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

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.

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TYY-31

TYY-31 Chemical Structure

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TYY-31 Related Antibodies

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Description

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)

In Vitro

TYY-31 is a highly selective S1PR1 agonist in Tango CHO cells, with single-digit picomolar potency against S1PR1, exhibiting over 106-fold selectivity over S1PR2, S1PR3 and S1PR5, and over 30000-fold selectivity over S1PR4[1].
TYY-31 (treated at 10 μM for 1.5 h followed by a 20 h recovery) potently induces S1PR1 internalization in HEK293T cells stably expressing S1PR1, with an EC50 of 0.73 nM[1].
TYY-31 (1-1000 nM) activates ERK1/2 phosphorylation in a concentration-dependent manner in S1PR1-expressing cells, indicating that it activates the downstream signaling pathway of S1PR1[1].

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

TYY-31 Related Antibodies
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 %
In Vivo

TYY-31 (0.1-1 mg/kg; p.o.; single administration) induces a dose-dependent and reversible decrease in peripheral blood lymphocyte counts in healthy male ICR mice. A significant reduction is observed in both the 0.3 mg/kg and 1 mg/kg dose groups at 3 h post-administration[1].
TYY-31 (0.1-1 mg/kg; p.o.; once daily; for 7 consecutive days) effectively ameliorates DSS-induced colitis in mice even at doses as low as 0.1 mg/kg, with the ameliorative effect at the 0.3 mg/kg dose being comparable to that of Ozanimod (HY-12288)[1].
TYY-31 (5 μM; environmental exposure; medium replaced daily) potently inhibits the expression of key pro-inflammatory mediators in dextran sulfate sodium (DSS)-induced intestinal inflammation of zebrafish (Danio rerio), and exhibits better efficacy than Ozanimod at the same concentration[1].

MedChemExpress (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.
Molecular Weight

487.53

Formula

C27H26FN5O3
SMILES

CC1=C(C2=NC=C(N=C2)F)C=CC(C3=NC(C4=CC=C(C(CC)=C4)CN[C@@H]5C[C@@H](C5)C(O)=O)=NO3)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TYY-31 Related Classifications

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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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