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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
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Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Chemical Structure| 1101854-58-3 Chemical Structure| 1101854-58-3

Structure of JZL184
CAS No.: 1101854-58-3

Chemical Structure| 1101854-58-3

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JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively.

4.5 *For Research Use Only !

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Product Details of JZL184

CAS No. :1101854-58-3
Formula : C27H24N2O9
M.W : 520.49
SMILES Code : O=C(N1CCC(C(C2=CC=C(OCO3)C3=C2)(C4=CC=C(OCO5)C5=C4)O)CC1)OC6=CC=C([N+]([O-])=O)C=C6
MDL No. :MFCD11976911
InChI Key :SEGYOKHGGFKMCX-UHFFFAOYSA-N
Pubchem ID :25021165

Safety of JZL184

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P301+P310
Class:6.1
UN#:2811
Packing Group:

Isoform Comparison

Biological Activity

Target
  • Lipase

    MAGL, IC50:8 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
GSC 528 cells 1 μM 24 hours JZL184 significantly reduced the self-renewal capacity of GSC 528 cells. PMC7293269
GSC X01 cells 1 μM 24 hours JZL184 significantly reduced the self-renewal capacity of GSC X01 cells. PMC7293269
Caco-2 cells 5 µM 6 hours Silencing MGL in Caco-2 cells resulted in up-regulation of PPAR-α and PPAR-γ, and down-regulation of inflaμMatory markers Tnfα and Cox2. PMC7317927
mouse brain membrane proteomes 50 nM 30 minutes Near-complete blockade of MAGL activity PMC2605181

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice Parkinsonism model oral 2 mg kg−1 once a week for 2 months JZL184 prevented MPTP-induced dopaminergic neuronal loss in the substantia nigra and significantly attenuated dopamine reductions PMC3249428
Mice CaMKII αT286A/T286A mouse model Intraperitoneal injection 40 mg/kg Once daily for 3 days JZL-184 significantly depressed motor activity in CaMKII αT286A/T286A mice but not in WT littermates. PMC3636998
mice hepatic ischemia/reperfusion injury model intraperitoneal injection 10-80 mg Once daily, during chemotherapy JZL184 significantly attenuated hepatic ischemia/reperfusion injury by enhancing endocannabinoid signaling and reducing eicosanoid production. PMC3608818
Mice MAGL knockout mice Intraperitoneal injection 40 mg/kg once, 1 hour before ischemia To investigate the long-term effects of JZL184 on the endocannabinoid system in mice, the results showed that JZL184 led to a loss of analgesic activity and produced cross-tolerance to cannabinoid receptor agonists. PMC2928870
Nude mice GSC X01 xenograft model Oral 50 μg Betulinic acid + 3 μg BMP2 single administration, lasting 4 weeks JZL184 significantly reduced tumor mass and suppressed TAM infiltration. PMC7293269
Mice Stress susceptibility model Systemic administration 20 mg/kg Once daily for 3 days JZL184 significantly reduced stress-induced anxiety-like behavior by enhancing 2-AG signaling and promoted resilience after stress. PMC5379055
Mice Shank3B–/– mouse model Intraperitoneal injection PLX5622-formulated AIN-76A diet 14 days JZL184 pretreatment prevented the blue light delivery–dependent suppression of sociability in the 3-chamber SI test in ChR2-expressing animals but did not affect SI in YFP-expressing controls. PMC7108917
Mice Mdr2−/− mouse model Dietary administration 100 mg/kg Daily for 5 to 9 months JZL184, by inhibiting MGL activity, ameliorated biliary fibrosis and inflammation in Mdr2?/? mice, reduced serum ALT and AP levels, and decreased the expression of liver fibrosis markers. PMC7317927
mice intraperitoneal injection 2 mg/kg/day TVB-3166, 100 mg/kg/day ABT-263 or ABT-199 Once daily for 42 days JZL184 significantly elevated brain 2-AG levels and induced CB1-dependent behavioral effects PMC2605181
Mice Conditioned place preference (CPP) and self-administration models Intraperitoneal injection 3 mg/kg and 10 mg/kg Once daily for 57 days JZL184 significantly attenuates the rewarding effects of opioids without affecting their analgesic properties PMC11606496

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.92mL

0.38mL

0.19mL

9.61mL

1.92mL

0.96mL

19.21mL

3.84mL

1.92mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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