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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Bradykinin Receptor Products |
|---|
| [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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