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LY 379268，Group II mGlu激动剂(ab120196)

Submit a review Q&A (6)References (8)
Chemical Structure - LY 379268, Group II mGlu agonist (ab120196)

    Key features and details

    • Group II mGlu agonist. Systemically active.
    • CAS Number: 191471-52-0
    • Purity: > 99%
    • Soluble in water to 25 mM (with heating)
    • Form / State: Solid
    • Source: Synthetic

    概述

    • 产品名称

      LY 379268，Group II mGlu激动剂

    • 描述

      Group II mGlu激动剂. Systemically active.

    • 生物学描述

      Highly potent and systemically active mGlu2 and mGlu3 agonist. EC50 values are 2.69 and 4.48 nM for hmGlu2 and hmGlu3, respectively and displays >80-fold selectivity over group I and group III receptors. Effective in several animal models of stroke, epilepsy, drug abuse, schizophrenia, and pain.

    • 纯度

      > 99%

    • CAS编号

      191471-52-0

    • 化学结构

      Chemical Structure

    性能

    图片

    • Chemical Structure - LY 379268, Group II mGlu agonist (ab120196)
      Chemical Structure - LY 379268, Group II mGlu agonist (ab120196)
      2D chemical structure image of ab120196, LY 379268, Group II mGlu agonist

    实验方案

    To our knowledge, customised protocols are not required for this product. Please try the standard protocols listed below and let us know how you get on.

    Click here to view the general protocols

    文献 (8)

    发表研究结果有使用 ab120196？请让我们知道，以便我们可以引用本数据表中的参考文章。

    ab120196 被引用在 8 文献中.

    • Špirková A  et al. Glutamate can act as a signaling molecule in mouse preimplantation embryos†. Biol Reprod 107:916-927 (2022). PubMed: 35746896
    • Liu J  et al. Abnormal Glu/mGluR2/3/PI3K pathway in the hippocampal neurovascular unit leads to diabetes-related depression. Neural Regen Res 16:727-733 (2021). PubMed: 33063735
    • Bragina L  et al. Differential expression of metabotropic glutamate and GABA receptors at neocortical glutamatergic and GABAergic axon terminals. Front Cell Neurosci 9:345 (2015). PubMed: 26388733
    • Yin S  et al. Selective actions of novel allosteric modulators reveal functional heteromers of metabotropic glutamate receptors in the CNS. J Neurosci 34:79-94 (2014). PubMed: 24381270
    • Cuccurazzu B  et al. Upregulation of mGlu2 Receptors via NF-?B p65 Acetylation Is Involved in the Proneurogenic and Antidepressant Effects of Acetyl-L-Carnitine. Neuropsychopharmacology 38:2220-30 (2013). PubMed: 23670591
    • Klakotskaia D  et al. Effects of group II and III metabotropic glutamate receptor ligands on conditioned taste aversion learning. Behav Brain Res 253:9-16 (2013). PubMed: 23827202
    • Gosnell HB  et al. mGluR8 modulates excitatory transmission in the bed nucleus of the stria terminalis in a stress-dependent manner. Neuropsychopharmacology 36:1599-607 (2011). PubMed: 21451497
    • Rylander D  et al. Pharmacological modulation of glutamate transmission in a rat model of L-DOPA-induced dyskinesia: effects on motor behavior and striatal nuclear signaling. J Pharmacol Exp Ther 330:227-35 (2009). PubMed: 19357321

    客户评价及客户问答

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    1-6 of 6 Abreviews or Q&A

    Question

    Can't disolve LY 379268 at 20mM in water + heating + sonication + DMSO.
    The datasheet says "Soluble in water to 25 mM (with warming)"

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    Answer

    Je suis désolé mais je n'ai pas reçu de réponse du laboratoire concernant le problème de solubilisation du LY 379268.
    Désolé pour le délai de notre réponse et merci pour votre patience.

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    Question

    I have accidentally resuspended this product in DMSO instead of water? Is there anything I can do to fix it?

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    Answer

    Since the compound has not dissolved then it depends whether all of the DMSO needs to be removed as this will be extremely difficult.

    If DMSO is not a problem then it may be possible to dissolve the compound by adding water and warming gently. Addition of 1 equivalent NaOH will aid the solubilisation of this compound.

    If DMSO is a problem then, unfortunately, it is very unlikely to be possible to remove it from the compound. It may be possible to decant the DMSO from the suspension once the solid has settled then add cold water and repeat this process a couple of times but it would be impossible to say, with certainty, how much solid would be recovered by this process. Alternatively the suspension could be filtered but, again, it wouldn’t be easy to know how much solid had been recovered due to the small quantity of solid.

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    Question

    Thank you very much for your professionalism. I'll let you know the outcome of this lot. I have discussed the problem with my collaborators who have used LY379268 and have made stock solutions of relatively high concentrations (up to 100mM). They suggest adding 1eq NaOH at the same time as the water. Would you please check with your chemists to see if this is a reasonable method. I would like to hear from Abcam before I try this with the new product you are sending me.
    Sincerely yours,

    Read More
    Answer

    My colleagues have carried out NMR and solubility testing with LY 379268 (ab120196). The NMR confirms that this compound is definitely LY 379268 and they have had no issue with solubility, even though the chemist reported that it took some time and prolonged stirring.
    Could you please let me know if the replacement sample is easier to dissolve than the original one?
    My colleagues are considering testing the sample you received originally, could you please let me know if you still have some of LY 379268 from the first vial and if it would be ok with you to send a small quantity back to us?
    Thank you.

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    Question

    Thank you very much for your professionalism. I'll let you know the outcome of this lot. I have discussed the problem with my collaborators who have used LY379268 and have made stock solutions of relatively high concentrations (up to 100mM). They suggest adding 1eq NaOH at the same time as the water. Would you please check with your chemists to see if this is a reasonable method. I would like to hear from Abcam before I try this with the new product you are sending me.
    Sincerely yours,

    Read More
    Answer

    Thank you for your message and your feedback.
    My colleagues from the lab agree with the suggestion of adding the 1eq of NaOH at the same time as the water if there is a similar issue with the new lot, as this should help.
    Also, my colleagues are very keen to discover the source of the problem and would be very grateful if you would agree to provide feedback on the new batch.
    I hope this is helpful.

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    Question

    Thankyou for your reply. I did exactly as the chemists suggested and the product remained cloudy. I didn't see any crystals, but the solution was not clear. I then added DMSO, as I said, after I tried to dissolve the product in water and the solution is a little clearer but I wouldn't say it is perfect. I then tried out the LY379268 in a slice preparation today. This group II agonist is supposed to reduce glutamate transmission at excitatory synapses by activating presynaptic mGlu2/2 receptors. In my experiment, there was no effect on evoked EPSCs at the mossy fiber / CA3 synapse. This is not normal. I think there may be a problem with your product. To begin with, it was impossible to dissolve in water (I tried 20 mM and you say we can go to 25 mM while other labs
    I know go up to 100 mM in water). Secondly, I have no physiological effect. I acknowledge that 1 experiment is not conclusive, but, I suspect a problem with this product.
    Sincerely,

    Read More
    Answer

    Thank you for confirming these details and for your cooperation.
    I forwarded your email to my colleagues, the details provided enable us to closely monitor the quality of our products.
    I am sorry this product did not perform as stated on the datasheet and for the inconvenience this has caused.
    As a quick I have issued a free of charge replacement with a different lot of ab120196, the order number is ****.
    To check the status of the order please contact our Customer Service team and reference this number.
    Please note that this free of charge replacement vial is also covered by our Abpromise guarantee. Should you still be experiencing difficulties, or if the replacement works, please do not hesitate to let us know.

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    Question

    Merci pour votre réponse. J'ai mis la "solution" au congélateur ... on verra. J'attends plus des informations sur le problème de solubilisation.

    Read More
    Answer

    Merci de nous avoir contactés et pour votre patience.
    Voici la réponse que j'ai reçu du laboratoire:
    "Our chemists have tested this batch and have the following advice:
    We would recommend that heat and sonication is used.
    · Heat in a 60°C water bath for approximately 10 minutes
    · Vortex/sonication on removal
    · Repeat as necessary
    The addition of DMSO is odd as we do not believe that this is necessary to get it into solution. DMSO appears to have no effect once the compound is in solution, however it may be having an effect if the customer is using the DMSO in an attempt to get it into solution".
    J'espère que ces informations vous seront utiles. N'hésitez pas à nous contacter de nouveau si vous avez d'autres questions.

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