Rivipansel  (Synonyms: GMI-1070)

Rivipansel is a small-molecule glycomimetic pan-selectin antagonist with inhibitory activity against E-selectin and P-selectin. Rivipansel binds tightly to the lectin domain of E-selectin, and selectively blocks the recognition of CD62L by E-selectin without affecting the binding of PSGL-1 to E-selectin. Rivipansel functionally inhibits the adhesion of hematopoietic cells to endothelial cells, and is applicable to research related to sickle cell disease^[1][2].

Rivipansel dose-dependently inhibits HL-60 cell adhesion to E-selectin-expressing CHO cells in an in vitro shear flow assay, with greater activity against E-selectin than P-selectin^[1].
Rivipansel (~6.5 μM) inhibits rolling of isolated human polymorphonuclear neutrophils (PMN) on a recombinant human E-selectin/ICAM-1 coated substrate with a IC₅₀ of ~6.5 μM, via a mechanism independent of PSGL-1^[2].
Rivipansel (6.5 μM) reduces E-selectin recognition of sialyl LewisX (sLe^x) on CD62L in isolated human polymorphonuclear neutrophil (PMN) lysates by ~70%^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Rivipansel (5-20 mg/kg; i.v.; single dose or single dose plus second dose) dose-dependently inhibits leukocyte adhesion and neutrophil-platelet aggregate formation in Townes SCD mice, with significant effects observed at 10 and 20 mg/kg and maximal efficacy at 20 mg/kg^[1].
Rivipansel (20 mg/kg; i.v.; single dose) rapidly restores cerebral tissue perfusion and reduces cerebral platelet microthrombi in TNFα-induced cerebral occlusion in Townes SCD mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1447.42

C₅₈H₇₄N₆O₃₁S₃

927881-99-0

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• [1]. Reema Jasuja, et al. Rivipansel: A Small Pan-Selectin Antagonist Improves Cerebral Perfusion and Inhibits Leukocyte Adhesion and in Murine Sickle Cell Disease Model. Blood (2016) 128 (22): 270.

  [2]. Scott I Simon, et al. Rivipansel (GMI-1070) Inhibits E-Selectin Recognition of Sialyl LewisX Expressed on CD62L (L-selectin) and Blocks Integrin Activation and Arrest of Human Neutrophils. Blood (2016) 128 (22): 2509.