2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation
  3. Cannabinoid Receptor Endogenous Metabolite HIF/HIF Prolyl-Hydroxylase TNF Receptor Interleukin Related
  4. GW-405833

GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values ​​of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values ​​of 16.1 μM and 4772 nM for CB1. GW-405833 also exhibits non-competitive CB1 antagonist, exerting its analgesic and and anti-inflammatory effect through a CB1 receptor (rather than CB2) dependent mechanism. GW-405833 can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF).

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GW-405833

GW-405833 Chemical Structure

CAS No. : 180002-83-9

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Based on 1 publication(s) in Google Scholar

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GW-405833 Related Antibodies

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Description

GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB2) agonist. GW405833 has EC50 and Ki values ​​of 0.65 nM and 3.92 nM for CB2, and EC50 and Ki values ​​of 16.1 μM and 4772 nM for CB1. GW-405833 also exhibits non-competitive CB1 antagonist, exerting its analgesic and and anti-inflammatory effect through a CB1 receptor (rather than CB2) dependent mechanism. GW-405833 can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF)[1][2][3][4][5].

IC50 & Target[1][5]

CB2

50.7 nM (EC50)

CB1

16.1 μM (EC50)

IL-1β

 

HIF-1α

 

Cellular Effect
Cell Line Type Value Description References
CHO EC50
16.1 μM
Compound: GW405833; L768242
Agonist activity at human CB1 receptor expressed in CHO cells coexpressing Galpha16 assessed as reduction in forsklin-induced cAMP production incubated for 30 mins by cAMP Hunter assay based fluorometric analysis
Agonist activity at human CB1 receptor expressed in CHO cells coexpressing Galpha16 assessed as reduction in forsklin-induced cAMP production incubated for 30 mins by cAMP Hunter assay based fluorometric analysis
[PMID: 32952995]
CHO EC50
50.7 nM
Compound: GW405833; L768242
Agonist activity at human CB2 receptor expressed in CHO cells coexpressing Galpha16 assessed as reduction in forsklin-induced cAMP production incubated for 30 mins by cAMP Hunter assay based fluorometric analysis
Agonist activity at human CB2 receptor expressed in CHO cells coexpressing Galpha16 assessed as reduction in forsklin-induced cAMP production incubated for 30 mins by cAMP Hunter assay based fluorometric analysis
[PMID: 32952995]
In Vitro

GW-405833 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].
GW-405833 (10 μM, 25 h) 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.

GW-405833 Related Antibodies

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

GW-405833 (3-30 mg/kg, i.p., single dose) 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].
GW-405833 (3 mg/kg, i.v., single dose) inhibits inflammation and footpad edema of rats by reducing cytokine production and oxidative stress[3].
GW-405833 (10 mg/kg, i.p., single dose) 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: Increased the paw withdrawal threshold in CB2KO and WT mice in a dose-dependent manner.
Restored mechanical paw withdrawal thresholds relative to baseline in CB2KO and WT mice at doses as low as 10 mg/kg.
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: Increased the survival rate of mice.
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.
Molecular Weight

447.35

Formula

C23H24Cl2N2O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(C(Cl)=CC=C1)Cl)N2C3=C(C=C(OC)C=C3)C(CCN4CCOCC4)=C2C
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 : 116.67 mg/mL (260.80 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 2.2354 mL 11.1769 mL 22.3539 mL
5 mM 0.4471 mL 2.2354 mL 4.4708 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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In Vivo Dissolution Calculator
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Purity & Documentation

Purity: 98.91%

SDS (420 KB)

COA (250 KB) HNMR (263 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
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 2.2354 mL 11.1769 mL 22.3539 mL 55.8847 mL
5 mM 0.4471 mL 2.2354 mL 4.4708 mL 11.1769 mL
10 mM 0.2235 mL 1.1177 mL 2.2354 mL 5.5885 mL
15 mM 0.1490 mL 0.7451 mL 1.4903 mL 3.7256 mL
20 mM 0.1118 mL 0.5588 mL 1.1177 mL 2.7942 mL
25 mM 0.0894 mL 0.4471 mL 0.8942 mL 2.2354 mL
30 mM 0.0745 mL 0.3726 mL 0.7451 mL 1.8628 mL
40 mM 0.0559 mL 0.2794 mL 0.5588 mL 1.3971 mL
50 mM 0.0447 mL 0.2235 mL 0.4471 mL 1.1177 mL
60 mM 0.0373 mL 0.1863 mL 0.3726 mL 0.9314 mL
80 mM 0.0279 mL 0.1397 mL 0.2794 mL 0.6986 mL
100 mM 0.0224 mL 0.1118 mL 0.2235 mL 0.5588 mL
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GW-405833 Related Classifications

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.

Keywords:

GW-405833180002-83-9L768242GW405833GW 405833L 768242L-768242Cannabinoid ReceptorEndogenous MetaboliteHIF/HIF Prolyl-HydroxylaseTNF ReceptorInterleukin RelatedHypoxia-inducible factorsHIFsHIF-PHTumor Necrosis Factor ReceptorTNFRILCarrageenanPaw oedemaOxidative stressCannabinoidChronic Constriction injuryNeuropathic painSpinal cordInhibitorinhibitorinhibit

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