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ELN-441958 is a potent, neutral antagonist of the B1 receptor, inhibiting the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with a Ki of 0.26 nM. ELN-441958 (ELN 441958) is highly selective for B1 over B2 receptors.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $56 | In Stock | |
| 5 mg | $137 | In Stock | |
| 10 mg | $223 | In Stock | |
| 25 mg | $377 | In Stock | |
| 50 mg | $538 | In Stock | |
| 100 mg | $732 | In Stock | |
| 200 mg | $988 | In Stock |
| Description | ELN-441958 is a potent, neutral antagonist of the B1 receptor, inhibiting the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with a Ki of 0.26 nM. ELN-441958 (ELN 441958) is highly selective for B1 over B2 receptors. |
| Targets&IC50 | Bradykinin B1:0.26 nM(ki) |
| Kinase Assay | IGF-IR Peptide Autophosphorylation: One microgram of constitutively active IGF-IR kinase domain peptide isincubated +/? varying concentrations of PQ 401 in 2% DMSO in 40 mM Tris (pH 7.4), 80 μMEGTA, 0.25% 2-mercaptoethanol, 80 μM Na3VO4, 10 mM MgCl2, and 2 mM MnCl2 for 20 minutes. ATP isthen added at a final concentration of 20 μM. Autophosphorylation of the kinase domain peptide isallowed to occur for 20 minutes at 22℃. The reaction isstopped by the addition of SDS-reducing buffer and the samples are run on SDS-PAGE. Following transfer to nitrocellulose membrane, peptide autophosphorylation isdetermined by Western blotting employing an antibody against phosphotyrosine (PY20). |
| Synonyms | ELN 441958 |
| Molecular Weight | 501.02 |
| Formula | C29H29ClN4O2 |
| Cas No. | 913064-47-8 |
| Smiles | Clc1cccc2CN(C(=O)c12)c1cccc(c1)C(=O)N1CCC2(CC1)CCN(CC2)c1ccncc1 |
| Relative Density. | 1.37 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 5.01 mg/mL (10 mM), Sonication is recommended. | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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