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AM281 (CAS 202463-68-1) LS-H10

CB1 receptor antagonist
LS-H10-1 / 1 mg / $175
LS-H10-5 / 5 mg / $205
LS-H10-10 / 10 mg / $245
USA Shipment Only
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Description: AM281 is a potent and selective central cannabinoid (CB1) receptor antagonist/inverse agonist (Ki =12 nM and 4,200 nM for CB1 and CB2, respectively). Structurally, it is an analog of the CB1 inverse agonist rimonabant . It has no effect on the vanilloid TRPV1 receptor. AM281 has been used to evaluate the potential effects of compounds at CB1. It has also been used to study the membrane localization and cycling of CB1. H10_ChemicalStructureImage.png
1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl-1H-pyrazole-3-carboxamide
 
biochemical, chemical, antagonist
LS-H10
202463-68-1
C21H19Cl2IN4O2
≥98%
A crystalline solid
 
ClC1=CC(Cl)=CC=C1N2C(C3=CC=C(I)C=C3)=C(C)C(C(NN4CCOCC4)=O)=N2
InChI=1S/C21H19Cl2IN4O2/c1-13-19(21(29)26-27-8-10-30-11-9-27)25-28(18-7-4-15(22)12-17(18)23)20(13)14-2-5-16(24)6-3-14/h2-7,12H,8-11H2,1H3,(H,26,29)
AJFFBPZYXRNAIC-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: CNR1 / CB1 related products

Usage Information

AM281 is supplied as a crystalline solid. A stock solution may be made by dissolving the AM281 in the solvent of choice. AM281 is soluble in organic solvents such as DMSO and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of AM281 in these solvents is approximately 1 mg/ml. AM281 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, AM281 should first be dissolved in DMF and then diluted with the aqueous buffer of choice. AM281 has a solubility of approximately 0.2 mg/ml in a 1:5 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Lan, R., Lu, Q., Fan, P., et al. AAPS Pharmsci. 1(3), 1-7 (1999).
  2. Gatley, S.J., Lan, R., Pyatt, B., et al. Life Sci. 61(14), PL-191-PL-197 (1997).
  3. Jerman, J.C., Gray, J., Brough, S.J., et al. Br. J. Anaesth. 89(6), 882-887 (2002).
  4. Baker, C.L. and McDougall, J.J. Br. J. Pharmacol. 142, 1361-1367 (2004).
  5. Brown, I., Cascio, M.G., Wahle, K.W.J., et al. Carcinogenesis 31(9), 1584-1591 (2010).

 


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