| Company Name: |
BOC Sciences |
| Tel: |
16314854226; +8616314854226 |
| Email: |
inquiry@bocsci.com |
AZ 12216052 manufacturers
- AZ12216052
-
- $31.00
-
2026-04-22
- CAS:1290628-31-7
- Purity: 99.78%
- Supply Ability: 10g
|
| | AZ 12216052 Basic information |
| Product Name: | AZ 12216052 | | Synonyms: | AZ 12216052;2-[[(4-Bromophenyl)methyl]thio]-N-[4-(1-methylpropyl)phenyl]acetamide;AZ12216052 >=98% (HPLC);Acetamide, 2-[[(4-bromophenyl)methyl]thio]-N-[4-(1-methylpropyl)phenyl]-;2-((4-Bromobenzyl)thio)-N-(4-(sec-butyl)phenyl)acetamide | | CAS: | 1290628-31-7 | | MF: | C19H22BrNOS | | MW: | 392.35308 | | EINECS: | | | Product Categories: | | | Mol File: | 1290628-31-7.mol |  |
| | AZ 12216052 Chemical Properties |
| Boiling point | 526.9±45.0 °C(Predicted) | | density | 1.323±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: soluble | | form | A crystalline solid | | pka | 13.70±0.70(Predicted) | | color | White to off-white |
| | AZ 12216052 Usage And Synthesis |
| Description | AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8). It potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM). In a cell-based model of Parkinson’s disease, AZ 12216052 inhibits MPP+-induced decreases in the viability of undifferentiated SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM. AZ 12216052 (10 mg/kg) increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response in mice, indicating anxiolytic-like activity in response to avoidable and unavoidable anxiogenic stimuli, respectively. | | Uses | AZ 12216052 is a positive allosteric modulator of mGluR8, which are attractive therapeutic targets for anxiety disorders. | | in vivo | AZ 12216052 (10 mg/kg; i.p.; 2 h prior to testing) reduces measures of anxiety, without affecting the velocity of the mice[3].
AZ12216052 (10 mg/kg; i.p.; single dose) exhibits remaining anxiolytic effects, might involve mGluR4 in mGluR8 / mice, as the mGluR4 PAM (Positive Allosteric Modulator) VU 0155041 also reduces measures of anxiety in wild-type mice[4]. | Animal Model: | WT and Apolipoprotein E-deficient (Apoe/) mice (C57BL/6J, 2-month-old) in the elevated zero maze[3] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection; singel dose, 2 h prior to testing | | Result: | Reduced measures of anxiety in the elevated zero maze without affecting the velocity of the mice.
Reduced the acoustic startle response. |
| | IC 50 | mGlu8 | | References | [1] ROBERT M. DUVOISIN . Acute pharmacological modulation of mGluR8 reduces measures of anxiety[J]. Behavioural Brain Research, 2010, 212 2: Pages 168-173. DOI: 10.1016/j.bbr.2010.04.006
[2] D. JANTAS . 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[J]. Neuropharmacology, 2014, 83: Pages 36-53. DOI: 10.1016/j.neuropharm.2014.03.019 |
| | AZ 12216052 Preparation Products And Raw materials |
|