貨號	規格	價格	上海	北京	武漢	南京
S81011-5mg	99.2%	￥500.00 S81011-5mg ￥500.00 現貨	9 9	-	-	-
S81011-10mg	99.2%	￥900.00 S81011-10mg ￥900.00 現貨	8 8	-	-	-
S81011-25mg	99.2%	￥1600.00 S81011-25mg ￥1600.00 現貨	7 7	-	-	-
S81011-100mg	99.2%	￥4100.00 S81011-100mg ￥4100.00 現貨	7 7	-	-	-

產品介紹

Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation

產品描述：

靶點：

S1PR1：6 nM (IC50)；S1PR3：2068 nM (IC50)；S1PR4：1956 nM (IC50)；S1PR5：142 nM (IC50);S1PReceptor;?LPLReceptor

體內研究：

Ponesimod (30 and 175 mg/kg; once daily p.o. for 8 d) prevents delayed-type hypersensitivity in mice. Ponesimod (30 mg/kg by gavage 3 h before and 6 h after adjuvant injection followed by 100 mg/kg/day by administration as food admix for 18 days) prevents adjuvant-induced arthritis in rats. Ponesimod (0.3-100 mg/kg; a single oral gavage) causes a dose-dependent reduction in lymphocyte count, with a plateau effect being reached at 3 mg/kg in rats. Ponesimod (100 mg/kg; once daily oral gavage for 7 d) results in a lymphocyte count reduction to 1900 lymphocytes/μL, and this effect is maintained over the entire 7 days studies. Lymphocyte count returned to baseline levels within 48 h after discontinuation of dosing.

參考文獻：

1. Bolli MH, et al. 2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists. J Med Chem. 2010 May 27;53(10):4198-211. 2. Piali L, et al. The selective sphingosine 1-phosphate receptor 1 agonist ponesimod protects against lymphocyte-mediated tissue inflammation. J Pharmacol Exp Ther. 2011 May;337(2):547-56. 3. Brossard P, et al. Pharmacokinetics and pharmacodynamics of ponesimod, a selective S1P1 receptor modulator, in the first-in-human study. Br J Clin Pharmacol. 2013 Dec;76(6):888-96.

溶解性：

DMSO : ≥ 100 mg/mL (216.93 mM)

保存條件：

2-8℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.169 ml	10.847 ml	21.693 ml
5 mM	0.434 ml	2.169 ml	4.339 ml
10 mM	0.217 ml	1.085 ml	2.169 ml
50 mM	0.043 ml	0.217 ml	0.434 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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Ponesimod ( ACT-128800)

(2Z,5Z)-5-(3-chloro-4-((R)-2,3-dihydroxypropoxy)benzylidene)-2-(propyliMino)-3-(o-tolyl)thiazolidin-4-one