ELN441958 |
Catalog No.GC16820
One-Click Copy Product Info
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ELN441958 is a potent, competitive, and selective bradykinin B1 receptor antagonist with a Ki value of 0.26nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 913064-47-8
Sample solution is provided at 25 µL, 10mM.
ELN441958 is a potent, competitive, and selective bradykinin B1 receptor antagonist with a Ki value of 0.26nM [1]. ELN441958 can target Nsp12_ortho and Nsp12_Palm1 sites and has potential inhibitory activity against SARS-CoV-2 replication[2]. ELN441958 has been widely used to alleviate thermal hyperalgesia in animal models[3].
In vitro, ELN441958 treatment at 1µM for 4h significantly inhibited octapeptide [des-Arg9]-Bradykinin (DABK) (0.1µM; 4h)-induced PTGS2 expression in human amniotic fibroblasts (HAFs)[4].
In vivo, ELN441958 treatment via subcutaneous injection at a single dose of 1mg/kg for 30min reduced anxiety-like behavior in DBA/2NCrl mice[5].
References:
[1] Hawkinson J E, Szoke B G, Garofalo A W, et al. Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958[J]. The Journal of pharmacology and experimental therapeutics, 2007, 322(2): 619-630.
[2] Gervasoni S, Manelfi C, Adobati S, et al. Target prediction by multiple virtual screenings: analyzing the SARS-CoV-2 phenotypic screening by the docking simulations submitted to the MEDIATE initiative[J]. International Journal of Molecular Sciences, 2023, 25(1): 450.
[3] Wisniewski P, Gangnus T, Burckhardt B B. Recent advances in the discovery and development of drugs targeting the kallikrein-kinin system[J]. Journal of translational medicine, 2024, 22(1): 388.
[4] Ni X, Wang W, Liu Y, et al. The bradykinin system contributes to the regulation of prostaglandin-endoperoxide synthase 2 expression in human amnion fibroblasts: Implications for term and preterm birth[J]. Frontiers in Endocrinology, 2022, 13: 873727.
[5] Rouhiainen A, Kulesskaya N, Mennesson M, et al. The bradykinin system in stress and anxiety in humans and mice[J]. Scientific reports, 2019, 9(1): 19437.
| Cell experiment [1]: | |
Cell lines | Human amnion fibroblasts (HAFs) |
Preparation Method | HAFs were cultured in DMEM medium containing 10% fetal bovine serum (FCS) and 1% antibiotics at 37°C in 5% CO2-95% air for 3 days. The medium was replaced with DMEM medium without phenol red and fetal bovine serum, and HAFs were treated with DABK (0.1µM) in the presence or absence of the ELN441958 (1µM) for 4h before measuring PTGS2 mRNA and protein abundance. |
Reaction Conditions | 1μM; 4h |
Applications | ELN441958 treatment inhibited the levels of PTGS2 mRNA and protein in HAFs induced by DABK. |
| Animal experiment [2]: | |
Animal models | DBA/2NCrl mice |
Preparation Method | 5-to 8-week-old DBA/2NCrl male mice were acclimated in a controlled temperature (22±2°C) and humidity (50±15%) facility with a 12-h light/dark cycle (lights on from 06:00 to 18:00), with ad libitum access to food and water, and housed individually for at least 1 week before experiments. Behavioral tests were performed 30 minutes after subcutaneous injection of a single dose (1mg/kg) of ELN441958. |
Dosage form | 1mg/kg for once; s.c. |
Applications | ELN441958 treatment significantly reduced anxiety-like behaviors in DBA/2NCrl mice. |
References: | |
| 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 |
| Solubility | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9959 mL | 9.9796 mL | 19.9593 mL |
| 5 mM | 399.2 μL | 1.9959 mL | 3.9919 mL |
| 10 mM | 199.6 μL | 998 μL | 1.9959 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)