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Cat. No.: HY-164584

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S1P5 receptor antagonist 1

S1P5 receptor antagonist 1 is a selective, blood-brain barrier-permeable S1P5 receptor antagonist with an EC₅₀ of 0.1 nM and a K_i of 4.4 nM. S1P5 receptor antagonist 1 inhibits the migration of natural killer cells towards sphingosine 1-phosphate in vitro, with no effect on T cell migration. S1P5 receptor antagonist 1 can be used in the research of central nervous system diseases.

For research use only. We do not sell to patients.

CAS No.: 1621065-22-2
Formula: C₂₈H₃₉NO₃
Molecular Weight:437.62

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Please store the product under the recommended conditions in the Certificate of Analysis.

S1P5 receptor antagonist 1 Chemical Structure

CAS No.: 1621065-22-2

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

All LPL Receptor Isoforms :

In Vitro

The S1P5 receptor antagonist 1 (Compound 15) (1-25000 nM; 1 h pretreatment) inhibits mouse spleen NK cell migration toward S1P with an IC₅₀ of 553 nM, has no effect on mouse spleen naive T cell migration, and shows a biphasic response with increased migration at 100 nM and inhibition at higher doses^[1].
The S1P5 receptor antagonist 1 has favorable in vitro hepatocyte stability, with a Qh% of 30% in rat hepatocytes and 49% in human hepatocytes^[1].

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

Parmacokinetics

Species	Dose	Route	CL	V_ss	T_1/2	AUC_0-24	C_max	T_max	Bioavailability
Rat^[1]	1 mg/kg	i.v.	12.2 mL/min/kg	4.2 L/kg	4.6 h	1416 mg/h/L	/	/	/
Rat^[1]	5 mg/kg	p.o.	/	/	4.5 h	6515 mg·h/L	947 ng/mL	0.75 h	92 %

In Vivo

S1P5 receptor antagonist 1 (Compound 15) (1-5 mg/kg; p.o., i.v.; single dose) administered to rats results in favorable systemic exposure, 92% oral bioavailability, and consistent brain penetration^[1].

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

Chemical Information

CAS No. 1621065-22-2
Molecular Weight 437.62
Formula C₂₈H₃₉NO₃
SMILES

C(C=1C2=C(C(C)=CC1O[C@@H]3CC[C@@H](C(C)(C)C)CC3)C=CC=C2)N4CCC(C(O)=O)CC4
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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]. Ma B, et al. Novel Potent Selective Orally Active S1P5 Receptor Antagonists. ACS Med Chem Lett. 2021;12(3):351-355. Published 2021 Jan 15. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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S1P5 receptor antagonist 1

All LPL Receptor Isoforms