AM251 - Moligand™, 10mM in DMSO , Antagonist of CB 1 receptor;Agonist of GPR18;Agonist of GPR55, CAS No.183232-66-8, Antagonist of CB 1 receptor;Agonist of GPR18;Agonist of GPR55

CAS: 183232-66-8 Cat. No.: A409175 분자식: C₂₂H₂₁Cl₂IN₄O 분자량: 555.24 EC 번호: 634-045-8

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

1H-Pyrazole-3-carboxamide, 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

Information

AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.
In vitro

AM251 reduces veratridine-dependent (tetrodotoxin suppressible) release of L-glutamic acid and GABA from synaptosomes with IC50 of 8.5 μM and 9.2 μM, respectively. AM251 increases (by 2.3 times) the K_d of radioligand without altering B_max. AM251 inhibits equilibrium binding by allosterically accelerating the dissociation of the [³H]-batrachotoxinin A 20-alpha-benzoate:sodium channel complex. AM251 reduces cholesteryl ester synthesis in unstimulated and acetylated LDL-stimulated Raw 264.7 macrophages, CB2^+/+ and CB2 ^−/− peritoneal macrophages.

In vivo

AM251 causes a sustained reduction of daily food intake in the rat. AM251 produces food avoidance and behaviors associated with nausea but does not impair feeding efficiency in rats. AM251 disrupts memory consolidation of the inhibitory avoidance task. AM251 has caused a significative decrease in the test step-down latency when compared to the control group, but no differences are detected in the open field habituation task, including the number of crossings, i.e. there are no motor effects. AM251 (4.0 mg/kg) reduces freezing during a conditioned tone cue played within a novel context.
Cell Data

cell lines：3T3-SA cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

동의어

1H-Pyrazole-3-carboxamide, 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-

사양 및 순도

Moligand™, 10mM in DMSO

생화학 및 생리적 메커니즘

AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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등급

Moligand™

작업 유형

AGONIST, ANTAGONIST

작동 메커니즘

Antagonist of CB 1 receptor;Agonist of GPR18;Agonist of GPR55

이름과 식별자

• 이성체 SMILES: CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)I
• WGK 독일: 3
• 분자량: 555.24
• Reaxy-Rn: 7780333
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7780333&ln=

관련 대상(인간)

CNR1 Tclin Cannabinoid receptor 1 (17 Activities)

Discover Target: CNR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GPR18 Tchem N-arachidonyl glycine receptor (1 Activities)

Discover Target: GPR18

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

화학 및 물리적 특성

• 용해성: Solubility (25°C) In vitro DMSO: 70 mg/mL (199.74 mM); Ethanol: 14 mg/mL (39.94 mM); Water: Insoluble
• 녹는점(°C): 196-198°C