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CB1/2 agonist 1

Catalog No.GC71002

CB1/2 agonist 1는 CB1R과 CB2R에 각각 56.15, 11.63 nM의 EC50s를 가진 강력하고 교차 혈액 뇌 장벽 CB1/2 agonist이다.

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CB1/2 agonist 1 Chemical Structure

Cas No.: 2986688-90-6

Size 가격 재고 수량
5 mg
US$90.00
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10 mg
US$144.00
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25 mg
US$315.00
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50 mg
US$495.00
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100 mg
US$855.00
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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents
CB1/2 agonist 1 is a potent and cross the blood-brain barrier CB1/2 agonist with EC50s of 56.15, 11.63 nM for CB1R and CB2R, respectively. CB1/2 agonist 1 reduces glutamate release and LPS-induced activation of microglial cells. CB1/2 agonist 1 shows anti-inflammatory and antinociceptive effects. CB1/2 agonist 1 has the potential for the research of multiple sclerosis.

CB1/2 agonist 1 (compound B2) (10 µM) inhibits AEA hydrolysis with an IC50 of 5.9 µM for FAAH[1].
CB1/2 agonist 1 shows high affinity for CB1R and CB2R with Kis of 2.9, 1.5 nM, respectively[1].
CB1/2 agonist 1 (10 µM) shows anti-inflammatory effect and significantly decreases the secretion of IL-1β and IL-6, increases the release of anti-inflammatory IL-10 to 483.7% in LPS-activated BV-2 cells[1].
CB1/2 agonist 1 (1, 10 µM) inhibits 4-AP-evoked glutamate release[1].

CB1/2 agonist 1 (5-50 mg/kg) dose-dependently relieves neuropathic pain in a mouse model of oxaliplatin-induced neuropathic pain[1].

References:
[1]. Arena C, et al. The endocannabinoid system dual-target ligand N-cycloheptyl-1,2-dihydro-5-bromo-1-(4-fluorobenzyl)-6-methyl-2-oxo-pyridine-3-carboxamide improves disease severity in a mouse model of multiple sclerosis. Eur J Med Chem. 2020 Dec 15;208:112858.

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