GLPBio

ELN441958

Catalog No.: GC16820Purity:>98.00%
COASDSData Sheet
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.

ELN441958
Cas No.: 913064-47-8
1mgIn Stock
$41.00
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5mgIn Stock
$103.00
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10mgIn Stock
$166.00
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25mgIn Stock
$277.00
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50mgIn Stock
$391.00
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Citations

1 publicationsPublications from researchers using this product
IF 18

Description

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.

Protocol

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:
[1] 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
[2] 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.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
913064-47-8
Chemical Name
7-chloro-2-(3-(9-(pyridin-4-yl)-3,9-diazaspiro[5.5]undecane-3-carbonyl)phenyl)isoindolin-1-one
SMILES
ClC1=CC=CC(CN2C3=CC=CC(C(N4CCC5(CC4)CCN(C6=CC=NC=C6)CC5)=O)=C3)=C1C2=O
Molecular Formula
C29H29ClN4O2
Molecular Weight
501.02
Solubility
DMSO : 100 mg/mL (199.59 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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