice, and reduces peripheral blood lymphocyte counts in mice in a dose-dependent manner. TYY-31 can be used for the research of ulcerative colitis[1].

IC50 & Target[1]

S1PR1

1.13 pM (EC50)

体外研究
(In Vitro)

TYY-31 是 Tango CHO 细胞中高选择性的 S1PR1 激动剂，对 S1PR1 具有个位数皮摩尔级的效力，对 S1PR2、S1PR3 和 S1PR5 的选择性超过 106 倍，对 S1PR4 的选择性超过 30000 倍[1]。
TYY-31 (以 10 μM 处理 1.5 h 后恢复 20 h) 可在稳定表达 S1PR1 的 HEK293T 细胞中强效诱导 S1PR1 内化，其 EC50 为 0.73 nM[1]。
TYY-31 (1-1000 nM) 可在表达 S1PR1 的细胞中以浓度依赖的方式激活 ERK1/2 磷酸化，表明其激活了 S1PR1 下游信号通路[1]。

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

TYY-31 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax AUC0-t T1/2 CL Vss F
Rat[1] 1 mg/kg i.v. 198.6 ng/mL 0.08 h 181.1 ng·h/mL 1.54 h 99.77 mL/min/kg 8.84 L/kg /
Rat[1] 10 mg/kg p.o. 374.9 ng/mL 2.67 h 2221 ng·h/mL 3.61 h 59.35 mL/min/kg / 122.6 %
Mice[1] 1 mg/kg i.v. 390.0 ng/mL 0.08 h 364.8 ng·h/mL 1.30 h 45.84 mL/min/kg 4.07 L/kg /
Mice[1] 1 mg/kg p.o. 130.8 ng/mL 0.50 h 235.0 ng·h/mL 2.86 h 59.17 mL/min/kg / 76.40 %
体内研究
(In Vivo)

TYY-31 (0.1-1 mg/kg；口服；单次) 可使健康雄性 ICR 小鼠的外周血淋巴细胞计数呈剂量依赖性可逆降低，给药后 3 小时，0.3 mg/kg 和 1 mg/kg 剂量组均观察到显著降低[1]。
TYY-31 (0.1-1 mg/kg；口服；每日一次；连续 7 天) 在低至 0.1 mg/kg 的剂量下即可有效改善小鼠 DSS 诱导的结肠炎，其中 0.3 mg/kg 剂量的改善效果与 Ozanimod (HY-12288) 相当[1]。
TYY-31 (5 μM；环境暴露；每日更换培养基) 可强效抑制 DSS 诱导的斑马鱼 (Danio rerio) 肠道炎症中关键促炎介质的表达，且相同浓度下的效果优于 Ozanimod[1]。

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

Animal Model: ICR (male, 18−20 g)[1]
Dosage: 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg
Administration: p.o.; single dose
Result: Induced a dose-dependent reduction in peripheral blood lymphocyte counts.
Significantly reduced lymphocyte counts at 3 hours postadministration in mice treated with 0.3 mg/kg and 1 mg/kg.
Substantially recovered lymphocyte counts to near baseline levels by 24 hours postadministration across all doses.
Animal Model: unspecified (6 per group, DSS-induced colitis model)[1]
Dosage: 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg
Administration: p.o.; daily; 7 days
Result: Dose-dependently mitigated DSS-induced weight loss, with 0.3 mg/kg and 1 mg/kg doses showing body weight recovery comparable to Ozanimod (1 mg/kg).
Significantly reduced DAI scores from day 9 onward across all doses, with 0.1 mg/kg and 0.3 mg/kg demonstrating efficacy comparable to Ozanimod (1 mg/kg).
Promoted significant recovery of colon length across all doses, including the low 0.1 mg/kg dose.
Maintained near-intact mucosal architecture with only focal ulcerations in treated mice, in contrast to the model group's severe inflammation, crypt loss, and epithelial damage.
Animal Model: larvae (4 days postfertilization)[1]
Dosage: 5 μM
Administration: environmental exposure; daily medium renewal
Result: Significantly suppressed DSS-induced upregulation of IL-1β, IL-8, MMP9, and TNF-α mRNA expression.
Exhibited more pronounced inhibitory effect on pro-inflammatory biomarkers than Ozanimod at the same 5 μM concentration.
分子量

487.53

Formula

C27H26FN5O3
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

TYY-31 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

TYY-31TYY31TYY 31LPL ReceptorLysophospholipid ReceptorERK1/2S1PR2β-arrestin pathwayS1PR4HEK293T cellsS1PR5S1PR1S1PR3dextran sulfate sodium-induced colitisTango CHO cellsInhibitorinhibitorinhibit

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目录号：
HY-183578
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