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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
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
Rimonabant demonstrates growth inhibition of Mtb with an MIC of 54 μM. MmpL3, an anti-TB target, is directly targeted by rimonabant[2]. Rimonabant itself (10-12-10-3 M, 12 concentrations) inhibits the basal binding of [35S]GTPgS to human cortical membranes in a concentration-dependent manner, with a -log IC50 of 4.7±0.2 (IC50 = 20 μM) and a maximal inhibition of 48±2%[3].
体内研究
Rimonabant (10 mg/kg by gavage) is administered for 2 weeks to 3-month-old male obese Zucker rats as an impaired glucose tolerance model and for 10 weeks to 6-month-old male obese Zucker rats as a model of the metabolic syndrome. RANTES and MCP-1 serum levels are increased in obese vs lean Zucker rats and significantly reduced by long-term treatment with Rimonabant, which slows weight gain in rats with the metabolic syndrome. Neutrophils and monocytes are significantly increased in young and old obese vs lean Zucker rats and lowered by Rimonabant. Platelet-bound fibrinogen is significantly enhanced in obese vs lean Zucker rats of both age, and is reduced by Rimonabant [1].
Rimonabant (20 mg daily) demonstrates a significant reduction in many cardiometabolic risk factors[4].
体外研究
Rimonabant demonstrates growth inhibition of Mtb with an MIC of 54 μM. MmpL3, an anti-TB target, is directly targeted by rimonabant[2].
Rimonabant itself (10-12-10-3 M, 12 concentrations) inhibits the basal binding of [35S]GTPgS to human cortical membranes in a concentration-dependent manner, with a -log IC50 of 4.7±0.2 (IC50 = 20 μM) and a maximal inhibition of 48±2%[3].
Rimonabant/利莫那班 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Primary myoblasts from DMD patients
1 µM
5 days
Promoted differentiation of myoblasts from DMD patients, increased expression of MYOG and TNNT-1
Nat Commun. 2018 Sep 27;9(1):3950.
Primary human satellite cells
1-3 µM
5 days
Promoted human satellite cell differentiation, increased expression of troponin-T-1 (TNNT1), myogenin (MYOG), and myosin heavy chain (MyHC)
Nat Commun. 2018 Sep 27;9(1):3950.
Rimonabant/利莫那班 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Chemotherapy-induced neuropathic pain model
Intraperitoneal injection
10 mg/kg
Once daily for 20 consecutive days
To assess whether Rimonabant precipitates signs of physical dependence after chronic dosing, results showed that Rimonabant precipitated signs of physical dependence in mice treated chronically with JZL184 or WIN55,212-2, but not in LEI-515-treated mice.
Nat Commun. 2023 Dec 5;14(1):8039
Mice
Diet-induced obesity (DIO) mouse model
Intraperitoneal injection
10 mg/kg
Once daily for 28 days
To evaluate the effects of Rimonabant on body weight and metabolic abnormalities in obese mice. Results showed that Rimonabant significantly reduced body weight and adiposity, improved glucose tolerance and insulin resistance, and reversed hepatic steatosis and plasma lipid profile abnormalities.
J Clin Invest. 2010 Aug;120(8):2953-66
Mdx mice
Duchenne muscular dystrophy model
Intraperitoneal injection
0.5 mg/kg
Three times per week for 2 weeks
Improved motor coordination and muscle strength in mdx mice, increased the number of regenerated myofibers, reduced inflammatory markers
Nat Commun. 2018 Sep 27;9(1):3950.
Mice
Obese mouse model
Intraperitoneal injection
1 mg/kg and 5 mg/kg
Single dose, observed for 5 minutes
Evaluate the blocking effect of Rimonabant on [11C]-OMAR uptake in the myocardium. Results showed that 5 mg/kg Rimonabant significantly blocked [11C]-OMAR uptake in the myocardium.
Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes, Ki=8.9 nM
10465552
CHO cells
Function assay
Antagonistic activity towards cannabinoid receptor 1 expressed as [3H]Arachidonic acid release in CHO cells, Kd=2.51 nM
14736243
CHOK1 cells
Function assay
Antagonist activity at human CB1 receptor expressed in CHOK1 cells by luciferase assay, IC50=0.12 μM
18243711
CHOK1 cells
Function assay
Antagonist activity at human CB1 receptor expressed in CHOK1 cells assessed as inhibition of CP-55940-induced response after 10 mins by GTPgamma[35S] binding assay, Ki=0.0016 μM
19351113
COS7 cells
Function assay
Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS7 cells, Ki=0.0051 μM
20015647
HEK cells
Function assay
Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.008 μM
18579386
HEK cells
Function assay
Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79 μM
18579386
HEK293 cells
Function assay
Immediate antagonist/Inverse agonist activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as reversal of 1 uM CP55,940-induced inhibition of 5 uM forskolin-induced cAMP accumulation by kinetic cAMP assay
26203658
HEK293 cells
Function assay
Displacement of [3H]CP-55940 from human recombinant CB2R expressed in HEK293 cells, IC50=1.6311 μM
19530697
N1E-115 cells
Function assay
Inverse agonist activity at CB1 receptor in mouse N1E-115 cells assessed as inhibition of WIN 55,212-2-induced ERK1/2 phosphorylation at 1 uM treated 5 mins prior to WIN 55,212-2 challenge by Western blot analysis
23357307
RD-HGA16 cells
Function assay
Antagonist activity at CB1 receptor (unknown origin) expressed in RD-HGA16 cells assessed as inhibition of CP55940-induced calcium mobilization by fluorometric imaging plate reader analysis
24944734
SF9 cells
Function assay
Inverse agonist at human CB1 receptor expressed in SF9 cells assessed as decrease in GTPgammaS level, IC50=1.35 nM
18448340
SF9 cells
Function assay
Antagonist activity at human CB2 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.815 μM
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