1. Neuronal Signaling Apoptosis Metabolic Enzyme/Protease
  2. Imidazoline Receptor Caspase Mitochondrial Metabolism Lactate Dehydrogenase
  3. AGN 192403 hydrochloride

AGN 192403 hydrochloride  (Synonyms: (+)-BRD4780)

Cat. No.: HY-101374A Purity: 99.96%
Handling Instructions Technical Support

AGN 192403 (BRD4780) hydrochloride is a potent and selective imidazoline-1 receptor antagonist with a Ki value of 42 nM. AGN 192403 hydrochloride is also a TMED9 inhibitor. AGN 192403 hydrochloride shows protective effects on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. AGN 192403 hydrochloride mitigates the proliferation and migration of differentiated glioma tumor cells. AGN 192403 hydrochloride can be used for glioma tumor and neurological diseases research.

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

AGN 192403 hydrochloride

AGN 192403 hydrochloride Chemical Structure

CAS No. : 1021868-90-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of AGN 192403 hydrochloride:

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

AGN 192403 (BRD4780) hydrochloride is a potent and selective imidazoline-1 receptor antagonist with a Ki value of 42 nM. AGN 192403 hydrochloride is also a TMED9 inhibitor. AGN 192403 hydrochloride shows protective effects on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. AGN 192403 hydrochloride mitigates the proliferation and migration of differentiated glioma tumor cells. AGN 192403 hydrochloride can be used for glioma tumor and neurological diseases research[1][2].

IC50 & Target[1]

imidazoline-1 receptor

42 nM (Ki)

Caspase-9

 

In Vitro

AGN 192403 (10-100 μM, 24 h) hydrochloride inhibits the former lysosomal destabilization and the subsequent decrease in mitochondrial potential in astrocytes exposed to Naphthazarin (HY-N7526)[1].
AGN 192403 (10-100 μM, 24 h) hydrochloride inhibits the Antimycin A- and Rotenone (HY-B1756)-induced decrease in mitochondrial potential, cytochrome c release, caspase-9 activation, and eventually LDH release in astrocytes[1].
AGN 192403 (4-25 μM, 14 days) hydrochloride exerts a remarkable inhibitory effect on glioma stem cells (GSC)s self-renewal, demonstrating almost complete inhibition of self-renewal at the highest concentration applied[2].
AGN 192403 (0-25 μM, 18-48 h) hydrochloride targets TMED9, reduces the stemness, reduces GSC migration, and inhibits GSC tumorigenic functions[2].
AGN 192403 (4-25 μM, 0-8 days) hydrochloride induces cell death in a dose dependent manner in patient-derived GSCs[2].
AGN 192403 (4-25 μM, 48 h-8 days) hydrochloride inhibits TMED9 and exerts anti-tumor effects in diffuse intrinsic pontine glioma (DIPG) cells[2].

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

Western Blot Analysis[2]

Cell Line: patient-derived GSCs
Concentration: 0, 4, 10, 25 μM
Incubation Time: 48 h
Result: Decreased TMED9 expression in a dose-dependent manner in three different patient-derived GSCs.

RT-PCR[2]

Cell Line: GSCs
Concentration: 10, 25 μM
Incubation Time: 48 h
Result: Showed a marked and dose dependent reduction in SOX2 expression.
Markedly reduced YKL40 expression.

Cell Migration Assay [2]

Cell Line: GSCs
Concentration: 10, 25 μM
Incubation Time: 18-20 h
Result: Dose-dependently reduced GSC migration.

Cell Viability Assay[2]

Cell Line: GSCs
Concentration: 4, 10, 25 μM
Incubation Time: 0, 1, 2, 3, 4, 5, 6, 7, 8 days
Result: Resulted in a dose-dependent induction of cell death, at multiple points over the course of one week.
In Vivo

AGN 192403 (3000 μg/kg, i.v., single dose pretreat) hydrochloride can bloack imidazoline-1 receptor without modifying the baseline values of heart rate and blood pressure in rats[3].

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

Molecular Weight

189.73

Formula

C10H20ClN

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)[C@@H]1[C@@H](N)[C@H]2CC[C@@H]1C2.Cl

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 : 100 mg/mL (527.06 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 5.2706 mL 26.3532 mL 52.7065 mL
5 mM 1.0541 mL 5.2706 mL 10.5413 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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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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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (13.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (13.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.96%

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 5.2706 mL 26.3532 mL 52.7065 mL 131.7662 mL
5 mM 1.0541 mL 5.2706 mL 10.5413 mL 26.3532 mL
10 mM 0.5271 mL 2.6353 mL 5.2706 mL 13.1766 mL
15 mM 0.3514 mL 1.7569 mL 3.5138 mL 8.7844 mL
20 mM 0.2635 mL 1.3177 mL 2.6353 mL 6.5883 mL
25 mM 0.2108 mL 1.0541 mL 2.1083 mL 5.2706 mL
30 mM 0.1757 mL 0.8784 mL 1.7569 mL 4.3922 mL
40 mM 0.1318 mL 0.6588 mL 1.3177 mL 3.2942 mL
50 mM 0.1054 mL 0.5271 mL 1.0541 mL 2.6353 mL
60 mM 0.0878 mL 0.4392 mL 0.8784 mL 2.1961 mL
80 mM 0.0659 mL 0.3294 mL 0.6588 mL 1.6471 mL
100 mM 0.0527 mL 0.2635 mL 0.5271 mL 1.3177 mL
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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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AGN 192403 hydrochloride
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HY-101374A
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