| Name | ELN-441958 |
| 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. |
| 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). |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 5.02 mg/mL (10.02 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2 mM), Sonication is recommended.
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| Keywords | low CNS exposure | Inhibitor | inhibit | high oral bioavailability | ELN-441958 | ELN441958 | BradykininReceptor | Bradykinin Receptor | B1 Receptor | anti-hyperalgesic |
| Inhibitors Related | Safotibant | NPC 567 acetate | [Des-Arg9]-Bradykinin acetate | Icatibant Acetate | B-Raf IN 14 | Anatibant 2HCl | (Hyp³)-Bradykinin acetate | Bradykinin (2-9) | MK-0686 | Zoliprofen | 5-Hydroxy-1-methylhydantoin | Sar-[D-Phe8]-des-Arg9-Bradykinin acetate |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Obesity Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | GPCR Compound Library | Anti-Cancer Compound Library |
United States
