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2760666-20-2
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S1P1 agonist 5
CAS No. : 2760666-20-2
MCE 国际站：S1P1 agonist 5
产品活性：S1P1 agonist 5 是一种选择性和具有口服活性的 S1P1 激动剂。S1P1 agonist 5 抑制淋巴细胞从淋巴组织排出到外周血。S1P1 agonist 5 具有研究多发性硬化症 (MS) 的潜力。
研究领域：GPCR/G Protein
作用靶点：LPL Receptor
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.
In Vivo: S1P1 agonist 5 shows good oral bioavaliabily in rats (F=54.2%) and dogs (F=31.8%).
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.
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.
Pharmacokinetic Parameters of S1P1 in rats, male beagle dogs.
| 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 |
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文献和实验both equilibration steps; however, it is not necessary. 4. Treat cells with agonist. (typically 5-25'). 5. Quickly aspirate media and add fixative (~ 2 ml/well). Fix for 15-20'. 6. Wash 3x. 7. Aspirate the final wash, taking care to dry the edges
Performing Bronchoalveolar Lavage in the Mouse
. Activation of the lung S1P1 receptor reduces allergen‐induced plasma leakage in mouse. Brit. J. Pharmacol. 158:1295‐1301. Delayre‐Orthez, C., Becker, J., De Blay, F., Frossard, N
Guidelines for the Use of Anesthetics, Analgesics and Tranquilizers in Laboratory Animals
. These side-effects are seen more with the mixed effect opiates than the pure analgesics. Naloxone is a opiate antagonist that can be used to reverse the effects of other narcotics. Other opiates, like buprenorphine, nalbuphine and nalorphine, have mixed agonist
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