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AM-251 (CAS 183232-66-8)

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Synonym: 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide

Application: An inverse agonist of the CB1 receptor

CAS Number: 183232-66-8

Purity: 98%

Molecular Weight: 555.24

Molecular Formula: C₂₂H₂₁Cl₂IN₄O

* Refer to Certificate of Analysis for lot specific data (including water content).

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AM-251 is a ¹²³I radioisotope and potent CB₁ receptor antagonist derivative of the CB₁ cannabinoid receptor inverse agonist SR141716A, presenting a radioprobe for in vivo binding studies at the CB₁ receptor with a higher affinity (K_i = 7.49 nM) for CB₁ than the parent compound (K_i = 11.5 nM). AM-251 has been employed in competitive binding studies to identify CB₁ affinity of different cannabimimetic agonists in vivo. Characterization of AM-251-CB₁ association with SPECT (single photon emission computed tomography) has been described. AM-251 is also a potent activator of the GPR55 receptor.

References

1. Gatley, S.J., et al. 1997. Life Sci. 61: PL 191-PL 197. PMID: 9335234
2. Lan, R., et al. 1999. J. Med. Chem. 42: 769-776. PMID: 10052983
3. McLaughlin, P.J., et al. 2003. Behav Pharmacol. 14: 583-588. PMID: 14665975
4. Fong, T.M. and Heymsfield, S.B. 2009. Int J Obes. 33: 947-955. PMID: 19597516

Physical State :

Solid

Solubility :

Soluble in DMSO (~10 mg/ml), ethanol (~10 mg/ml), DMF (~10 mg/ml), and 1:3 DMSO:PBS (pH 7.2) (~14 mg/ml). Insoluble in water.

Storage :

Store at room temperature

Melting Point :

196-198° C

Density :

~1.7 g/cm³ (Predicted)

Refractive Index :

n²⁰_D 1.70 (Predicted)

IC50 :

Cannabinoid CB1 receptor: IC₅₀ = 0.32 nM (human); [3H]SR-141716: IC₅₀ = 0.59 nM (human CBR1 S383A mutant expressed in CHO cells); GPR55: EC₅₀50 = 39 nM

Ki Data :

CB1 receptor: K_i= 7.5 nM

pK Values :

pK_a: 11.31 (Predicted), pK_b: 3.22 (Predicted)

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

WGK Germany :

PubChem CID :

2125

MDL Number :

MFCD01861181

SMILES :

CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)I

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AM-251 Product Citations

See how others have used AM-251. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 30620895 Askari, VR.|Shafiee-Nick, R.| et al. 2019. Life Sci. 219: 40-73.

PMID: # 23315130 Pai, WY. et al. 2013. Transgenic Res. 22: 823-38.

PMID: # 23251393 Chen, SW. et al. 2012. PLoS ONE. 7: e50850.

Citations 1 to 3 of 3 total

Rated 5 out of 5 by KG from McLaughlin et al McLaughlin et al. (PubMed ID 14665975) found that CB1 antagonist AM-251 suppressed appetite in rats. -SCBT Publication Review

Date published: 2015-07-04

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AM-251 (CAS 183232-66-8)

QUICK LINKS

References

Download SDS (MSDS)

Certificate of Analysis

AM-251 Product Citations

AM-251 (CAS 183232-66-8)

QUICK LINKS

References

Download SDS (MSDS)

Certificate of Analysis

AM-251 Product Citations

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