5-(4-[4-cyanobut-1-ynyl]phenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1,1-dioxo-thiomorpholino)-1H-pyrazole-3-carboxamide
- Product Name
- 5-(4-[4-cyanobut-1-ynyl]phenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1,1-dioxo-thiomorpholino)-1H-pyrazole-3-carboxamide
- CAS No.
- 1245626-05-4
- Chemical Name
- 5-(4-[4-cyanobut-1-ynyl]phenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1,1-dioxo-thiomorpholino)-1H-pyrazole-3-carboxamide
- 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-
- CBNumber
- CB52750957
- Molecular Formula
- C26H23Cl2N5O3S
- Formula Weight
- 556.46
- MOL File
- 1245626-05-4.mol
5-(4-[4-cyanobut-1-ynyl]phenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1,1-dioxo-thiomorpholino)-1H-pyrazole-3-carboxamide Property
- storage temp.
- 2-8°C
- solubility
- DMSO: >25mg/mL
- form
- powder
- color
- white to off-white
N-Bromosuccinimide Price
- Product number
- A1987
- Product name
- AM6545
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $276
- Updated
- 2024/03/01
- Product number
- A1987
- Product name
- AM6545
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $878
- Updated
- 2024/03/01
- Product number
- 16316
- Product name
- AM6545
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 16316
- Product name
- AM6545
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $161
- Updated
- 2024/03/01
- Product number
- 16316
- Product name
- AM6545
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $235
- Updated
- 2024/03/01
5-(4-[4-cyanobut-1-ynyl]phenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1,1-dioxo-thiomorpholino)-1H-pyrazole-3-carboxamide Chemical Properties,Usage,Production
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 albuminuria, inflammation 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
5-(4-[4-cyanobut-1-ynyl]phenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1,1-dioxo-thiomorpholino)-1H-pyrazole-3-carboxamide Preparation Products And Raw materials
Raw materials
Preparation Products
5-(4-[4-cyanobut-1-ynyl]phenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1,1-dioxo-thiomorpholino)-1H-pyrazole-3-carboxamide Suppliers
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