Overview

  • Product name
    LY 379268, Group II mGlu agonist
  • Description
    Group II mGlu agonist. Systemically active.
  • Biological description
    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.
  • Purity
    > 99%

Properties

References

This product has been referenced in:
  • Imre G The preclinical properties of a novel group II metabotropic glutamate receptor agonist LY379268. CNS Drug Rev 13:444-64 (2007). Read more (PubMed: 18078428) »
  • Collado I  et al. (2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties. J Med Chem 45:3619-29 (2002). Read more (PubMed: 12166935) »
  • Moldrich RX  et al. Anti-epileptic activity of group II metabotropic glutamate receptor agonists (--)-2-oxa-4-aminobicyclo[3.1.0]hexane-4,6-dicarboxylate (LY379268) and (--)-2-thia-4-aminobicyclo[3.1.0]hexane-4,6-dicarboxylate (LY389795). Neuropharmacology 41:8-18 (2001). Read more (PubMed: 11445181) »
See all 6 Publications for this product

Customer reviews and Q&As

1-6 of 6 Abreviews or Q&A

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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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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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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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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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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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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Please note: All products are "FOR RESEARCH USE ONLY AND ARE NOT INTENDED FOR DIAGNOSTIC OR THERAPEUTIC USE, NOT FOR USE IN HUMANS"

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