J Hicks

Literature NMR? Is that a catalogue of how the compound should look in an NMR? I don't know where to access that data.

So I had an NMR done on the compound, but now I'm trying to make sense of it. I've attached the files. Can anyone help me understand if what this NMR means. This it's the compound that it's supposeded to be: https://medkoo.com/products/15235 Any thoughts would be greatly appreciated. BCJ-5279_1H_2.pdf BCJ-5279_1H.pdf

Thank you, so I assume from your comments that it is a possibility that the substance I received is structurally incorrect, despite having those test results.

MT-II is another peptide analogue of MSH with high binding affinity to the MC1R receptor. Thus it is being used as a control in this study. Is it possible to figure the dose response curve of substance 5 from the information laid out in the paper? From what is being said here in this thread, a dose response curve would illustrate the changing effects of substance 5, rather than merely the EC(50). Also, I assume the pharmacokinetic profile of peptides varies by the peptide type, so there is no way to predict the likely cMAX from substance 5, without an actual trial being done. It seems to me that these two pieces of information, the dose response curve, and the cMAX are the key pieces of information required to understand the drug dose required to stimulate the MC1R receptor.

Thanks for your reply. Does this mean then, that the substance I have received could be structurally incorrect despite the test results noted above?

CMAX refers to the maximum concentration of a specific compound in the plasma following a specific dose.

Hi all, I am conducting research into photo-protection of human skin to prevent skin damage. I have received a promising small molecule compound from a Chinese supplier and I have conducted some basic tests to check if it is in fact the correct substance. So far, I have received a HPLC analysis and also an independent mass spec, which seems to match the target compound (see below). Do you think is it also necessary to have a NMR analysis to confirm the structure? In other words, is it possible that the compound I have received could be 'structurally incorrect', despite having the same mass as the target compound? Any help or comments to answer this question would be welcome, I am attaching the data I have on the compound to this thread and further information on the substance can be found at the following link: https://medkoo.com/products/15235 Mass Spec HPLC

Many thanks for your help with this. So, from what I understand here, if compound 5 reaches a molarity of 4.5nM or higher in the plasma, it will thus achieve the EC(50) level of agonist activity for the MC1 receptor. So the pertinent information/data here would be the dose and related CMAX from a pharmacokinetic profile of the substance. However, as there are no studies at this time on the pharmacokinetics of the compound, any answers will only be theoretical unfortunately.

In other words, you don't know the answer, so why not reserve the pointless, condescending comments? For those who actually understand the question, substance 15 is dosed at 1mg per day to stimulate mc1r receptors, I'm looking to understand if substance 5 is likely to stimulate the same receptor at doses of around 5-10mg, rather than 500mg, as implied by the EC(50). Anyone with knowledge of peptide pharmacokinetics or receptor agonists have an opinion?

Can anyone recommend a forum where you might actually get an answer to a question like this? As opposed to just being interrogated about your reason for posting and then ignored?

No, it's not a homework problem.

We'll I'm wondering if substance 5 would require a much higher dose in vivo than substance 15 to activate the mc1r receptor.

Hi all, I have a question about how drug dose relates to receptor binding efficiency. I have attached a photo of some peptides designed as novel MC1R receptor agonists from the following paper: https://www.researchgate.net/publication/320823039_Design_of_MC1R_Selective_g-MSH_Analogues_with_Canonical_Amino_Acids_Leads_to_Potency_and_Pigmentation The question is this: Substance 5 on the list shows an EC(50) on the MC1R receptor of 4.5nM, whilst substance 15 shows an EC(50) of 0.01nM. Does this effectively mean that substance 5 requires a 450 fold dose to match the potential effect of substance 15, assuming that pharmacokinetics are roughly equal? Any thoughts you might have would be welcome. Cheers guys.