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ELN-441958 is a potent, neutral, competitive and selective oral bioavailable bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor.
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.
| Molecular Weight | 501.02 |
| Formula | C29H29ClN4O2 |
| CAS Number | 913064-47-8 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Bradykinin Receptor Products |
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| SSR240612
Treatment with the kinin B1 receptor antagonist, SSR240612, provided a protective effect against organ damage by interfering with multiple target functions, including the suppression of B1R-induced inflammation and platelet aggregation. |
| Icatibant (HOE 140) acetate
Icatibant (HOE-140) acetate is a potent and specific peptide antagonist of bradykinin B2 receptor, with IC50 value of 1.07 nM and Ki value of 0.798 nM, respectively. |
| Bradykinin
Bradykinin (bradykinin) is a vasodilator active peptide produced by the kinin-releasing enzyme-kinin system that modulates inflammation by causing vasodilation, increasing vascular permeability, and stimulating prostaglandin synthesis. |
| Icatibant
Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively. |
| [Des-Arg9]-Bradykinin
[Des-Arg9]-Bradykinin is a Bradykinin (B1) receptor agonist that displays selectivity for B1 over B2 receptors. |
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