379 replies to this topic

[Reformed-Redan]

Just to note. I'm not spearheading this group buy. ScienceGuy will. ScienceGuy, could you please let us know the total cost for only the positive optical isomer of IDRA-21 as that is the active form of it. The negative isomer may actually inhibit the action of the positive one at the binding site so it's kind of important that it be only the positive optical isomer or else you just end up with a dud.

Edited by yadayada, 26 May 2013 - 05:53 AM.

[ScienceGuy]

We need just the positive optical isomer so what would be the cost of that ScienceGuy?

...ScienceGuy, could you please let us know the total cost for only the positive optical isomer of IDRA-21 as that is the active form of it. The negative isomer may actually inhibit the action of the positive one at the binding site so it's kind of important that it be only the positive optical isomer or else you just end up with a dud.

I did in fact originally specifically requested the POSITIVE OPTICAL ISOMER of IDRA-21; however, this was their reply:

"There is one problem - only one publication in literature describes preparation of pure + enatiomer and its done by chromatographic resolution on very exotic material, on HPLC apparatus... Not doable on 10g scale, even if I would have 2 months to do it.
We had a brainstorm over this and come to a conclusion to try separate optical isomers by crystallization with chiral amines (and few other substances), but I can't say what results it will give as I need ~50g of racemate first, so one of my chemists can try to separate them.

So if you want racemate that's not a problem, but for (+)-IDRA-21 I cannot offer anything reasonable yet."

Thoughts?

Do you want me to obtain a quotation for the POSITIVE OPTICAL ISOMER anyway, even though the cost will likely not be "reasonable"?

Edited by ScienceGuy, 26 May 2013 - 09:17 AM.

[Reformed-Redan]

We need just the positive optical isomer so what would be the cost of that ScienceGuy?

...ScienceGuy, could you please let us know the total cost for only the positive optical isomer of IDRA-21 as that is the active form of it. The negative isomer may actually inhibit the action of the positive one at the binding site so it's kind of important that it be only the positive optical isomer or else you just end up with a dud.

I did in fact originally specifically requested the POSITIVE OPTICAL ISOMER of IDRA-21; however, this was their reply:

"There is one problem - only one publication in literature describes preparation of pure + enatiomer and its done by chromatographic resolution on very exotic material, on HPLC apparatus... Not doable on 10g scale, even if I would have 2 months to do it.
We had a brainstorm over this and come to a conclusion to try separate optical isomers by crystallization with chiral amines (and few other substances), but I can't say what results it will give as I need ~50g of racemate first, so one of my chemists can try to separate them.

So if you want racemate that's not a problem, but for (+)-IDRA-21 I cannot offer anything reasonable yet."

Thoughts?

Do you want me to obtain a quotation for the POSITIVE OPTICAL ISOMER anyway, even though the cost will likely not be "reasonable"?

No, I think racemic might have to do unless someone figures out how to isolate the positive isomer within reasonable bounds. Can you please wait for the synthesis and payment. I'll try and see another quote.

[paul]

The price sounds good, I'm down already just letting you know I'm happy to pay, maybe we could get a bit more if a lot of people are interested.

[spookytooth]

I'm still interested!

[CalMinera]

^^^ As am I. Awaiting further figures.

[Balouk]

I am interested, maby people from EU can go together an make a group?

[Googoltarian]

The negative isomer may actually inhibit the action of the positive one at the binding site so it's kind of important that it be only the positive optical isomer or else you just end up with a dud.

Thoughts?

http://dx.doi.org/10...oma.2008.09.087
http://dx.doi.org/10...asy.2006.11.035

Those articles describe racemization and hydrolysis of IDRA-21 and its enantiomers. IMHO its a waste of time to separate isomers of IDRA, because of racemization in solution, and this includes solutions in vivo.

I was also thinking about possible salts of IDRA similar to salts of Diazoxide - it forms salts with sodium and potassium which are soluble in water, whereas free form is not soluble in water at all. Salt formation will be tried by some labrats

First article points out that IDRA is possibly hydrolysed by stomach acid to quite significant extent, so sublingual administration will improve availability, if in salt form even better results should be expected.

[Reformed-Redan]

The negative isomer may actually inhibit the action of the positive one at the binding site so it's kind of important that it be only the positive optical isomer or else you just end up with a dud.

Thoughts?

http://dx.doi.org/10...oma.2008.09.087
http://dx.doi.org/10...asy.2006.11.035

Those articles describe racemization and hydrolysis of IDRA-21 and its enantiomers. IMHO its a waste of time to separate isomers of IDRA, because of racemization in solution, and this includes solutions in vivo.

I was also thinking about possible salts of IDRA similar to salts of Diazoxide - it forms salts with sodium and potassium which are soluble in water, whereas free form is not soluble in water at all. Salt formation will be tried by some labrats

First article points out that IDRA is possibly hydrolysed by stomach acid to quite significant extent, so sublingual administration will improve availability, if in salt form even better results should be expected.

I've been thinking about instead shoot for the gold and do the 5'ethyl or 5'alkyl derivative of IDRA-21. I'm not sure they are only active in the positive racemic form and are more potent and increase the duration of the EPSP wave spike. Kind of a win win situation.

[1thoughtMaze1]

count me in please

[keflex]

I'd like to particpate as well.

[Reformed-Redan]

UPDATE:

Hi Everyone,

I have now received the quotation from the EUROPEAN CUSTOM SYNTHESIS LAB whom I have used previously; and it is as follows:

IDRA-21 RACEMATE; PURITY: >99.9%; QUANTITY: 200g = US$5,200

Thoughts?

So, I'm wondering how many spots for this grooup buy to fill. At 20 people with 10g each of IDRA-21 the price is a little too steep. Wondering if ScienceGuy, will you be purchasing half of 200g? Thanks.

[autopilot]

Just reiterating. I'm in. Thought I said that such a while ago.

[moomoo]

Please count me in. Happy to trial.

[mr.ed]

Greetings, I am new here but been lurking for a while.
If you still looking for people to buy idra21 you can count me in.

[Reformed-Redan]

Here is the list of persons interested:

spookeytooth
allstargajo
genesis187
ScienceGuy
PWAIN
DamnedOwl
Karmakenic
Hebbeh
prunk
Colli
paul
cATsE
mait
empedocles
peakplasma
izan82
jvvd
Metagene
autopilot
kylehere
shields_05
lourdaud
soulfiremage
lostfalco
Rior
brendan1
FrankMH
DorianGray
Patrick Sylvester
Megatrone
Psionic
dasheenster
Artificiality
SUB-Rx
CalMinera
Daz_Bike
Werper
Neosback
OpaqueMind
Web
Dashwolf
Amorphous
lukem5
sunshinefrost
Picard
"..."
Steve Zissou
brand2
Thor
meatsauce
Karmakenic
ihsanozkan
cere_user5678910
v7znay
trip96
alecnevsky
CLR
Balouk
1thoughtMaze1
keflex
moomoo
mr.ed

Whew! What a long list. This might be a logistical nightmare; but, nothing that can't be done for you guys! By the looks of it there are 60 people interested in obtaining this compound. Insane! The price for 60 members would be around $100 with shipping costs included. I don't know if the supplier is willing to deal with writing out labels for 60 people so we need three distributors. UK/EU, US, and Australia. Anyone willing to be these distributors?

[extiron]

I´m also interested.

[Reformed-Redan]

I'm sorry at 60 people with 5200 it should come out to be around $95.

[uralsky]

Please count me in too if not late

[Reformed-Redan]

Please count me in too if not late

Got you in. Sorry it's unrelated, I got an unlabeled payment from the BPAP group buy. Was it you?

[meta1]

Longtime forum lurker here, please count me in if it is not too late.

[gg141717]

Count me in to, i am very curious

[1thoughtMaze1]

ok 60 people 200g approx 95 each, not bad. sorry I missed it, what's the dosage?

[progress_]

I'm in!

[mr.ed]

Ok, so how does it work here? Do you have rules/guidelines for a group buy? I searched the forum but couldnt find anything?

[Reformed-Redan]

Hey guys. Please stay tuned. I'll be waiting until the BPAP and PRL group buy are done. This might take a while. Too many things are going on at the moment. Anyone else can make this group buy happen, you have the list of participants and setting up payitsquare isn't hard at all.

[Tivows]

In

[Q did it!]

Just want to let everyone here know that the PRL-8-53 has spots open again due to a "Minor but interesting setback. Silver lining in allowing more potentially interested participants." as it has been put. Check the link below to get caught up

http://www.longecity...930#entry591108

[phil8462643]

I am also interested when the time comes for the group buy! thx.

[ExYank]

Hi

Count me in on this

Thanks