DREADD agonist 21

CAS No. 56296-18-5

DREADD agonist 21 ( —— )

Catalog No. M26175 CAS No. 56296-18-5

DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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2MG 42 In Stock
5MG 80 In Stock
10MG 115 In Stock
25MG 215 In Stock
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Biological Information

  • Product Name
    DREADD agonist 21
  • Note
    Research use only, not for human use.
  • Brief Description
    DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).
  • Description
    DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).(In Vitro):DREADD agonist 21 is a highly selective and potent agonist for muscarinic DREADDs (pEC50 for hM1Dq=6.54 and that for hM4Di=7.77 in pERK assays). DREADD agonist 21 potently activates hM3Dq in Chinese hamster ovary (CHO) cells transfected cells in vitro (pEC50: 8.48±0.05) and it also potently activates hM1Dq, hM3Dq, and hM4Di. DREADD agonist 21 does not activate human M3 receptor (hM3). DREADD agonist 21 displays high binding affinities to 5HT2A and 5HT2C serotonin receptor, α1A adrenergic receptor, and H1 histamine receptor with Ki values of 66, 170, 280, and 6 nM, respectively. In addition to being inactive at hM3, DREADD agonist 21, a potent full agonist of hM3Dq (EC50=1.7 nM), is only 3.5-fold selective for hM3Dq over H1, 40-fold selective over 5HT2A, 100-fold selective over 5HT2C, and 165-fold selective over α1A. DREADD agonist 21 binds to hM1, hM4, hM1Dq and hM4Di receptors (pKis of 5.97, 5.44, 7.20, and 6.75, respectively). (In Vivo):DREADD agonist 21 has excellent pharmacokinetic properties, bioavailability and brain penetrability. DREADD agonist 21 (0.3, 1.0, and 3.0 mg/kg; i.p.) activates neuronal hM3Dq in mice. DREADD agonist 21 (0.1, 1, and 10 mg/kg; i.p.) shows 95.1% plasma protein binding and 95% brain protein bounding in mice.
  • Synonyms
    ——
  • Pathway
    Endocrinology/Hormones
  • Target
    5-HT Receptor
  • Recptor
    Nuclear receptor NOT
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    56296-18-5
  • Formula Weight
    278.4
  • Molecular Formula
    C17H18N4
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    C1CN(CCN1)C1=Nc2ccccc2Nc2ccccc12
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.A Almario Garcia, P Lardenois, A Olivier. 2-ARYL-6-PHENYLIMIDAZO[1,2-α]PYRIDINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF:WO, WO2008034974 A1.
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