Limaprost

SKU: orb1219287

Description

Limaprost is an analog of PGE1 with structural modifications intended to give it a prolonged half-life and greater potency.It is a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost can be used for pain relief, has antianginal effects, and has potential for ischaemic symptoms treatment.By a concentration-dependent manner, Limaprost inhibits the IL-1-mediated induction of nerve growth factor (IC50: 70.9 nM human IVD cells) [3].PGE1 and limaprost exhibited a novel pharmacological action that suppresses NGF expression in human IVD cells, and other prostanoids differentially regulated NGF expression. Limaprost has been used to treat patients with lumbar spinal stenosis in Japan and was proved to be effective in relieving symptoms.Platelet aggregation, adhesiveness, bleeding time, and thrombocytopenia induced by ADP and collagen infusion in guinea-pigs are inhibited by oral administration of Limaprost at the same doses or doses less than those relieving vasopressin-induced ST depression of ECG. Intra-coronary injection of Limaprost (1-100 ng/kg) in dogs causes a remarkable increase in coronary blood flow without any influence on heart rate, blood pressure, myocardial oxygen consumption, and redox potential. Limaprost given orally at more than 100 mg/kg relieves vasopressin-induced ST depression of rat electrocardiogram. Resistance in both large and small vessels of the dog coronary artery is decreased by intravenous injection of Limaprost (1-3 mg/kg).(In Vitro):Limaprost inhibits the IL-1-mediated induction of nerve growth factor (NGF) in a concentration-dependent manner with an IC50 value of 70.9 nM human IVD cells.(In Vivo):Limaprost (OP1206) given orally at more than 100 μg/kg relieves Argipressin-induced ST depression of rat electrocardiogram (ECG).Intra-coronary injection of Limaprost (OP1206; 1-100 ng/kg) in dogs results in a remarkable increase of coronary blood flow without any influence on heart rate, blood pressure, myocardial oxygen consumption and redox potential.Resistance in both large and small vessels of dog coronary artery is decreased by intravenous injection of Limaprost (OP1206; 1-3 mg/kg).Platelet aggregation, adhesiveness, bleeding time, and thrombocytopenia induced by ADP and collagen infusion in guinea-pigs are inhibited by oral administration of Limaprost (OP1206) at the same doses or doses less than those relieving Argipressin-induced ST depression of ECG.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 74397-12-9
• MW: 380.52
• Purity: >98% (HPLC)
• Formula: C₂₂H₃₆O₅
• SMILES: O=C(O)/C=C/CCCC[C@@H]1[C@@H](/C=C/[C@@H](O)C[C@@H](C)CCCC)[C@H](O)CC1=O
• Target: PGE synthase
• Solubility: DMSO:40 mg/mL (105.12 mM)

Bioactivity

• In Vivo:
  Limaprost (OP1206) given orally at more than 100 μg/kg relieves Argipressin-induced ST depression of rat electrocardiogram (ECG). Intra-coronary injection of Limaprost (OP1206; 1-100 ng/kg) in dogs results in a remarkable increase of coronary blood flow without any influence on heart rate, blood pressure, myocardial oxygen consumption and redox potential. Resistance in both large and small vessels of dog coronary artery is decreased by intravenous injection of Limaprost (OP1206; 1-3 mg/kg). Platelet aggregation, adhesiveness, bleeding time, and thrombocytopenia induced by ADP and collagen infusion in guinea-pigs are inhibited by oral administration of Limaprost (OP1206) at the same doses or doses less than those relieving Argipressin-induced ST depression of ECG.
• In Vitro:
  Limaprost inhibits the IL-1-mediated induction of nerve growth factor (NGF) in a concentration-dependent manner with an IC50 value of 70.9 nMhuman IVD cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

17α,20-dimethyl-δ2-PGE1,ONO1206,OP1206

Quick Database Links

Gene Symbol

PGE synthase