1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. JP1302

JP1302 is a potent, selective, high affinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 shows antidepressant and antipsychotic-like effects. JP1302 can be used for neuropsychiatric disorders and renal dysfunction research.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (JP1302 dihydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

JP1302 Chemical Structure

JP1302 Chemical Structure

CAS No. : 80259-18-3

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Description

JP1302 is a potent, selective, high affinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 shows antidepressant and antipsychotic-like effects. JP1302 can be used for neuropsychiatric disorders and renal dysfunction research[1][2][3].

IC50 & Target

human α2C-adrenoceptor

28±2 nM (Ki)

human α2B-adrenoceptor

1470±130 nM (Ki)

human α2A-adrenoceptor

3150±50 nM (Ki)

rodent α2D-adrenoceptor

1700±200 nM (Ki)

In Vitro

JP1302 shows about 100-fold higher affinity than for α2A or α2B[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JP1302 (1-10 μmol/kg) decreases immobility time in the FST to a level similar to that seen with 10-30 μmol/kg of the antidepressant Desipramine (HY-B1272A)[1].
JP1302 (5 μmol/kg, once) is capable of complete reversal of the impairment in PPI induced in Sprague-Dawley rats by the psychotomimetic NMDA receptor antagonist, phencyclidine and similar results are found in Wistar rats[1].
JP1302 (3 mg/kg, IV, once) significantly ameliorates renal dysfunction[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague Dawley rats (8 weeks old)[3]
Dosage: 3 mg/kg
Administration: IV, pre-treatment: administered 5 min before the induction of ischemia, post-treatment: injected 45 min after the initiation of reperfusion
Result: Significantly ameliorated renal dysfunction in the rats at 24 h after reperfusion. post-ischemic administration of JP-1302 significantly ameliorated renal dysfunction, histological damage and reduced apoptotic cells and pro-inflammatory cytokine mRNA expression.
Molecular Weight

368.47

Formula

C24H24N4

CAS No.
SMILES

CN1CCN(C2=CC=C(NC3=C(C=CC=C4)C4=NC5=CC=CC=C53)C=C2)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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JP1302 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
JP1302
Cat. No.:
HY-103213A
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