ELN-441958
CAS No. : 913064-47-8
| Size | Price | Stock |
|---|---|---|
| 5mg | $280 | In-stock |
| 10mg | $450 | In-stock |
| 25mg | $900 | In-stock |
| 50mg | $1440 | In-stock |
| 100 mg | Get quote | |
| 200 mg | Get quote | |
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| Cat. No. : | HY-15043 |
| M.Wt: | 501.02 |
| Formula: | C29H29ClN4O2 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse[1].
IC50 & Target: Ki: 0.26 nM (native human bradykinin B1 receptor)[1]
In Vitro: ELN-441958 is selective for primate over rodent B1 receptors with a rank order potency (KB, nanomolar) of human (0.12 ± 0.02) ~ rhesus monkey (0.24 ± 0.01) > rat (1.5 ± 0.4) > mouse (14 ± 4)[1].
ELN-441958 has good permeability and metabolic stability[1].
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[1].
ELN-441958 (0-10 mg/kg; i.v. or p.o.) exhibits a favorable pharmacokinetic profile in the rat and rhesus monkey[1].
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