AM251 , ≥98% , 183232-66-8
Synonym(s):
1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide
CAS NO.：183232-66-8
Empirical Formula: C22H21Cl2IN4O
Molecular Weight: 555.24
MDL number: MFCD01861181
| Pack Size | Price | Stock | Quantity |
| 5MG | RMB351.20 | In Stock |
|
| 25MG | RMB1359.20 | In Stock |
|
| 100MG | RMB3839.20 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| Melting point: | 195-196℃ |
| Density | 1.65±0.1 g/cm3(Predicted) |
| storage temp. | Store at RT |
| solubility | DMSO: >10 mg/mL, soluble |
| pka | 11.31±0.20(Predicted) |
| form | solid |
| color | white |
| Stability: | Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| CAS DataBase Reference | 183232-66-8 |
Description and Uses
AM251 is a cannabinoid 1 (CB1) receptor 1 antagonist. It binds to CB1 receptors in rat forebrain membrane preparations (Ki = 7.5 nM) and is selective over CB2 receptors in mouse spleen preparations (Ki = 2,290 nM) in radioligand binding assays. AM251 inhibits GTPγS binding induced by the CB receptor agonist CP 55,940 in HEK293 cells expressing human CB1 receptors (EC50 = 8 nM). AM251 (10 mg/kg) decreases immobility time in the forced swim test in wild-type but not CB1 receptor-deficient mice. It reduces fasting-induced food intake and body weight gain in mice when administered at a dose of 30 mg/kg. AM251 also induces GTPγS binding in HEK293 cells expressing the orphan receptor GPR55 (EC50 = 39 nM) and potentiates GABA-induced GABAA receptor currents (EC50 = 0.4 μM). It prevents TGF-β1-induced epithelial-to-mesenchymal transition (EMT), inhibits SMAD2/3 and p38 MAPK activation, and reduces the expression of EMT-related transcription factors in HK-2 renal tubule epithelial cells. AM251 induces cell cycle arrest at the G2/M phase and apoptosis in A375 human melanoma cells.
Inhibitor of CB1 receptors. AM 251is a biarylpyrazole compound which has been considered for many years as the prototypical cannabinoid (CB) receptor antagonist
Safety
| Symbol(GHS) |  GHS07 |
| Signal word | Warning |
| Hazard statements | H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
| Hazard Codes | Xi |
| Risk Statements | 36/37/38 |
| Safety Statements | 26-36 |
| WGK Germany | 3 |
| HS Code | 2933.39.6190 |
