An imidazoline I1 receptor antagonist
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BRD4780 (hydrochloride)

Item No. 43542

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1R,2R,3R,4S)-rel-3-(1-methylethyl)-bicyclo[2.2.1]heptan-2-amine, monohydrochloride
CAS Number
1021868-90-5
Synonyms
  • AGN 192403
Molecular Formula
C10H19N • HCl
Formula Weight
189.7
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Soluble: ≥ 10 mg/mlPBS (pH 7.2): Soluble: ≥ 10 mg/ml
SMILES
CC([C@H]1[C@@]2([H])C[C@@](CC2)([H])[C@@H]1N)C.Cl
InChi Code
InChI=1S/C10H19N.ClH/c1-6(2)9-7-3-4-8(5-7)10(9)11;/h6-10H,3-5,11H2,1-2H3;1H/t7-,8+,9+,10+;/m1./s1
InChi Key
KSTGYMXUFHCTSM-MRUBQFBLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $31

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    5 mg

    $147

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    10 mg

    $247

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    50 mg

    $1,001

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    Product Description

    BRD4780 is an antagonist of the imidazoline I1 receptor (Ki = 42 nM).1 It is selective for the imidazoline I1 receptor over α1-, α2A-, α2B-, and α2C-adrenergic receptors (Kis = >100, >20, >20, and >20 µM, respectively). BRD4780 also binds to transmembrane P24 trafficking protein 9 (TMED9) in a thermal shift assay and releases mucin 1-fs (MUC1-fs), a mutant form of MUC1 caused by a frameshift mutation in MUC1, from TMED9-containing vesicles in kidney cells isolated from patients with MUC1 kidney disease.2 In vivo, BRD4780 (1, 10, and 50 mg/kg) reduces renal MUC1-fs accumulation in transgenic mice heterozygous for human MUC1-fs.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Munk, S.A., Lai, R.K., Burke, J.E., et al. Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent. J. Med. Chem. 39(6), 1193-1195 (1996).

    2. Dvela-Levitt, M., Kost-Alimova, M., Emani, M., et al. Small molecule targets TMED9 and promotes lysosomal degradation to reverse proteinopathy. Cell 178(3), 521-535 (2019).