ADX71743 | CAS#1431641-29-0 | mGlu7 modulator

ADX71743
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 531407

CAS#: 1431641-29-0

Description: ADX71743 is a potent and selective negative allosteric modulator of metabotropic glutamate receptor 7. ADX71743 is a suitable compound to help unravel the physiologic role of mGlu(7) and to better understand its implication in central nervous system diseases. Few selective ligands are available for this receptor, and so ADX71743 has played an important role into scientific research into the role of this receptor in various processes such as memory formation, nociception, absence seizures and psychosis.

Chemical Structure

ADX71743

CAS# 1431641-29-0

Instruction

Theoretical Analysis

MedKoo Cat#: 531407
Name: ADX71743
CAS#: 1431641-29-0
Chemical Formula: C17H19NO2
Exact Mass: 269.14
Molecular Weight: 269.344
Elemental Analysis: C, 75.81; H, 7.11; N, 5.20; O, 11.88

Price and Availability

Size	Price	Availability
10mg	USD 550	2 Weeks
25mg	USD 1250	2 Weeks
50mg	USD 2250	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: ADX71743; ADX-71743; ADX 71743;

IUPAC/Chemical Name: 6-(2,4-dimethylphenyl)-2-ethyl-4,5,6,7-tetrahydro-1,3-benzoxazol-4-one

InChi Key: CPKZCQHJDFSOJT-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H19NO2/c1-4-16-18-17-14(19)8-12(9-15(17)20-16)13-6-5-10(2)7-11(13)3/h5-7,12H,4,8-9H2,1-3H3

SMILES Code: O=C1CC(C2=CC=C(C)C=C2C)CC3=C1N=C(CC)O3

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: Metabotropic glutamate receptor 7 (mGlu(7)) has been suggested to be a promising novel target for treatment of a range of disorders, including anxiety, post-traumatic stress disorder, depression, drug abuse, and schizophrenia.

Instruction:

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Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 269.34 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.

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: Lin X, Fisher NM, Dogra S, Senter RK, Reed CW, Kalbfleisch JJ, Lindsley CW, Asher WB, Xiang Z, Niswender CM, Javitch JA. Differential activity of mGlu7 allosteric modulators provides evidence for mGlu7/8 heterodimers at hippocampal Schaffer collateral-CA1 synapses. J Biol Chem. 2022 Oct;298(10):102458. doi: 10.1016/j.jbc.2022.102458. Epub 2022 Sep 5. PMID: 36063995; PMCID: PMC9531177.

2: Cieślik P, Woźniak M, Kaczorowska K, Brański P, Burnat G, Chocyk A, Bobula B, Gruca P, Litwa E, Pałucha-Poniewiera A, Wąsik A, Pilc A, Wierońska J. Negative Allosteric Modulators of mGlu7 Receptor as Putative Antipsychotic Drugs. Front Mol Neurosci. 2018 Sep 20;11:316. doi: 10.3389/fnmol.2018.00316. PMID: 30294258; PMCID: PMC6158327.

3: Marabese I, Boccella S, Iannotta M, Luongo L, de Novellis V, Guida F, Serra N, Farina A, Maione S, Palazzo E. Metabotropic glutamate receptor subtype 7 in the dorsal striatum oppositely modulates pain in sham and neuropathic rats. Neuropharmacology. 2018 Jun;135:86-99. doi: 10.1016/j.neuropharm.2018.03.003. Epub 2018 Mar 2. PMID: 29505788.

4: Fisher NM, Gogliotti RG, Vermudez SAD, Stansley BJ, Conn PJ, Niswender CM. Genetic Reduction or Negative Modulation of mGlu7 Does Not Impact Anxiety and Fear Learning Phenotypes in a Mouse Model of MECP2 Duplication Syndrome. ACS Chem Neurosci. 2018 Sep 19;9(9):2210-2217. doi: 10.1021/acschemneuro.7b00414. Epub 2017 Dec 14. PMID: 29227625; PMCID: PMC6002927.

5: Tassin V, Girard B, Chotte A, Fontanaud P, Rigault D, Kalinichev M, Perroy J, Acher F, Fagni L, Bertaso F. Phasic and Tonic mGlu7 Receptor Activity Modulates the Thalamocortical Network. Front Neural Circuits. 2016 Apr 25;10:31. doi: 10.3389/fncir.2016.00031. PMID: 27199672; PMCID: PMC4842779.

6: Moloney RD, Golubeva AV, O'Connor RM, Kalinichev M, Dinan TG, Cryan JF. Negative allosteric modulation of the mGlu7 receptor reduces visceral hypersensitivity in a stress-sensitive rat strain. Neurobiol Stress. 2015 Apr 4;2:28-33. doi: 10.1016/j.ynstr.2015.04.001. PMID: 26844237; PMCID: PMC4721404.

7: Klar R, Walker AG, Ghose D, Grueter BA, Engers DW, Hopkins CR, Lindsley CW, Xiang Z, Conn PJ, Niswender CM. Activation of Metabotropic Glutamate Receptor 7 Is Required for Induction of Long-Term Potentiation at SC-CA1 Synapses in the Hippocampus. J Neurosci. 2015 May 13;35(19):7600-15. doi: 10.1523/JNEUROSCI.4543-14.2015. PMID: 25972184; PMCID: PMC4429158.

8: Nickols HH, Conn PJ. Development of allosteric modulators of GPCRs for treatment of CNS disorders. Neurobiol Dis. 2014 Jan;61:55-71. doi: 10.1016/j.nbd.2013.09.013. Epub 2013 Sep 27. PMID: 24076101; PMCID: PMC3875303.

9: Kalinichev M, Rouillier M, Girard F, Royer-Urios I, Bournique B, Finn T, Charvin D, Campo B, Le Poul E, Mutel V, Poli S, Neale SA, Salt TE, Lütjens R. ADX71743, a potent and selective negative allosteric modulator of metabotropic glutamate receptor 7: in vitro and in vivo characterization. J Pharmacol Exp Ther. 2013 Mar;344(3):624-36. doi: 10.1124/jpet.112.200915. Epub 2012 Dec 20. Erratum in: J Pharmacol Exp Ther. 2013 May;345(2):328. PMID: 23257312.

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