A 5-HT4 receptor partial agonist
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CJ-033466

Item No. 42394

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-amino-6-chloro-2-methyl-N-[[1-(2-methylpropyl)-4-piperidinyl]methyl]-imidazo[1,2-a]pyridine-8-carboxamide
CAS Number
519148-48-2
Molecular Formula
C19H28ClN5O
Formula Weight
377.9
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mLEthanol: Slightly soluble: 0.1-1 mg/mL
SMILES
CC(C)CN1CCC(CNC(C2=CC(Cl)=C(N)N3C2=NC(C)=C3)=O)CC1
InChi Code
InChI=1S/C19H28ClN5O/c1-12(2)10-24-6-4-14(5-7-24)9-22-19(26)15-8-16(20)17(21)25-11-13(3)23-18(15)25/h8,11-12,14H,4-7,9-10,21H2,1-3H3,(H,22,26)
InChi Key
ISKHMDNIWXPUGR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $31

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    5 mg

    $147

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    10 mg

    $278

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    25 mg

    $655

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    Product Description

    CJ-033466 is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4.1 It induces cAMP accumulation in HEK293 cells expressing human 5-HT4D receptors and relaxation of rat tunica muscularis mucosae strips (EC50s = 0.927 and 1.3 nM, respectively). CJ-033466 selectively binds to 5-HT4D over 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, and 5-HT2B receptors (Kis = 1.26, >4,820, >5,070, 2,150, 1,400, and 2,900 nM, respectively) and 5-HT3, 5-HT7, and dopamine D2 receptors (Kis = 4,590, >3,890, and 2,150 nM, respectively), as well as a panel of greater than 50 additional receptors at 1,000 nM. CJ-033466 (0.3 mg/kg) increases gastric antral motility in conscious dogs in the fasted or postprandial states. It reverses clonidine-induced decreases in gastric emptying in a dog model of gastroparesis. CJ-033466 also induces superoxide production in a light-dependent manner and is phototoxic to NIH3T3 fibroblasts (IC50s = 11.4 and 203.3 µg/ml in the presence and absence of light, respectively).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mikami, T., Ochi, Y., Suzuki, K., et al. 5-Amino-6-chloro-N-[(1-isobutylpiperidin-4-yl)methyl]-2-methylimidazo[1,2-α]pyridine-8-carboxamide (CJ-033,466), a novel and selective 5-hydroxytryptamine4 receptor partial agonist: Pharmacological profile in vitro and gastroprokinetic effect in conscious dogs. J. Pharmacol. Exp. Ther. 325(1), 190-199 (2008).

    2. Onoue, S., Igarashi, N., Yamauchi, Y., et al. In vitro phototoxic potential and photochemical properties of imidazopyridine derivative: A novel 5-HT4 partial agonist. J. Pharm. Sci. 97(10), 4307-4318 (2008).