S1P1 agonist 5
S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS).
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- CAS No.: 2760666-20-2
- Formule: C23H24ClN2NaO4
- Masse moléculaire:450.89
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
S1P1 agonist 5 (compound 21l) shows excellent in vitro efficacies with EC50s of 7.03 nM and 11.8 nM for β-arrestin recruitment and internalization, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
S1P1 agonist 5 (10 mg/kg; p.o.) inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood and that lymphopenia can be recovered within 24 hours[1].
S1P1 agonist 5 (3, 10 mg/kg, p.o., once daily for 20 days) ameliorates the disease progression and overall severity in EAE mice, showing favorable drug-like properties[1].
Pharmacokinetic Parameters of S1P1 in rats, male beagle dogs[1].
| administration | parameters | rat | dog |
| i.v. | T1/2 (h) | 1.4±0.3 | 5.70±1.2 |
| AUC0-∞ (ng*h/mL) | 931.3±95.7 | 14,830.8±5475.4 | |
| CL (mL/min/kg) | 17.6±2.0 | 149.9±62.5 | |
| Vss (L/kg) | 1.7±0.2 | 828.7±134.2 | |
| p.o. | Cmax (ng/mL) | 1661.1±916.6 | 3979.4±483.5 |
| Tmax(h) | 0.9±0.8 | 1.3±0.5 | |
| T1/2 (h) | 1.4±0.2 | 4.9±0.6 | |
| AUC0-∞ (ng*h/mL) | 5044.9±1061 | 23,109.9±7752.2 | |
| F (%) | 54.2 | 31.8 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:rats, male beagle dogs[1]
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Dosage:
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Administration:1 mg/kg for i.v. and 10 mg/kg for p.o (rats); 2 mg/kg for i.v. and 10 mg/kg for p.o.(dogs)
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Result:Showed good oral bioavaliabily in rats (F=54.2%) and dogs (F=31.8%).
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Animal Model:male wistar rats (5 week, 160-180 g)[1]
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Dosage:10 mg/kg
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Administration:p.o.
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Result:Inhibited the lymphocyte egress from the lymphoid tissue to the peripheral blood and that lymphopenia can be recovered within 24 hours.
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Animal Model:female C57BL/6 mice (10 weeks,19−22 g) (experimental autoimmune encephalitis (EAE) mouse model)[1]
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Dosage:3, 10 mg/kg (dissolved in 2.5% DMSO and 5% Kolliphor HS 15 (Sigma-Aldrich) in distilled water)
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Administration:p.o., once daily, 20 days
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Result:Ameliorated the disease progression and overall severity in EAE mice, showing favorable drug-like properties.
Chemical Information
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CAS No. 2760666-20-2
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Masse moléculaire 450.89
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Formule C23H24ClN2NaO4
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SMILES
O=C(C1CN(CC2=CC=C(C=C2)C3=NOC(C3)C4=CC(Cl)=C(C=C4)OC(C)C)C1)O[Na]
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
S1P1 agonist 5 Related Classifications
HY-144126 Related Classifications
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