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. GW405833 hydrochloride

GW405833 hydrochloride  (Synonyms: L768242 hydrochloride)

Cat. No.: HY-110036A Purity: 99.59%
COA
SDS
Handling Instructions Technical Support

GW405833 (L768242) hydrochloride 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. 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.

GW405833 hydrochloride

GW405833 hydrochloride Chemical Structure

CAS No. : 1202865-22-2

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
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of GW405833 hydrochloride:

GW405833 hydrochloride Related Antibodies

Top Publications Citing Use of Products

View All Cannabinoid Receptor Isoform Specific Products:

View All Isoforms
CB1 CB2

View All HIF/HIF Prolyl-Hydroxylase Isoform Specific Products:

View All Isoforms
HIF-1α HIF

View All TNF Receptor Isoform Specific Products:

View All Isoforms
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

View All Interleukin Related Isoform Specific Products:

View All Isoforms
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GW405833 (L768242) hydrochloride 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. 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)[1][2][3][4][5][6].

IC50 & Target[1][5]

CB2

50.7 nM (IC50)

CB1

16.1 μM (IC50)

IL-1β

 

HIF-1α

 

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.

GW405833 hydrochloride 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

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.
Molecular Weight

483.82

Formula

C23H25Cl3N2O3
CAS No.
Appearance

Solid

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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0669 mL 10.3344 mL 20.6688 mL
5 mM 0.4134 mL 2.0669 mL 4.1338 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

GW405833 hydrochloride 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:

GW4058331202865-22-2L768242GW 405833GW-405833L 768242L-768242Cannabinoid ReceptorEndogenous MetaboliteHIF/HIF Prolyl-HydroxylaseTNF ReceptorInterleukin RelatedHypoxia-inducible factorsHIFsHIF-PHTumor Necrosis Factor ReceptorTNFRILCarrageenanPaw oedemaOxidative stressCannabinoidChronic Constriction injuryNeuropathic painSpinal cordInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GW405833 hydrochloride
Cat. No.:
HY-110036A
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

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) Portuguese - PT (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.