AKP-11 (Synonyms:S1P1 agonist 1)
目录号 : KCM10725 CAS No. : 1220973-37-4 纯度 : ≥95%
AKP-11 is an agonist of sphingosine-1-phosphate receptor 1 (S1P) with an EC value of 0.047 μM for [S]GTPγS binding to CHO-K1 cell membranes expressing the human receptor. It decreases surface expression of S1P and increases phosphorylation of Akt and ERK in CHO cells expressing S1P-HA when used at a concentration of 100 nM. AKP-11 (1.3 and 3 mg/kg) reduces protein levels of IFN-γ and IL-17 in spinal cord tissue and decreases disease severity in a rat model of experimental autoimmune encephalomyelitis (EAE). It decreases peripheral counts of total lymphocytes and total, CD4, CD8, and CD26L T cells in an EAE rat model, as well as in healthy control animals, when administered at a dose of 1.3 mg/kg.
规格 价格 是否有货 数量
1mg
In-stock
5mg
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10mg
In-stock
25mg 询价 In-stock
10 mM * 1 mL in DMSO 询价 In-stock

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生物活性

AKP-11 (S1P1 Agonist 1) is a S1P1 agonist with immunomodulatory activities.

体外研究

AKP-11 (S1P1 Agonist 1) binds to S1P1 is internalized and activates intracellular AKT and ERKs cellular signaling pathways.

AKP-11 (S1P1 Agonist 1) mediated S1P1 downregulation is independent of sphingosine kinase activity indicating it to be a direct agonist of S1P1.

AKP-11 (S1P1 Agonist 1) decreases cell surface expression of S1P1 in in vitro cell culture mode.

体内研究

AKP-11 (S1P1 Agonist 1) (1.3mg/kg) attenuates EAE disease. EAE is the animal model of multiple sclerosis which is extensively used for investigating clinical studies for multiple sclerosis drugs. AKP-11 (S1P1 Agonist 1) treatment reduces peripheral total blood lymphocyte and T lymphocyte counts significantly. The reduction in total lymphocytes and T cells are 48% and 41% in AKP11 treated animals, respectively. The reduction in the CD4+ and CD8+ T cell populations are 41% and 40% in S1P1 Agonist 1 treated animals, respectively. AKP-11 (S1P1 Agonist 1)treatment reduces CNS infiltration of T cells and Cytokines and enhances neuroprotection. AKP-11 (S1P1 Agonist 1) treatment has little effect on the heart rate of animals. The decrease in blood pressure is also smaller with S1P1 Agonist 1 treatment as compared animals treated with FTY720.

分子式
C22H22ClN3O5
分子量
443.88
CAS号
1220973-37-4
中文名称
AKP-11
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶解性数据
In Vitro: 

DMSO: ≥ 125 mg/mL (281.61 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
                                           
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
                                                                                                                    
1 mM 2.2529 mL 11.2643 mL 22.5286 mL
5 mM 0.4506 mL 2.2529 mL 4.5057 mL
10 mM 0.2253 mL 1.1264 mL 2.2529 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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