DC Chemicals Limited
China
Product Name: AM 281
Price: $625.0/100mg $1250.0/250mg $2500.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: AM 281
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

202463-68-1

202463-68-1 structure

202463-68-1 structure

Name: AM281
Chemical Name: 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-morpholin-4-ylpyrazole-3-carboxamide
CAS Number: 202463-68-1
Molecular Formula: C₂₁H₁₉Cl₂IN₄O₂
Molecular Weight: 557.212
Catalog: Signaling Pathways GPCR/G Protein Cannabinoid Receptor
Create Date: 2018-12-28 17:22:00
Modify Date: 2024-01-11 19:37:18
AM281 is a selective CB1 receptor antagonist with an IC50 of 9.91 nM. AM281 inhibits CB2 receptor with an IC50 of 13000 nM[1].

Name	1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-morpholin-4-ylpyrazole-3-carboxamide
Synonyms	AM 281 1H-Pyrazole-3-carboxamide, 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl- Tocris-1115 S1595_Selleck 1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(morpholin-4-yl)-1H-pyrazole-3-carboxamide MFCD01861180 1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(4-morpholinyl)-1H-pyrazole-3-carboxamide

Description	AM281 is a selective CB1 receptor antagonist with an IC50 of 9.91 nM. AM281 inhibits CB2 receptor with an IC50 of 13000 nM[1].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor
Target	CB1:9.91 nM (IC50) CB2:13000 nM (IC50)
In Vitro	AM281 (0.01-10 μM) promotes a concentration dependent increase in 10 μM Aβ 25-35 induced neurotoxicity in SH-SY5Y cells in the presence of 10 μM KSO 1-6[2].
In Vivo	Acute administration (2.5, 5 and 10 mg/kg) of AM281 shortens exploration time and improves memory performance, as does chronic administration (0.62, 1.25 and 2.5 mg/kg) of AM281[3]. Chronic administration of AM281 at 2.5 mg/kg improves recognition index to the 22.1±4.8 and single dose of AM281 at 5 mg/kg improves the memory impairment to the 8.5±4, as compared with vehicle-treated which is 4.8±2.5. Administration of AM281 at a dose of 2.5 mg/kg in chronic form and 5 mg/kg in acute dose improve memory[3]. Animal Model: Male NMRI mice with the weight of 25-30 g[3] Dosage: 0.62, 1.25 and 2.5 mg/kg (chronic administration); 2.5, 5 and 10 mg/kg (acute administration) Administration: Administrated i.p. every day concurrently with morphine except the day of experiment (chronic administration); Singly injected 40 min before second trial (acute administration) Result: The simultaneous daily administration of AM281 with morphine significantly shortened the exploration time, as compared with morphine-dependent mice receiving vehicle. Acute administration at a dose of 5 mg/kg, significantly augmented recognition index.
References	[1]. K S S Dossou, et al. Development and preliminary validation of a plate-based CB1/CB2 receptor functional assay. Anal Biochem. 2013 Jun 15;437(2):138-43. [2]. Milton, NG, et al. Effects of the CB1 cannabinoid receptor antagonist AM281 on kissorphin protection against amyloid-β neurotoxicity. [3]. G Vaseghi, et al. The effect of AM281, a cannabinoid antagonist, on memory performance during spontaneous morphine withdrawal in mice. Res Pharm Sci. 2013 Jan;8(1):59-64.

Density	1.7±0.1 g/cm3
Molecular Formula	C₂₁H₁₉Cl₂IN₄O₂
Molecular Weight	557.212
Exact Mass	555.992981
PSA	59.39000
LogP	4.90
Index of Refraction	1.706
Storage condition	2-8C

Symbol	GHS06
Signal Word	Danger
Hazard Statements	H300-H315-H319-H335
Precautionary Statements	P261-P264-P301 + P310-P305 + P351 + P338
Personal Protective Equipment	Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges
Hazard Codes	T: Toxic;
Risk Phrases	R25
Safety Phrases	26-36/37/39-45
RIDADR	UN 2811 6