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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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[Hyp3]-Bradykinin
[Hyp3]-Bradykinin, naturally occurring peptide hormone, is a bradykinin receptor agonist. |
Bradykinin (1-6)
Bradykinin (1-6) is an amino-truncated Bradykinin peptide. |
Lys-[Des-Arg9]Bradykinin TFA
Lys-[Des-Arg9]Bradykinin TFA, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. |
Lobradimil
Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). |
[Tyr8] Bradykinin
[Tyr8] Bradykinin is a B2 kinin receptor agonist. |
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