| Identification | Back Directory | [Name]
REVERSIN 121 | [CAS]
174630-04-7 | [Synonyms]
REVERSIN 121
BOC-ASP(OBZL)-LYS(Z)-OTBU
L-Lysine, N-[(1,1-dimethylethoxy)carbonyl]-L-α-aspartyl-N6-[(phenylmethoxy)carbonyl]-, 2-(1,1-dimethylethyl) 1-(phenylmethyl) ester | [Molecular Formula]
C34H47N3O9 | [MDL Number]
MFCD03788012 | [MOL File]
174630-04-7.mol | [Molecular Weight]
641.75 |
| Chemical Properties | Back Directory | [Melting point ]
200°C | [Boiling point ]
786.8±60.0 °C(Predicted) | [density ]
1.163±0.06 g/cm3(Predicted) | [storage temp. ]
−20°C | [solubility ]
DMSO or ethanol: soluble | [form ]
powder | [pka]
10.75±0.46(Predicted) | [color ]
white |
| Hazard Information | Back Directory | [Description]
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 Kd 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. | [Uses]
Reversin 121 has been used to determine the activity of P-glycoprotein in human retinal pigment epithelium. | [General Description]
Reversin 121 is an analog of reversin and a dipeptide derivative. | [Biochem/physiol Actions]
Peptide chemosensitizer, inhibitor of P-glycoprotein. | [in vivo]
Reversin 121 (2.5 mg/kg, plus 5-fluorouracil, 35 mg/kg/day, i.p.) decreases tumor size and prevalence of metastases[1].
| Animal Model: | Orthotopic pancreatic carcinoma mouse model[1]. | | 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. |
| [References]
[1] FRANCES J SHAROM . Interaction of the P-glycoprotein multidrug transporter (MDR1) with high affinity peptide chemosensitizers in isolated membranes, reconstituted systems, and intact cells[J]. Biochemical pharmacology, 1999, 58 4: Pages 571-586. DOI: 10.1016/s0006-2952(99)00139-2
[2] EUNICE L KWAK. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2005, 102 21: 7665-7670. DOI: 10.1073/pnas.0502860102
[3] PRIYANKA S. RANA . Calibration and characterization of intracellular Asante Potassium Green probes, APG-2 and APG-4[J]. Analytical biochemistry, 2019, 567: Pages 8-13. DOI: 10.1016/j.ab.2018.11.024 |
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