Rivipansel
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 927881-99-0
- 分子式: C58H74N6O31S3
- 分子量:1447.42
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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 (sLex) 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 (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.
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Animal Model:Townes sickle cell disease (TNFα-induced cerebral microvascular occlusion)[1]
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Dosage:20 mg/kg
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Administration:i.v.; single dose
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Result:Rapidly reversed the TNFα-induced reduction in cerebral tissue perfusion.
Reduced the platelet microthrombi present in the cerebral microvasculature of TNFα-treated mice.
化学情報
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CAS 番号 927881-99-0
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分子量 1447.42
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分子式 C58H74N6O31S3
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SMILES
O=C([C@H]1C[C@H]([C@@H]([C@H](C1)NC(C2=CC(NC(N2)=O)=O)=O)O[C@H]3[C@H]([C@@H]([C@@H]([C@@H](O3)C)O)O)O)O[C@H]4[C@@H]([C@H]([C@H]([C@H](O4)CO)O)O[C@H](C(O)=O)CC5CCCCC5)OC(C6=CC=CC=C6)=O)NCCNC(COCCOCC(NC7=CC(S(=O)(O)=O)=CC8=C7C(S(=O)(O)=O)=CC(S(=O)(O)=O)=C8)=O)=O
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別名
GMI-1070
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)