S1PR1/S1PR5 agonist-1
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.
For research use only. We do not sell to patients.
- Formula: C29H28N4O4
- Molecular Weight:496.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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S1PR1 40.0 nM (EC50) |
S1PR5 22.9 nM (EC50) |
S1PR1/S1PR5 agonist-1 potently activates S1PR1 in CHO-K1 cells stably expressing S1PR1/Gα16, with an EC50 of 40.0 ± 2.5 nM[1].
S1PR1/S1PR5 agonist-1 potently activates S1PR5 in cells stably expressing S1PR5/Gα16/CHO-K1, with an EC50 of 22.9 ± 0.5 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
S1PR1/S1PR5 agonist-1 (3 mg/kg; p.o.; once daily; 10 days) significantly attenuates dextran sodium sulfate-induced colitis in male C57BL/6J mice, with efficacy superior to 50 mg/kg 5-ASA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (male, 10 weeks old, SPF grade)[1]
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Dosage:3 mg/kg
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Administration:p.o.
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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.
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Animal Model:C57BL/6J mice (male, DSS-induced colitis model)[1]
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Dosage:3 mg/kg
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Administration:p.o.; once daily; 10 days
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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.
Chemical Information
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Molecular Weight 496.56
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Formula C29H28N4O4
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SMILES
CC(OC(C=CC(C1=NC(C2=CC=C(C3=C2C=CC=C3)CN4C[C@@H]([C@H](C4)C)C(O)=O)=NO1)=C5)=C5C#N)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
S1PR1/S1PR5 agonist-1 Related Classifications
HY-181875 Related Classifications
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