Cat. No.: HY-110036A

GW405833 hydrochloride

(Synonyms: L768242 hydrochloride)

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Based on 1 Customer Validation

GW405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB₂) agonist. GW405833 has EC₅₀ and K_i values of 0.65 nM and 3.92 nM for CB₂, and EC₅₀ and K_i values of 16.1 μM and 4772 nM for CB₁. GW405833 hydrochloride also exhibits non-competitive CB₁ antagonist, exerting its analgesic effect through a CB₁ receptor (rather than CB₂) dependent mechanism. GW405833 hydrochloride can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 hydrochloride inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF).

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

Purity: 99.59%
CAS No.: 1202865-22-2
Formula: C₂₃H₂₅Cl₃N₂O₃
Molecular Weight:483.82

Storage:

4°C, sealed storage, away from moisture

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

GW405833 hydrochloride Chemical Structure

CAS No.: 1202865-22-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]^[5]

CB2

50.7 nM (IC₅₀)

CB1

16.1 μM (IC₅₀)

IL-1β

HIF-1α

All Cannabinoid Receptor Isoforms :

All Interleukin Related Isoforms :

All HIF/HIF Prolyl-Hydroxylase Isoforms :

All TNF Receptor Isoforms :

In Vitro

GW405833 hydrochloride behaves as a low-efficacy agonist in spleen membranes from human, mice and rats and exhibits a reverse agonist effect in hCB2-CHO cells^[4].
GW405833 (10 μM, 25 h) hydrochloride inhibits the proliferation of hepatic macrophages through downregulating HIF-1α to inhibit glycolysis^[5].

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

ELISA Assay^[5]

Cell Line:

RAW264.7 macrophages
Concentration:

10 μM
Incubation Time:

After 1 hour of pre-treatment, add LPS for 24 h
Result:

Reduced the expressions of TNF-α and IL-1β.

Western Blot Analysis^[5]

Cell Line:

RAW264.7 macrophages
Concentration:

10 μM
Incubation Time:

After 1 hour of pre-treatment, add LPS for 24 h
Result:

Inhibited the expression of HIF-1α, PKM2 and CB2R.

In Vivo

GW405833 (3-30 mg/kg, i.p., single dose) hydrochloride dose-dependently reverses mice mechanical abnormal pain in both neuropathic pain and inflammatory pain models through CB1 receptors rather than CB2 receptors and does not produce typical cannabinoid-like effects^[1].
GW405833 (3 mg/kg, i.v., single dose) hydrochloride inhibits inflammation and footpad edema of rats by reducing cytokine production and oxidative stress^[3].
GW405833 (10 mg/kg, i.p., single dose) hydrochloride protects against cell death in acute liver failure (ALF) rats model through downregulating HIF-1α to inhibit glycolysis^[5].

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

Animal Model:

Partial sciatic nerve ligation (PSNL) model to induce neuropathic pain and inflammatory model induced by complete Freund's adjuvant (CFA) (HY-153808) established in CB1KO mice and CB2KO mice, WT mice^[1]
Dosage:

3, 10 and 30 mg/kg
Administration:

Intraperitoneal injection (i.p.), single dose
Result:

Retained antiallodynic effects in CB2KO mice.
Produced a dose-dependent increase in mechanical threshold in WT mice, but this antiallodynic effect was absent in CB1KO mice.
Blocked the antihyperalgesic effect by the CB1 antagonist rimonabant (HY-14136), but not by the CB2 antagonist SR144528 (HY-13439). Did not produce typical cannabinoid-like effects and did not trigger stage symptoms.

Animal Model:

The footpad edema model induced by Carrageenan (HY-125474) model established in Wistar‑albino rats weighing 200-250 g^[3]
Dosage:

3 mg/kg
Administration:

Intravenous injection (i.v.), single dose
Result:

Significantly reduced the levels of serum TNF-α and IL-1β.
Reduced the MDA content in the tissue, increased the GSH level, and inhibited the MPO activity.
Significantly reduced the infiltration of inflammatory cells and restored tissue damage.

Animal Model:

ALF model established in male Wistars rats(200-350 g)^[5]
Dosage:

10 mg/kg
Administration:

Intraperitoneal injection (i.p.), single dose
Result:

Significantly reduced ALT/AST levels, with a downward trend observed in TBIL but not reaching statistical significance.
Reduced F4/80+, significantly inhibited CD86, and increased CD206.
Reduced the expressions of TNF-α and IL-1β, as well as HIF-1α.
The regulatory effects on liver function, inflammatory factors and HIF-1α completely disappeared in CB2R-/- mice.

Chemical Information

CAS No. 1202865-22-2
Appearance Solid
Molecular Weight 483.82
Formula C₂₃H₂₅Cl₃N₂O₃
Color White to off-white
SMILES

O=C(C1=C(C(Cl)=CC=C1)Cl)N2C3=C(C=C(OC)C=C3)C(CCN4CCOCC4)=C2C.Cl
Synonyms

L768242 hydrochloride
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:

DMSO : 125 mg/mL (258.36 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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0669 mL

10.3344 mL

20.6688 mL

5 mM

0.4134 mL

2.0669 mL

4.1338 mL

10 mM

0.2067 mL

1.0334 mL

2.0669 mL

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.

Molarity Calculator

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

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Li AL, Carey LM, Mackie K, Hohmann AG. Cannabinoid CB2 Agonist GW405833 Suppresses Inflammatory and Neuropathic Pain through a CB1 Mechanism that is Independent of CB2 Receptors in Mice. J Pharmacol Exp Ther. 2017;362(2):296-305. [Content Brief]

[2]. Li J, et al. Indole compounds with N-ethyl morpholine moieties as CB2 receptor agonists for anti-inflammatory management of pain: synthesis and biological evaluation. Medchemcomm. 2019 Sep 17;10(11):1935-1947. [Content Brief]

[3]. Parlar A, Arslan SO, Doğan MF, et al. The exogenous administration of CB2 specific agonist, GW405833, inhibits inflammation by reducing cytokine production and oxidative stress. Exp Ther Med. 2018;16(6):4900-4908. [Content Brief]

[4]. Marini P, Cascio MG, King A, Pertwee RG, Ross RA. Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors. Br J Pharmacol. 2013;169(4):887-899. [Content Brief]

[5]. Cai SL, et al. CB2R agonist GW405833 alleviates acute liver failure in mice via inhibiting HIF-1α-mediated reprogramming of glycometabolism and macrophage proliferation. Acta Pharmacol Sin. 2023 Jul;44(7):1391-1403. [Content Brief]

[6]. Valenzano KJ, et al. Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy. Neuropharmacology. 2005 Apr;48(5):658-72. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0669 mL	10.3344 mL	20.6688 mL	51.6721 mL
	5 mM	0.4134 mL	2.0669 mL	4.1338 mL	10.3344 mL
	10 mM	0.2067 mL	1.0334 mL	2.0669 mL	5.1672 mL
	15 mM	0.1378 mL	0.6890 mL	1.3779 mL	3.4448 mL
	20 mM	0.1033 mL	0.5167 mL	1.0334 mL	2.5836 mL
	25 mM	0.0827 mL	0.4134 mL	0.8268 mL	2.0669 mL
	30 mM	0.0689 mL	0.3445 mL	0.6890 mL	1.7224 mL
	40 mM	0.0517 mL	0.2584 mL	0.5167 mL	1.2918 mL
	50 mM	0.0413 mL	0.2067 mL	0.4134 mL	1.0334 mL
	60 mM	0.0344 mL	0.1722 mL	0.3445 mL	0.8612 mL
	80 mM	0.0258 mL	0.1292 mL	0.2584 mL	0.6459 mL
	100 mM	0.0207 mL	0.1033 mL	0.2067 mL	0.5167 mL

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GW405833 hydrochloride

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All Cannabinoid Receptor Isoforms

All Interleukin Related Isoforms

All HIF/HIF Prolyl-Hydroxylase Isoforms

All TNF Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GW405833 hydrochloride Related Classifications

HY-110036A Related Classifications