| Identification | Back Directory | [Name]
5-(4-[4-cyanobut-1-ynyl]phenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1,1-dioxo-thiomorpholino)-1H-pyrazole-3-carboxamide | [CAS]
1245626-05-4 | [Synonyms]
AM6545
AM-6545,AM6545
5-(4-[4-cyanobut-1-ynyl]phenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1,1-dioxo-thiomorpholino)-1H-pyrazole-3-carboxamide
5-[4-(4-Cyano-1-butyn-1-yl)phenyl]-1-(2,4-dichlorophenyl)-N-(1,1-dioxido-4-thiomorpholinyl)-4-methyl-1H-pyrazole-3-carboxamide
1H-Pyrazole-3-carboxamide, 5-[4-(4-cyano-1-butyn-1-yl)phenyl]-1-(2,4-dichlorophenyl)-N-(1,1-dioxido-4-thiomorpholinyl)-4-methyl- | [Molecular Formula]
C26H23Cl2N5O3S | [MDL Number]
MFCD19053178 | [MOL File]
1245626-05-4.mol | [Molecular Weight]
556.46 |
| Hazard Information | Back Directory | [Uses]
AM 6545 is a novel CB1 antagonist which suppresses food intake and food-motivated behaviours. Potential for use as an appetite suppressant. | [Biological Activity]
AM6545 helps in decreasing the development of albuminuriainflammation and expression of markers of fibrosis. It also helps in the down-regulation of nephrin and podocin. It has the ability to repress the ingestion of food and food-reinforced behaviour.''AM6545 is a peripheral CB1 cannabinoid receptor antagonist and appetite suppressant. | [in vivo]
AM6545 (5-20 mg/kg; i.p.; once daily; 7 days or single dose) reduces food intake and sustaines body weight in Sprague Dawley rats at 10 and 20 mg/kg when treated chronically or acutely[1].
AM6545 (10 mg/kg; ip; single dose) treatment of C57BL/6 J mice specifically induces PKA signaling activation in adipose tissue and upregulated Akt-mTOR and ERK phosphorylation levels[2].
AM6545 (10 mg/kg; i.p.; once daily; 4 weeks) significantly improves renal function, inhibited proteinuria, uric acid excretion and renal fibrosis in a rat model of metabolic syndrome[3].
| Animal Model: | Sprague Dawley rats (male, 250-275 g; normal/high-fat diet models)[1] | | Dosage: | 5 mg/kg, 10 mg/kg, 20 mg/kg (4% DMSO, 1% Tween 80 in saline) | | Administration: | Intraperitoneal injection, daily for 7 days or single dose.
| | Result: | Reduced food intake (30% inhibition at 3 h) and body weight gain (days 4-7) at 10 mg/kg dose, without inducing conditioned taste avoidance or gaping. |
| Animal Model: | Metabolic syndrome rats (male, Wistar; high-fructose/high-salt diet-induced)[3] | | Dosage: | 10 mg/kg (0.5% carboxymethylcellulose) | | Administration: | Intraperitoneal injection, daily for 4 weeks | | Result: |
Reduced proteinuria (50%) and urinary uric acid (attenuated 10-fold increase), alleviated glomerular hypertrophy, tubular injury, and collagen deposition, and suppressed renal TGFβ1 expression. |
| Animal Model: | C57BL/6 mice (male, 18.5-21.0 g; normal diet)[2] | | Dosage: | 10 mg/kg (4% DMSO, 10% Tween 80, 80-95% saline) | | Administration: | Intraperitoneal injection, single.
| | Result: | Significantly modified p-PKA substrates in adipose and liver tissue, but the responsive substrates are tissue-specific and remain to be determined
Upregulated ERK1 phosphorylation at Thr202 in WAT, liver, TA.
Upregulated p-Akt(Ser473) and p-mTOR(Ser2448) in liver.
|
| [storage]
Store at +4°C |
|
| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
NewCan Biotech Limited
|
| Tel: |
+86-0571-86912261 +86-15658003402 |
| Website: |
https://www.newcanbio.com/ |
|