RP 001 (hydrochloride)
目录号 : KCM12036 CAS No. : 1781880-34-9 纯度 : ≥98%
RP 001 is a potent sphingosine-1-phosphate receptor 1 (S1P) agonist (EC = 9 pM). It is competitive with W146 , a selective S1P antagonist, and induces internalization and polyubiquitination of S1P in a dose-dependent manner. RP 001 induces dose-dependent lymphopenia in mice (EC = 0.03 mg/kg). It reduces S1P-EGFP expression ex vivo on lymphocytes in the isolated lymph node of Edg1 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.
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生物活性

RP 001 (hydrochloride) is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP 001 (hydrochloride) induces internalization and polyubiquitination of S1P1. RP 001 (hydrochloride) has little activity on S1P2-S1P4 and only moderate affinity for S1P5.

体外研究

RP 001 (hydrochloride) elicits dose-dependent lymphopenia of CD4+ T cells. RP 001 (hydrochloride) induces acute lymphopenia with rapid recovery to untreated levels.

体内研究

RP-001 hydrochloride causes dose-dependent rapid lymphopenia with an EC50 of 0.03 mg/kg.

分子式
C24H24N4O4.HCl
分子量
468.93
CAS号
1781880-34-9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

DMSO: 29.4 mg/mL (62.70 mM; Need ultrasonic and warming)

配制储备液
                                           
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
                                                                                                                    
1 mM 2.1325 mL 10.6626 mL 21.3251 mL
5 mM 0.4265 mL 2.1325 mL 4.265 mL
10 mM 0.2133 mL 1.0663 mL 2.1325 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 (protect from light, stored under nitrogen)。-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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工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,

体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

配置后的溶液总体积:

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