1. GPCR/G Protein Neuronal Signaling
  2. Cannabinoid Receptor
  3. PGN36

PGN36 is a selective cannabinoid CB2 receptor (CB2R) antagonist with Kis of 0.09 µM and >40 µM for CB2R and CB1R, respectively. PGN36 abolishes the increase in collagen type I gene expression by the inducer of bone activity. PGN36 is able to cross the blood-brain barrier. PGN36 can be used for the study of frontotemporal dementia (FTD).

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PGN36 Chemical Structure

PGN36 Chemical Structure

CAS No. : 1564253-75-3

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Description

PGN36 is a selective cannabinoid CB2 receptor (CB2R) antagonist with Kis of 0.09 µM and >40 µM for CB2R and CB1R, respectively. PGN36 abolishes the increase in collagen type I gene expression by the inducer of bone activity. PGN36 is able to cross the blood-brain barrier. PGN36 can be used for the study of frontotemporal dementia (FTD)[1][2].

IC50 & Target

cannabinoid type-2 receptors

0.09 μM (Ki)

In Vivo

PGN36 (5 mg/kg; i.p.; daily; for three weeks) reverses cognitive decline, neurodegeneration and pyroptosis in a TAU protein-dependent frontotemporal dementia (FTD) mouse model[2].

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

Animal Model: Six-month-old mice received stereotaxic injections of an adeno-associated virus expressing human TAUP301L protein (AAV-TAUP301L) into the right hippocampus[2].
Dosage: 5 mg/kg
Administration: i.p.; daily; for three weeks
Result: Effectively alleviates TAUP301L-induced cognitive decline.
Reduced TAU protein expression levels and restore synaptic plasticity.
Modulated TAUP301L-induced pyroptosis.
Molecular Weight

365.43

Formula

C21H23N3O3

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=[N+](C1=CC2=C(N(CC3=CC=CC=C3)N=C2OCC4CCCCC4)C=C1)[O-]

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 12.5 mg/mL (34.21 mM; ultrasonic and warming and heat to 60°C; 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 2.7365 mL 13.6825 mL 27.3650 mL
5 mM 0.5473 mL 2.7365 mL 5.4730 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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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 2.7365 mL 13.6825 mL 27.3650 mL 68.4126 mL
5 mM 0.5473 mL 2.7365 mL 5.4730 mL 13.6825 mL
10 mM 0.2737 mL 1.3683 mL 2.7365 mL 6.8413 mL
15 mM 0.1824 mL 0.9122 mL 1.8243 mL 4.5608 mL
20 mM 0.1368 mL 0.6841 mL 1.3683 mL 3.4206 mL
25 mM 0.1095 mL 0.5473 mL 1.0946 mL 2.7365 mL
30 mM 0.0912 mL 0.4561 mL 0.9122 mL 2.2804 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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PGN36
Cat. No.:
HY-146134
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