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.
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。