ELN441958 |
| رقم الكتالوجGC16820 |
ELN441958 هو مناهض لمستقبلات البراديكينين B1 قوي ومحايد وتنافسي وانتقائي مع Ki يبلغ 0.26 نانومتر ضد مستقبل براديكينين B1 البشري الأصلي.
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Cas No.: 913064-47-8
Sample solution is provided at 25 µL, 10mM.
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ELN441958 is a novel, potent and selective bradykinin B1 receptor antagonist with Ki value of 0.26 nM [1].
The bradykinin B1 receptor is a G-protein coupled receptor with principal ligand of bradykinin and plays an important role in chronic pain and inflammation [1].
ELN441958 is a novel, potent and selective bradykinin B1 receptor antagonist. In IMR-90 lung fibroblast cell membranes, ELN441958 competitively inhibited the binding of the agonist [3H]DAKD to the human B1 receptor with Ki value of 0.26 nM. In IMR-90 cells expressing the native human B1 receptor, ELN441958 concentration-dependently antagonized calcium mobilization induced by DAKD with KB value of 0.12 nM. ELN441958 is highly selective for B1 over B2 receptors. ELN441958 failed to inhibit the calcium mobilization induced by B2-receptor agonist BK. ELN441958 also inhibited human μ-, δ-, κ- opioid receptors and muscarinic M1 receptor with Ki values of 0.13, 0.69, 1.5 and 0.37 μM, respectively. ELN441958 is also an agonist at the δ-opioid receptor (EC50 = 0.76 μM) and μ-opioid receptor. In vitro, ELN441958 exhibited good permeability and metabolic stability [1].
In rats and rhesus monkeys, ELN441958 exhibited high oral bioavailability and moderate plasma half-lives. In rhesus monkeys, ELN441958 dose-dependently reduced the thermal hyperalgesia induced by carrageenan with ED50 value of ~3 mg/kg s.c [1].
Reference:
[1]. Hawkinson JE, Szoke BG, Garofalo AW, et al. Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958, J Pharmacol Exp Ther, 2007, 322(2): 619-630.
| Cas No. | 913064-47-8 | SDF | |
| Chemical Name | 7-chloro-2-(3-(9-(pyridin-4-yl)-3,9-diazaspiro[5.5]undecane-3-carbonyl)phenyl)isoindolin-1-one | ||
| Canonical SMILES | ClC1=CC=CC(CN2C3=CC=CC(C(N4CCC5(CC4)CCN(C6=CC=NC=C6)CC5)=O)=C3)=C1C2=O | ||
| Formula | C29H29ClN4O2 | M.Wt | 501.02 |
| الذوبان | DMSO : 100 mg/mL (199.59 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9959 mL | 9.9796 mL | 19.9593 mL |
| 5 mM | 0.3992 mL | 1.9959 mL | 3.9919 mL |
| 10 mM | 0.1996 mL | 0.998 mL | 1.9959 mL |
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
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