Rimonabant , ≥98% , 168273-06-1
CAS NO.:168273-06-1
Empirical Formula: C22H21Cl3N4O
Molecular Weight: 463.79
MDL number: MFCD04034714
EINECS: 200-223-5
Pack Size | Price | Stock | Quantity |
50MG | RMB173.60 | In Stock |
|
10MG | RMB415.20 | In Stock |
|
100MG | RMB1935.20 | In Stock |
|
others | Enquire |
PRODUCT Properties
Melting point: | 154.7 °C |
Density | 1.41±0.1 g/cm3(Predicted) |
storage temp. | RT |
solubility | Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 20 mg/ml). |
pka | 11.31±0.20(Predicted) |
form | solid |
color | White |
Stability: | Stable for 1 year from date of purchase as supplied. Protect from moisture. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
Description and Uses
Rimonabant is a first-in-class drug launched as an oral treatment for obesity, and its mechanism of action involves the selective antagonism of cannabinoid type 1 (CB1) receptor. It is specifically indicated as an adjunct to diet and exercise for the treatment of obese patients (body mass index [BMI]≥30 kg/m2), or overweight patients (BMI>27 kg/m2) with associated risk factors such as type 2 diabetes or dyslipidemia. Additionally, rimonabant is currently under development as a treatment for nicotine dependence. The CB1 and CB2 receptors, along with their endogenous ligands, constitute the endocannabinoid system. The CB1 receptor is expressed in the brain, adipose tissue, and several peripheral organs; the CB2 receptor is predominantly expressed in immune cells. Activation of the CB1 receptor in the CNS is associated with appetite stimulation and the modulation of brain reward mechanism, whereas activation in the periphery favors metabolic processes that lead to hepatic lipogenesis and impaired glucose homeostasis. Rimonabant acts by selectively blocking the action of central and peripheral CB1 receptors, thereby reducing food intake and improving lipid and glucose metabolism.
Rimonabant is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane
Safety
Symbol(GHS) | GHS08,GHS09 |
Signal word | Danger |
Hazard statements | H410-H372 |
Precautionary statements | P260-P264-P270-P314-P501-P273-P391-P501 |