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Purity: ≥98%
VU 0361737 (VU0361737; VU-0361737) is a novel, brain-penetrable and selective positive allosteric modulator (PAM) for mGlu4 receptor with important biological activity. It inhibits mGlu4 receptor with an EC50 of 240 nM and 110 nM at human and rat receptors, respectively. It exhibits little activity against mGlu5/8 receptors.
| ln Vitro |
VU0361737 exhibits inactive behavior at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and weak activity at mGlu5 and mGlu8 receptors[1]. In human neuroblastoma SH-SY5Y cells, VU0361737 (1–10 μM) partially attenuates the effects of doxorubicin and staurosporine on cell death[3].
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| ln Vivo |
After intraperitoneal administration (rat 10 mg/kg), VU0361737 shows terminal elimination half-lives (rat 1.9 h) because of high plasma clearance (894 mL/min/kg)[1].
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| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (225- 250 g)[1]
Doses: 10 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: intraperitoneal (ip)injection Experimental Results: T1/2 (1.9 h). |
| References |
[1]. Engers DW, et al. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J Med Chem. 2009 Jul 23;52(14):4115-8.
[2]. Engers DW, et al. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. J Med Ch [3]. Jantas D, et al. 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 |
| Molecular Formula |
C13H11CLN2O2
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| Molecular Weight |
262.69
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| CAS # |
1161205-04-4
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| Related CAS # |
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| SMILES |
O=C(C1=NC=CC=C1)NC2=CC=C(Cl)C(OC)=C2
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8068 mL | 19.0338 mL | 38.0677 mL | |
| 5 mM | 0.7614 mL | 3.8068 mL | 7.6135 mL | |
| 10 mM | 0.3807 mL | 1.9034 mL | 3.8068 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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Initial HTS hits.J Med Chem.2009 Jul 23;52(14):4115-8. |
Chemical structure of (-)-PHCCC,1, the mGluR4 ago-potentiator VU0155041,2, and mGluR4 PAMs VU0001171,3, VU0080241,4, and VU0092145,5.J Med Chem.2009 Jul 23;52(14):4115-8. |
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