A bradykinin B1 receptor antagonist
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ELN441958

Item No. 43214

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-chloro-2,3-dihydro-2-[3-[[9-(4-pyridinyl)-3,9-diazaspiro[5.5]undec-3-yl]carbonyl]phenyl]-1H-isoindol-1-one
CAS Number
913064-47-8
Molecular Formula
C29H29ClN4O2
Formula Weight
501.0
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(N1CCC2(CC1)CCN(CC2)C3=CC=NC=C3)C4=CC=CC(N5CC6=C(C5=O)C(Cl)=CC=C6)=C4
InChi Code
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
InChi Key
ARYQHSWJGHCGJS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $65

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    5 mg

    $276

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    10 mg

    $423

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    Product Description

    ELN441958 is a bradykinin B1 receptor antagonist (Ki = 0.26 nM).1 It is selective for the bradykinin B1 receptor over a panel of greater than 100 enzymes and receptors at 10 µM but does bind to the μ-, δ-, and κ-opioid receptors and M1 muscarinic receptor (Kis = 0.13, 0.69, 1.5, and 0.37 µM, respectively). ELN441958 inhibits calcium mobilization induced by the bradykinin B1 receptor agonist (Des-Arg10)-kallidin (DAKD) in IMR-90 cells expressing the human bradykinin B1 receptor (KB = 0.12 nM). It increases tail withdrawal latencies in a rhesus monkey model of carrageenan-induced hyperalgesia when administered at doses of 3 or 10 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description 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. Pharmacol. Exp. Ther. 322(2), 619-630 (2007).