ChemicalBook CAS DataBase List 1245626-05-4

1245626-05-4

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
Molecular Formula	C26H23Cl2N5O3S
MDL Number	MFCD19053178
Molecular Weight	556.46
MOL File	1245626-05-4.mol

Chemical Properties

storage temp.	2-8°C
solubility	DMSO: >25mg/mL
form	powder
color	white to off-white
InChIKey	XBHQLFVDGLPBCK-UHFFFAOYSA-N
SMILES	Cc1c(nn(-c2ccc(Cl)cc2Cl)c1-c3ccc(cc3)C#CCCC#N)C(=O)NN4CCS(=O)(=O)CC4

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H319
Precautionary statements	P305+P351+P338
Hazard Codes	Xi
Risk Statements	36 less more
Safety Statements	26 less more
WGK Germany	3
Storage Class	11 - Combustible Solids
Hazard Classifications	Eye Irrit. 2

Hazard Information

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

Spectrum Detail

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