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.

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JP1302

JP1302 Chemical Structure

CAS No. : 80259-18-3

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Based on 1 publication(s) in Google Scholar

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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.html" class="link-product" target="_blank">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.
Appearance

Solid

Color

Brown to red

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (135.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7139 mL 13.5696 mL 27.1392 mL
5 mM 0.5428 mL 2.7139 mL 5.4279 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7139 mL 13.5696 mL 27.1393 mL 67.8481 mL
5 mM 0.5428 mL 2.7139 mL 5.4279 mL 13.5696 mL
10 mM 0.2714 mL 1.3570 mL 2.7139 mL 6.7848 mL
15 mM 0.1809 mL 0.9046 mL 1.8093 mL 4.5232 mL
20 mM 0.1357 mL 0.6785 mL 1.3570 mL 3.3924 mL
25 mM 0.1086 mL 0.5428 mL 1.0856 mL 2.7139 mL
30 mM 0.0905 mL 0.4523 mL 0.9046 mL 2.2616 mL
40 mM 0.0678 mL 0.3392 mL 0.6785 mL 1.6962 mL
50 mM 0.0543 mL 0.2714 mL 0.5428 mL 1.3570 mL
60 mM 0.0452 mL 0.2262 mL 0.4523 mL 1.1308 mL
80 mM 0.0339 mL 0.1696 mL 0.3392 mL 0.8481 mL
100 mM 0.0271 mL 0.1357 mL 0.2714 mL 0.6785 mL
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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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