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

JP1302 dihydrochloride 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 dihydrochloride shows antidepressant and antipsychotic-like effects. JP1302 dihydrochloride can be used for neuropsychiatric disorders and renal dysfunction research.

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

JP1302 dihydrochloride Chemical Structure

JP1302 dihydrochloride Chemical Structure

CAS No. : 1259314-65-2

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

JP1302 dihydrochloride 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 dihydrochloride shows antidepressant and antipsychotic-like effects. JP1302 dihydrochloride 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

441.40

Formula

C24H26Cl2N4

CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

CN1CCN(C2=CC=C(NC3=C(C=CC=C4)C4=NC5=CC=CC=C53)C=C2)CC1.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 12.5 mg/mL (28.32 mM; Need ultrasonic)

DMSO : 5 mg/mL (11.33 mM; ultrasonic and adjust pH to 5 with NaOH; 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 2.2655 mL 11.3276 mL 22.6552 mL
5 mM 0.4531 mL 2.2655 mL 4.5310 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 5 mg/mL (11.33 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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 (sealed storage, away from moisture). 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 / H2O 1 mM 2.2655 mL 11.3276 mL 22.6552 mL 56.6380 mL
5 mM 0.4531 mL 2.2655 mL 4.5310 mL 11.3276 mL
10 mM 0.2266 mL 1.1328 mL 2.2655 mL 5.6638 mL
H2O 15 mM 0.1510 mL 0.7552 mL 1.5103 mL 3.7759 mL
20 mM 0.1133 mL 0.5664 mL 1.1328 mL 2.8319 mL
25 mM 0.0906 mL 0.4531 mL 0.9062 mL 2.2655 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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JP1302 dihydrochloride Related Classifications

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  • 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 dihydrochloride
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HY-103213
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