| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
hCB2-R 7.3 (pEC50) rat CB2-R 7.5 (pEC50)
GW 833972A targets the cannabinoid type 2 (CB2) receptor as a selective agonist. It shows high potency at CB2 with pEC50 values of 7.3 for human CB2 and 7.5 for rat CB2. The compound exhibits 1000-fold selectivity over the CB1 receptor. GW 833972A also binds to BMAL2 (brain and muscle ARNT-like protein 2) with high affinity and facilitates its protein degradation. The compound's mechanism involves CB2 receptor activation, which modulates immune responses and inflammation. |
|---|---|
| ln Vitro |
Inhibiting capsaicin-induced depolarization in humans and guinea pigs, as well as prostaglandin E(2) and hypertonic saline-induced depolarization of the isolated guinea pig vagus nerve, are the effects of GW 833972A (0.3-300 μM; 10 min) [1].
In vitro, GW 833972A demonstrates potent CB2 agonist activity with pEC50 values of 7.3 (human CB2) and 7.5 (rat CB2). It shows 1000-fold selectivity over CB1 receptors. The compound inhibits induced neuronal depolarization in sensory nerve preparations. It also binds to BMAL2 with high affinity and facilitates its protein degradation. Standard in vitro assays include receptor binding studies, [35S]GTPγS binding assays for G protein activation, cAMP accumulation assays, and electrophysiological recordings of neuronal depolarization. |
| ln Vivo |
Citric acid-induced coughing in conscious guinea pigs is inhibited by GW 833972A (30 mg/kg, 2 mL/kg; intraperitoneal injection; single dosage, administered 30 minutes before the commencement of the test). Additionally, it prevents the major bronchus from leaking plasma proteins when exposed to capsaicin [1].
In vivo, GW 833972A inhibits citric acid-induced cough in animal models. The compound's CB2 agonist activity and inhibition of neuronal depolarization contribute to its antitussive effects. The compound has been studied in guinea-pig and human airway sensory nerve function models. Its high selectivity for CB2 over CB1 (1000-fold) suggests that its effects are mediated primarily through CB2 activation with minimal CB1-related side effects. The compound is used in research to study respiratory conditions and cough. |
| Enzyme Assay |
For non-cell-based receptor binding assays, GW 833972A can be evaluated using membrane preparations from cells expressing human or rat CB2 or CB1 receptors. Radioligand binding displacement experiments are performed using [3H]-CP55940 as the radiolabeled ligand. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at 30°C for 60 minutes. Bound radioligand is separated from free by filtration through GF/B filters. Nonspecific binding is determined in the presence of excess unlabeled ligand. Ki or IC50 values are calculated from displacement curves.
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| Cell Assay |
For in vitro cellular assays, cells expressing human or rat CB2 receptors are cultured in appropriate media. For G protein activation assays, [35S]GTPγS binding is measured in membrane preparations. Cells are treated with various concentrations of the compound and bound [35S]GTPγS is measured. For cAMP accumulation assays, cells are pre-incubated with forskolin to stimulate cAMP production, then treated with various concentrations of the compound. cAMP levels are measured using ELISA or HTRF-based detection. For neuronal depolarization assays, sensory nerve preparations are mounted in tissue baths and compound effects on depolarization are measured electrophysiologically.
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| Animal Protocol |
For in vivo animal studies, GW 833972A is typically administered to rodents or guinea pigs via oral or intraperitoneal administration. In cough models, citric acid aerosol is used to induce cough, and the number of coughs is counted following compound administration. In models of airway inflammation, inflammatory markers and airway hyperresponsiveness are assessed. Dosing regimens vary depending on the specific model. Blood and tissue samples may be collected for pharmacokinetic analysis.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of GW 833972A have not been extensively characterized. The compound has a molecular weight of 444.24 and a molecular formula of C18H14Cl2F3N5O. Based on its molecular properties, the compound is expected to have moderate lipophilicity and good oral bioavailability. Comprehensive ADME studies would be needed for full pharmacokinetic characterization, including assessment of oral bioavailability, half-life, protein binding, and tissue distribution.
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| Toxicity/Toxicokinetics |
The toxicity profile of GW 833972A has not been extensively reported. As a selective CB2 agonist with 1000-fold selectivity over CB1, it is expected to have minimal psychoactive side effects. The compound is for research use only and not for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies, as well as assessment of effects on the respiratory system and immune function.
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| References | |
| Additional Infomation |
Structure in the first source
GW 833972A is a potent, selective CB2 receptor agonist with pEC50 values of 7.3 (human CB2) and 7.5 (rat CB2), showing 1000-fold selectivity over CB1. It inhibits induced neuronal depolarization and citric acid-induced cough in animal models. The compound also binds to BMAL2 with high affinity and facilitates its protein degradation. GW 833972A is used in research to study respiratory conditions, cough, and CB2 receptor function. It is available for research purposes only. |
| Molecular Formula |
C18H14CL2F3N5O
|
|---|---|
| Molecular Weight |
444.24
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| Exact Mass |
443.053
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| CAS # |
1092502-33-4
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| PubChem CID |
71312007
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| Appearance |
White to off-white solid powder
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| LogP |
5.667
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
29
|
| Complexity |
518
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1=CC=CC(=C1)NC1=NC=C(C(NCC2C=CN=CC=2)=O)C(C(F)(F)F)=N1.Cl
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| InChi Key |
UBHSVFAUAKIVKL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H13ClF3N5O.ClH/c19-12-2-1-3-13(8-12)26-17-25-10-14(15(27-17)18(20,21)22)16(28)24-9-11-4-6-23-7-5-11;/h1-8,10H,9H2,(H,24,28)(H,25,26,27);1H
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| Chemical Name |
2-(3-chloroanilino)-N-(pyridin-4-ylmethyl)-4-(trifluoromethyl)pyrimidine-5-carboxamide;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2510 mL | 11.2552 mL | 22.5104 mL | |
| 5 mM | 0.4502 mL | 2.2510 mL | 4.5021 mL | |
| 10 mM | 0.2251 mL | 1.1255 mL | 2.2510 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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