ELN 441958 - CAS 913064-47-8
Catalog number:
913064-47-8
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C29H29ClN4O2
Molecular Weight:
501.02
COA:
Inquire
Targets:
Bradykinin Receptor
Description:
ELN441958 is a novel, potent and selective bradykinin B1 receptor antagonist with Ki value of 0.26 nM. It competitively inhibited the binding of the agonist [3H]DAKD to the human B1 receptor in IMR-90 lung fibroblast cell membranes. It is highly selective for B1 over B2 receptors and >500/ 2000-fold selective for the B1 over μ/δ-opioid receptor. It 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. It exhibited good permeability and metabolic stability in vitro. It exhibited high oral bioavailability and moderate plasma half-lives in rats and rhesus monkeys. It does not inhibit the activation of the human bradykinin B2 receptor at concentrations up to 10 μM. It has a moderate clearance and volume of distribution in both species following i.v. administration, consistent with the high metabolic stability in rat, rhesus, and human microsomes.
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Purity:
>98%
Appearance:
Solid powder
Synonyms:
ELN-441958;7-Chloro-2-[3-[[9-(pyridin-4-yl)-3,9-diazaspiro[5.5]undecan-3-yl]carbonyl]phenyl]-2,3-dihydroisoindol-1-one
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
ELN441958 exhibited high oral bioavailability and moderate plasma half-lives.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams to Kilograms
Boiling Point:
738.4±60.0 °C | Condition: Press: 760 Torr
Density:
1.37±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
ARYQHSWJGHCGJS-UHFFFAOYSA-N
InChI:
InChI=1S/C29H29ClN4O2/c30-25-6-2-4-22-20-34(28(36)26(22)25)24-5-1-3-21(19-24)27(35)33-17-11-29(12-18-33)9-15-32(16-10-29)23-7-13-31-14-8-23/h1-8,13-14,19H,9-12,15-18,20H2
Canonical SMILES:
C1CN(CCC12CCN(CC2)C(=O)C3=CC(=CC=C3)N4CC5=C(C4=O)C(=CC=C5)Cl)C6=CC=NC=C6
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CAS 913064-47-8 ELN 441958

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