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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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E655235-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $309.90 |
Specifications & Purity | 10mM in DMSO |
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Biochemical and Physiological Mechanisms | ELN-441958 is a potent, neutral, competitive and selective bradykinin B 1 receptor antagonist with a K i of 0.26 nM against native human bradykinin B 1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse. |
Storage Temp | Store at -80°C |
Shipped In | Ice chest + Ice pads |
Product Description | ELN-441958 is a potent, neutral, competitive and selective bradykinin B 1 receptor antagonist with a K i of 0.26 nM against native human bradykinin B 1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse In Vitro ELN-441958 is selective for primate over rodent B 1 receptors with a rank order potency (K B , nanomolar) of human (0.12 ± 0.02) ~ rhesus monkey (0.24 ± 0.01) > rat (1.5 ± 0.4) > mouse (14 ± 4). ELN-441958 has good permeability and metabolic stability. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo ELN-441958 (1-10 mg/kg; s.c.; once) dose-dependently reduces carrageenan-induced thermal hyperalgesia in a rhesus monkey tail-withdrawal model . ELN-441958 (0-10 mg/kg; i.v. or p.o.) exhibits a favorable pharmacokinetic profile in the rat and rhesus monkey . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Adult male and female rhesus monkeys Dosage: 1, 3, or 10 mg/kg Administration: Subcutaneous injection, 30 min before carrageenan injection Result: Increased the tail-withdrawal latencies in a dose-dependent manner. Animal Model: Rhesus monkeys or Sprague-Dawley rats Dosage: 2.5 or 10 mg/kg for rats, 1 mg/kg or 5 mg/kg for rhesus monkeys Administration: Intravenous injection (2.5 mg/kg and 1 mg/kg) or oral administration (10 mg/kg and 5 mg/kg) (Pharmacokinetic Analysis) Result: In rats: When dosed intravenously, showed a moderate volume of distribution (2.7 L/kg, approximately four times total body water) and a moderate clearance (0.96 L/h/kg, approximately 24% of hepatic blood flow). The terminal plasma half-life of this compound in rats was 1.7 h. When dosed orally, the concentrations increased to a maximum of 1.2 g/mL at 2 h after dosing. The oral availability was 57%. In rhesus monkeys: When dosed intravenously, showed a moderate volume of distribution (2.7 L/kg) and a moderate clearance (0.49 L/h/kg, approximately 32% of hepatic blood flow). The terminal plasma half-life was 3.9 h. When dosed orally, the concentrations increased to a maximum of 3.6 g/mL at 3.3 h after dosing. The calculated oral bioavailability was greater than 100%. IC50& Target:K i : 0.26 nM (native human bradykinin B 1 receptor) |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Canonical SMILES | C1CN(CCC12CCN(CC2)C(=O)C3=CC(=CC=C3)N4CC5=C(C4=O)C(=CC=C5)Cl)C6=CC=NC=C6 |
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Molecular Weight | 501 |