>>Signaling Pathways>> GPCR/G protein>> mGluR >>(1R,2S)-VU0155041

(1R,2S)-VU0155041

Catalog No.GC34963

(1R,2S)-VU0155041, VU0155041의 시스 위치이성질체는 EC50이 2.35μM인 부분 mGluR4 작용제입니다.

Products are for research use only. Not for human use. We do not sell to patients.

(1R,2S)-VU0155041 Chemical Structure

Cas No.: 1263273-14-8

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$71.00
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5mg
US$65.00
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10mg
US$102.00
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25mg
US$204.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Animal experiment:

Rats: TVC rats are injected with reserpine and kept in their home cages for 2 hr after injection. Activity is measured by placing rats in photocell activity cages equipped with 16×16 infrared beams. After a 30 min baseline period, rats are given a single intracerebroventricular injection of either L-AP4 (100, 300 or 1000 nM), VU0155041 (93 or 316 nM), or corresponding vehicles, and motor activity is recorded for an additional 30 min[1].

References:

[1]. Niswender CM, et al. Discovery, characterization, and antiparkinsonian effect of novel positiveallosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol. 2008 Nov;74(5):1345-58.

Background

(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.

At both human and rat receptors, the Cis regioisomer of VU0155041 is similar in potency (798±58 nM at human mGluR4 and 693±140 nM at rat mGluR4). Conversely, the concentration-response curve for the Trans regioisomer (VU0155040) does not plateau at the maximum concentration tested. Fold-shift experiments at 30 μM of VU0155041 also shows that the Cis regioisomer is more effective at this concentration on both human and rat mGluR4. VU0155041, induces concentration-dependent shifts in the baseline when examined in fold shift experiments using the thallium flux assay. VU0155041 induces a response that reaches approximately 45% of the maximal glutamate response. VU0155041is a partial agonist of mGluR4 that activates the receptor by interacting with a site that is distinct from the glutamate binding site. VU0155041 exhibitsselectivity for mGluR4 relative to 67 different targets and does not affect the function of striatal NMDA receptors[1].

VU0155041 is soluble in an aqueous vehicle and intracerebroventricular administration of 31 to 316 nM of VU0155041 dose-dependently decreases haloperidol-induced catalepsy and reserpine-induced akinesia in rats. VU0155041, at doses of 31 and 92 nmol, is also able to significantly decrease the cataleptic effects of haloperidol, and the effects of the compound are still present 30 min after infusion. Icv infusion of a 316 nmol dose of VU0155041 also results in a significant reversal of akinesia[1].

References:
[1]. Niswender CM, et al. Discovery, characterization, and antiparkinsonian effect of novel positiveallosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol. 2008 Nov;74(5):1345-58.

Chemical Properties

Cas No. 1263273-14-8 SDF
Canonical SMILES O=C([C@H]1[C@@H](C(NC2=CC(Cl)=CC(Cl)=C2)=O)CCCC1)O
Formula C14H15Cl2NO3 M.Wt 316.18
Solubility DMSO: ≥ 59 mg/mL (186.60 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.1628 mL 15.8138 mL 31.6276 mL
5 mM 0.6326 mL 3.1628 mL 6.3255 mL
10 mM 0.3163 mL 1.5814 mL 3.1628 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 24 reference(s) in Google Scholar.)

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