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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- Formel: C27H26FN5O3
- Molecular Weight:487.53
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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S1PR1 1.13 pM (EC50) |
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.
| 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 % |
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.
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Animal Model:ICR (male, 18−20 g)[1]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg
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Administration:p.o.; single dose
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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.
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Animal Model:unspecified (6 per group, DSS-induced colitis model)[1]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg
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Administration:p.o.; daily; 7 days
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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.
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Animal Model:larvae (4 days postfertilization)[1]
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Dosage:5 μM
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Administration:environmental exposure; daily medium renewal
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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.
Chemical Information
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Molecular Weight 487.53
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Formel C27H26FN5O3
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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