S1PR1/S1PR5 agonist-1

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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.

S1PR1/S1PR5 agonist-1 Chemical Structure

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

S1PR1

40.0 nM (EC₅₀)

S1PR5

22.9 nM (EC₅₀)

In Vitro

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.

Parmacokinetics

Species	Dose	Route	T_1/2	AUC_last	T_max	C_max	Bioavailability
Mice^[1]	20 mg/kg	p.o.	2.2 ± 0.1 h	79634.0 ± 16163.0 ng·h/mL	1.3 ± 0.6 h	13458.0 ± 4056.0 ng/mL	105.0 %
Mice^[1]	2 mg/kg	i.v.	1.1 h	7573.0 ± 1385.0 ng·h/mL	/	/	/

In Vivo

S1PR1/S1PR5 agonist-1 (3 mg/kg; p.o.) preserves cardiac function and shows no significant negative chronotropic effects in male C57BL/6J mice^[1].
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.

Animal Model:	C57BL/6J mice (male, 10 weeks old, SPF grade)^[1]
Dosage:	3 mg/kg
Administration:	p.o.
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.

Animal Model:	C57BL/6J mice (male, DSS-induced colitis model)^[1]
Dosage:	3 mg/kg
Administration:	p.o.; once daily; 10 days
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.

Molecular Weight

496.56

Formula

C₂₉H₂₈N₄O₄

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

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

Handling Instructions (2659 KB)

References

[1]. Wei X, et al. Discovery of Novel Selective Dual Agonists Targeting S1PR1 and S1PR5 for the Treatment of Inflammatory Bowel Disease. J Med Chem. 2026;69(5):5575-5593. [Content Brief]