Reversin 121 is a hydrophobic peptide chemosensitizer that can reverse P-glycoprotein-mediated multidrug resistance. It binds to the P-glycoprotein multidrug transporter (MDR1) with a K value of 77 nM. Reversin 121 modulates P-glycoprotein ATPase activity in Sf9 insect cell membranes expressing human MDR1, plasma membrane vesicles from multidrug-resistant cells, and reconstituted proteoliposomes as well as in a variety of MDR1-expressing intact tumor cells.
Reversin 121 is a P-glycoprotein inhibitor. Reversin 121 increases the ATPase activity of MDR1. Reversin 121 reverses P-glycoprotein-mediated multidrug resistance. Reversin 121 can be used in the research of cancers.
IC50&Target
P-glycoprotein
体外研究
Reversin 121 (12 μg/mL) (with gemcitabine) reduces the proportions of tumor cells positive for MDR proteins in Panc1 cell.
Reversin 121 (5 μM) reverses the resistance against paclitaxel in paclitaxel-resistant NCI-H460 cell.
Reversin 121 (10 μM, 48 h) inhibits T cell proliferation.
体内研究
Reversin 121 (2.5 mg/kg, plus 5-fluorouracil, 35 mg/kg/day, i.p.) decreases tumor size and prevalence of metastases.
Animal Model:
Orthotopic pancreatic carcinoma mouse model
Dosage:
2.5 mg/kg, plus 5-fluorouracil, 35 mg/kg/day
Administration:
Intraperitoneal injection (i.p.), 5 days a week
Result:
Decreased in MRP3-positive cells.
分子式
C34H47N3O9
分子量
641.75
CAS号
174630-04-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisture and light, under nitrogen
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: 100 mg/mL (155.82 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
1.5582 mL
7.7912 mL
15.5824 mL
5 mM
0.3116 mL
1.5582 mL
3.1165 mL
10 mM
0.1558 mL
0.7791 mL
1.5582 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 (sealed storage, away from moisture and light, 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。