AZ12216052
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 531498

CAS#: 1290628-31-7

Description: AZ12216052 is a mGluR II and III activator. AZ12216052 potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM). AZ12216052 reduced measures of anxiety in wild-type mice. AZ12216052 also reduced measures of anxiety in the elevated zero maze and the acoustic startle response in mGluR8(-/-) mice.

Chemical Structure

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AZ12216052
CAS# 1290628-31-7
Instruction

Theoretical Analysis

MedKoo Cat#: 531498
Name: AZ12216052
CAS#: 1290628-31-7
Chemical Formula: C19H22BrNOS
Exact Mass: 391.06
Molecular Weight: 392.355
Elemental Analysis: C, 58.16; H, 5.65; Br, 20.37; N, 3.57; O, 4.08; S, 8.17

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 Weeks
100mg USD 750 2 Weeks
200mg USD 1250 2 Weeks
500mg USD 2650 2 Weeks
1g USD 3950 2 Weeks
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Synonym: AZ 12216052; AZ-12216052; AZ12216052

IUPAC/Chemical Name: 2-{[(4-bromophenyl)methyl]sulfanyl}-N-[4-(butan-2-yl)phenyl]acetamide

InChi Key: QKUYZJOTWYRWNF-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H22BrNOS/c1-3-14(2)16-6-10-18(11-7-16)21-19(22)13-23-12-15-4-8-17(20)9-5-15/h4-11,14H,3,12-13H2,1-2H3,(H,21,22)

SMILES Code: O=C(NC1=CC=C(C(CC)C)C=C1)CSCC2=CC=C(Br)C=C2

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 392.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Jantas D, Greda A, Leskiewicz M, Grygier B, Pilc A, Lason W. Neuroprotective effects of mGluR II and III activators against staurosporine- and doxorubicin-induced cellular injury in SH-SY5Y cells: New evidence for a mechanism involving inhibition of AIF translocation. Neurochem Int. 2015 Sep;88:124-37. doi: 10.1016/j.neuint.2014.12.011. PubMed PMID: 25661514.

2: Jantas D, Greda A, Golda S, Korostynski M, Grygier B, Roman A, Pilc A, Lason W. Neuroprotective effects of metabotropic glutamate receptor group II and III activators against MPP(+)-induced cell death in human neuroblastoma SH-SY5Y cells: the impact of cell differentiation state. Neuropharmacology. 2014 Aug;83:36-53. doi: 10.1016/j.neuropharm.2014.03.019. PubMed PMID: 24713472.

3: Rossi F, Marabese I, De Chiaro M, Boccella S, Luongo L, Guida F, De Gregorio D, Giordano C, de Novellis V, Palazzo E, Maione S. Dorsal striatum metabotropic glutamate receptor 8 affects nocifensive responses and rostral ventromedial medulla cell activity in neuropathic pain conditions. J Neurophysiol. 2014 Jun 1;111(11):2196-209. doi: 10.1152/jn.00212.2013. PubMed PMID: 24304862.

4: Reed BT, Morgans CW, Duvoisin RM. Differential modulation of retinal ganglion cell light responses by orthosteric and allosteric metabotropic glutamate receptor 8 compounds. Neuropharmacology. 2013 Apr;67:88-94. doi: 10.1016/j.neuropharm.2012.09.023. PubMed PMID: 23164615; PubMed Central PMCID: PMC3562428.

5: Duvoisin RM, Villasana L, Davis MJ, Winder DG, Raber J. Opposing roles of mGluR8 in measures of anxiety involving non-social and social challenges. Behav Brain Res. 2011 Aug 1;221(1):50-4. doi: 10.1016/j.bbr.2011.02.049. PubMed PMID: 21382421; PubMed Central PMCID: PMC3079808.

6: Duvoisin RM, Pfankuch T, Wilson JM, Grabell J, Chhajlani V, Brown DG, Johnson E, Raber J. Acute pharmacological modulation of mGluR8 reduces measures of anxiety. Behav Brain Res. 2010 Oct 15;212(2):168-73. doi: 10.1016/j.bbr.2010.04.006. PubMed PMID: 20385173; PubMed Central PMCID: PMC2892883.