A potent S1P1 receptor agonist
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RP 001 (hydrochloride)

Item No. 16636

Technical Information
Formal Name
N-[4-[5-[3-cyano-4-(1-methylethoxy)phenyl]-1,2,4-oxadiazol-3-yl]-2,3-dihydro-1H-inden-1-yl]-β-alanine, monohydrochloride
CAS Number
1781880-34-9
Molecular Formula
C24H24N4O4 • HCl
Formula Weight
Purity
≥98%
Formulation
A solid
SMILES
OC(CCNC1CCC2=C(C3=NOC(C4=CC(C#N)=C(OC(C)C)C=C4)=N3)C=CC=C21)=O.Cl
InChi Code
InChI=1S/C24H24N4O4.ClH/c1-14(2)31-21-9-6-15(12-16(21)13-25)24-27-23(28-32-24)19-5-3-4-18-17(19)7-8-20(18)26-11-10-22(29)30;/h3-6,9,12,14,20,26H,7-8,10-11H2,1-2H3,(H,29,30);1H
InChi Key
ZHPGSGYEFGEZAL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    RP 001 is a potent sphingosine-1-phosphate receptor 1 (S1P1) agonist (EC50 = 9 pM).1 It is competitive with W146 (Item No. 10009109), a selective S1P1 antagonist, and induces internalization and polyubiquitination of S1P1 in a dose-dependent manner. RP 001 induces dose-dependent lymphopenia in mice (EC50 = 0.03 mg/kg). It reduces S1P1-EGFP expression ex vivo on lymphocytes in the isolated lymph node of Edg1eGFP/eGFP mice but has no effect in vivo. RP 001 also completely inhibits M. stadtmanae (MSS) rechallenge-induced enlargement of B cell-rich tertiary lymphoid tissues (TLTs) and reduces neutrophil accumulation in the airways of a mouse model of experimental hypersensitivity pneumonitis.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cahalan, S.M., Gonzalez-Cabrera, P.J., Sarkisyan, G., et alActions of a picomolar short-acting S1P1 agonist in S1P1-eGFP knock-in mice. Nat. Chem. Biol. 7(5), 254-256 (2011).

    2. Huppé, C.A., Lecours, P.B., Lechasseur, A., et alA sphingosine-1-phosphate receptor 1 agonist inhibits tertiary lymphoid tissue reactivation and hypersensitivity in the lung. Mucosal. Immunol. 11(1), 112-119 (2018).