URB602
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $420 | Check With Us |
| 500mg | $630 | Check With Us |
| 1g | $945 | Check With Us |
: Cat #: V3273 CAS #: 565460-15-3 Purity ≥ 98%
Description: URB602 is a selective inhibitor of the monoacylglycerol lipase (MGL) which inhibits rat brain MGL enzyme with IC50 of 28±4 μM via a noncompetitive mechanism. MGL is a serine hydrolase involved in the biological deactivation of the endocannabinoid 2-arachidonoyl-sn-glycerol (2-AG). Pretreatment with URB602 protects from the long-term consequences of neonatal hypoxic-ischemic brain injury in rats. URB602 inhibits monoacylglycerol lipase and selectively blocks 2-arachidonoylglycerol degradation in intact brain slices. RB602 (100 microM) elevates 2-AG levels in hippocampal slice cultures without affecting levels of other endocannabinoid-related substances. Thus, URB602 may provide a useful tool by which to investigate the physiological roles of 2-AG and explore the potential interest of MGL as a therapeutic target.
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| Molecular Weight (MW) | 295.38 |
|---|---|
| Molecular Formula | C19H21NO2 |
| CAS No. | 565460-15-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: ≥ 30 mg/mLr |
| Water: N/Ar | |
| Ethanol: N/A | |
| SMILES Code | O=C(OC1CCCCC1)NC2=CC(C3=CC=CC=C3)=CC=C2 |
| Synonyms | URB602, URB-602, URB 602 |
| Protocol | In Vitro | In vitro activity: URB602 is a selective inhibitor of the monoacylglycerol lipase (MGL) which inhibits rat brain MGL enzyme with IC50 of 28±4 μM via a noncompetitive mechanism. MGL is a serine hydrolase involved in the biological deactivation of the endocannabinoid 2-arachidonoyl-sn-glycerol (2-AG). Pretreatment with URB602 protects from the long-term consequences of neonatal hypoxic-ischemic brain injury in rats. URB602 inhibits monoacylglycerol lipase and selectively blocks 2-arachidonoylglycerol degradation in intact brain slices. RB602 (100 microM) elevates 2-AG levels in hippocampal slice cultures without affecting levels of other endocannabinoid-related substances. Thus, URB602 may provide a useful tool by which to investigate the physiological roles of 2-AG and explore the potential interest of MGL as a therapeutic target. Without URB602, the apparent Michaelis constant (Km) of MGL for 2-AG is 24±1.7 μM and the maximum velocity (Vmax) is 1814±51 nmol min per mg protein; with URB602, the Km is 20±0.4 μM and the Vmax is 541±20 nmol min per 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. URB602 is an inhibitor of monoacylglycerol lipase (MGL), a serine hydrolase involved in the biological deactivation of the endocannabinoid 2-arachidonoyl-sn-glycerol (2-AG). URB602 weakly inhibits recombinant MGL (IC50=223±63 μM) through a rapid and 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). Cell Assay: RB602 (100 microM) elevates 2-AG levels in hippocampal slice cultures without affecting levels of other endocannabinoid-related substances. |
|---|---|---|
| In Vivo | URB602 (20 and 40 mg/kg) is able to reduce upper GI transit and slow colonic propulsion. When taken together as whole gut transit, URB602 dose dependently inhibits transit (P<0.05) compared with the vehicle control group. The inhibitory action of 40 mg/kg URB602 on whole gut transit is absent in these mice, indicating CB1 receptor involvement in the inhibitory action. URB602 decreases the AUC of pain behaviour during the early phase of the formalin test with an ED50 of 0.06±0.028 μg for JZL184 and 120±51.3 μg for URB602 in adult male Sprague-Dawley rats. Both MGL inhibitors also suppresses pain behaviour during the late phase of formalin pain, with an ED50 of 0.03±0.011 μg for JZL184 and 66±23.9 μg for URB602. | |
| Animal model | Male C57BL/6 mice (5-6 wk; 20-26 g) or female CB1-/- mice (8 wk; 18-22 g) | |
| Formulation | Dissolved in 10% DMSO/Tween 80 in saline | |
| Dosages | 20 and 40 mg/kg | |
| Administration | i.p. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 3.3855 mL | 16.9273 mL | 33.8547 mL | 67.7094 mL |
| 5mM | 0.6771 mL | 3.3855 mL | 6.7709 mL | 13.5419 mL |
| 10mM | 0.3385 mL | 1.6927 mL | 3.3855 mL | 6.7709 mL |
| 20mM | 0.1693 mL | 0.8464 mL | 1.6927 mL | 3.3855 mL |
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Step Two: Enter the in vivo formulation
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
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PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
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ddH2O,mix and clarify.
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