Product Details
| Product Name:
URB602 |
CAS No.:
565460-15-3 |
| Purity:
99.90% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | URB602 |
| Description | URB602 is a specific monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL (IC50: 28±4 μM) through a noncompetitive mechanism. |
| Kinase Assay | Samples containing either URB602 (300 μM), MGL (1.4 pM), or both URB602 and MGL are incubated at 37°C for 30 min in assay buffer. At various time points, the reaction is stopped with an equal volume of ice-cold methanol and directly analyzed in positive ionization mode by LC/MS. A SB-CN column (150×2.1 mm i.d., 5 μm) eluted is used with a linear gradient of methanol in water containing 0.25% acetic acid and 5 mM ammonium acetate (from 60% to 100% of methanol in 8 min) at a flow rate of 0.5 mL/min with column temperature at 50°C. Capillary voltage is set at 4 kV and fragmentor voltage is 100V. Nebulizer pressure is set at 60 psi. N2 is used as drying gas at a flow rate of 13 liters/min and a temperature of 350°C. ESI is in the positive mode and a full scan spectrum is acquired from m/z 100 to 600. Extracted ion chromatograms are used to quantify URB602 ([M+H]+, m/z 296)[2]. |
| In vitro | The apparent Km of MGL for 2-AG is 24±1.7 μM and the Vmax is 1814±51 nmol/min/mg protein; with URB602, the Km is 20±0.4 μM and the Vmax is 541±20 nmol/min/mg protein (n=4). When organotypic slice cultures of rat forebrain are incubated with URB602 (100 μM), both baseline and Ca2+-ionophore-stimulated 2-arachidonoylglycerol (2-AG) concentrations are increased[1]. URB602 weakly inhibits recombinant MGL (IC50: 223±63 μM) through a rapid and noncompetitive mechanism. |
| In vivo | URB602 (20-40 mg/kg) can reduce upper GI transit and slow colonic propulsion. In whole gut transit, URB602 dose-dependently inhibits transit (P<0.05) compared with the vehicle control group. The inhibitory action of URB602 (40 mg/kg) on whole gut transit is absent in these mice, demonstrating CB1 receptor involvement in the inhibitory action[3]. During the early phase of the formalin test, URB602 decreases the AUC of pain behavior for JZL184 (ED50: 0.06±0.028 μg) and for URB602 (ED50: 120±51.3 μg) in adult male Sprague-Dawley rats. Both MGL inhibitors also suppress pain behavior during the late phase of formalin pain for JZL184 (ED50: 0.03±0.011 μg) and for URB602 (ED50: 66±23.9 μg). |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (186.2 mM)
|
| Keywords | URB 602 | Bacterial | URB-602 | inhibit | URB602 | Inhibitor |
| Inhibitors Related | Neomycin sulfate | Dehydroacetic acid sodium | Ampicillin sodium | Methyl anthranilate | Doxycycline (hyclate) | Kanamycin sulfate | G-418 disulfate | Sulfamethoxazole sodium | Metronidazole | Doxycycline | Dimethyl sulfoxide | Crystal Violet |
| Related Compound Libraries | Bioactive Compound Library | Anti-Obesity Compound Library | Inhibitor Library | Anti-Bacterial Compound Library | NO PAINS Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Bioactive Lipid Compound Library | Anti-Metabolism Disease Compound Library | Anti-Infection Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
You may like
-
CAS:1074-59-5
$30.00 / 25mg
-
CAS:56839-43-1
$39.00 / 25mg
-
CAS:22252-43-3
$52.00 / 10g
Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$9.80/1.8KG |
VIP6Y
|
Career Henan Chemical Co
|
2020-01-11 |
United States