Atraric Acid a Potent Antiandrogen

[ALightInTheDark]

I think it helps against itchy scalp ... but maybe atraric acid has a very short half life because it works only for one hour or 2.

I should try another vehicle ... something that could help to make A-acid to penetrate in a slow way.

Are you using Atraric alone or the whole formula?

 

[folfoxorack]

@ALightInTheDark : "I just received the powder. I mixed it with Alpecin Medicinal Forte (without caffeine), 5g in 50 ml. I will try only on the left side, and if itchy scalp go away the will mean it works." I'm just trying Atraric Acid.

 

[ALightInTheDark]

@ALightInTheDark : "I just received the powder. I mixed it with Alpecin Medicinal Forte (without caffeine), 5g in 50 ml. I will try only on the left side, and if itchy scalp go away the will mean it works." I'm just trying Atraric Acid.

You should really use the whole formula. And change the vehicle to Serioyxl/Stemoxydyl + 2% DMSO like indicated
If it's doin something then I'm sure the whole thing will work better !

 

[folfoxorack]

@ALightInTheDark : You can try yourself, and we will compare our results. I'm trying the cheapest way because I'm low on money.

 

[ALightInTheDark]

@ALightInTheDark : You can try yourself, and we will compare our results. I'm trying the cheapest way because I'm low on money.

I'm in then I will buy everything soon.

 

[folfoxorack]

@ALightInTheDark : Ok good luck. I bought it from creatingperfume, if you're looking for a source.

 

[folfoxorack]

I dont think it's helping ... I still have itchy scalp, sometimes it seems to decrease it and often it seems to do nothing.

 

[Ollie]

Hows this experiment going ?

 

[MrOscar]

I'm trying atraric acid bought as Evernyl some months ago. Unfortunately I got a 10% solution erroneously labeled by the seller as "90% Evernyl ". The seller recognised they did a mistake and they are shipping me the powder.
I have used it at an actual % of 0.22%, 2 ml, in combination with spearmint e.o. 0.5% and allspices e.o. 0.5%.
I'll be using atraric acid at 0.2-0.4% entrapped in ethosomes (phytosterols added) in Pemulen Tr2 gel (hydrophobic side chains C10-C30), with estriol 0.1-0.2%, lipoic acid 0.4% and 0.25% spearmint e.o., trusting on the super efficient delivery of ethosomes. Pemulen and sterols are there with the aim to hamper systemic delivery...maybe I should kill the spearmint as it should work as permeation enhancer and would decrease the size of ethosomes.
I'll make a batch in the next days.

 

[ElToso]

I'm trying atraric acid bought as Evernyl some months ago. Unfortunately I got a 10% solution erroneously labeled by the seller as "90% Evernyl ". The seller recognised they did a mistake and they are shipping me the powder.
I have used it at an actual % of 0.22%, 2 ml, in combination with spearmint e.o. 0.5% and allspices e.o. 0.5%.
I'll be using atraric acid at 0.2-0.4% entrapped in ethosomes (phytosterols added) in Pemulen Tr2 gel (hydrophobic side chains C10-C30), with estriol 0.1-0.2%, lipoic acid 0.4% and 0.25% spearmint e.o., trusting on the super efficient delivery of ethosomes. Pemulen and sterols are there with the aim to hamper systemic delivery.
I'll make a batch in the next days.

Finally here

 

[MrOscar]

yeah! Thanks @FollicleGuardian

 

[FollicleGuardian]

I'm trying atraric acid bought as Evernyl some months ago. Unfortunately I got a 10% solution erroneously labeled by the seller as "90% Evernyl ". The seller recognised they did a mistake and they are shipping me the powder.
I have used it at an actual % of 0.22%, 2 ml, in combination with spearmint e.o. 0.5% and allspices e.o. 0.5%.
I'll be using atraric acid at 0.2-0.4% entrapped in ethosomes (phytosterols added) in Pemulen Tr2 gel (hydrophobic side chains C10-C30), with estriol 0.1-0.2%, lipoic acid 0.4% and 0.25% spearmint e.o., trusting on the super efficient delivery of ethosomes. Pemulen and sterols are there with the aim to hamper systemic delivery...maybe I should kill the spearmint as it should work as permeation enhancer and would decrease the size of ethosomes.
I'll make a batch in the next days.

Glad you're here. Your knowledge about hair loss is world class. Incredibly interesting atraric acid project. I would love it if you keep us updated on this one.

 

[MrOscar]

Hi,
I'm speculating about atraric acid topical dosage.
Here some calculations I have made by using topical finasteride as reference compound even it has obviously different mechanism of action. This to come to a dosage estimate for atraric acid.I don't know if Finasteride is the best reference compound, but at least some info are available for it and I have not a better reference: please share the info and data if you have topical AAs dosage data not giving relevant sides.
Finasteride IC50 as 5ARi is 69 nM. A common effective topical dosage range is 0.1% and 1.5 ml as average volume. Drug dose is then 1.5 mg.
With 1.5 mg we have approx 0.004 millimoles of finasteride.
Atraric acid inhibits AR nuclear translocation at 10 microM, in the presence of 10 nM of DHT in vitro (and IC50 is 3 uM). Under 5ARI inhibition scalp DHT, should be about half of the original concentration.
If we factor the two respective potencies (10 uM for atraric), atraric acid should be then dosed 145X finasteride, so with 150 molar mass, the dose would be 87 mg or , rounded up to 2 ml at 4.5%.
By approaching ethosomes (studies common delivery is 90%), I might go for 0.5%, 2 ml gel.

Any thoughts and better references for topical AAs dosages?

 

[FollicleGuardian]

Hi,
I'm speculating about atraric acid topical dosage.
Here some calculations I have made by using topical finasteride as reference compound even it has obviously different mechanism of action. This to come to a dosage estimate for atraric acid.I don't know if Finasteride is the best reference compound, but at least some info are available for it and I have not a better reference: please share the info and data if you have topical AAs dosage data not giving relevant sides.
Finasteride IC50 as 5ARi is 69 nM. A common effective topical dosage range is 0.1% and 1.5 ml as average volume. Drug dose is then 1.5 mg.
With 1.5 mg we have approx 0.004 millimoles of finasteride.
Atraric acid inhibits AR nuclear translocation at 10 microM, in the presence of 10 nM of DHT in vitro (and IC50 is 3 uM). Under 5ARI inhibition scalp DHT, should be about half of this concentration.
If we factor the two respective potencies (10 uM for atraric), atraric acid should be then dosed 145X finasteride, so with 150 molar mass, the dose would be 87 mg or , rounded up to 2 ml at 4.5%.
By approaching ethosomes (studies common delivery is 90%), I might go for 0.5%, 2 ml gel.

Any thoughts and better references for topical AAs dosages?

Don’t know if this would help for better reference but:

RU58841, 0.8-1.1 nM IC50, No systemic action at 10 mg.

 

[MrOscar]

Got the powder few days ago and made the ethosomes gel, 100 ml batch, in combination with estriol.
Component A (2X strength)
3% refined lecithin (97% fosfolipids, 40% phosphatidyl choline
0.2% Phytosterols (approx 10% of ethanol soluble phospholipids)
Atraric acid 1%
Estriol 0.2%
30% Ethanol
15% Butylene glycol
Deionized water 55%
Ethosomes made by cold method , by dissolving all the actives and lecithin in ethanol-butylene glycol. Used ultrasonic bath for getting fully dispersed the lecithin, as it has a some phospholipids that won't dissolve in ethanol; Phytosterols are not the easiest stuff to be dissolved and require sonication for full dissolution. Then slow water addition under magnetic stirring, followed by sonication in a bath to getting ethosomes size reduction.

Component B (gel 2X strength)
Ethanol 30%
Butylene glycol 15%
Tromethamine (Tris base buffer), 0.53%. Dosage taken by the Lubrizol application guide for Pemulen gel neutralisation as it is acidic.
Pemulen Tr2 0.2%
Deionized water 55%


Component A and B mixed in equal volume to make the gel at target concentrations, so half of everything, with the exception for the base vehicle that is the same for both the components.

Started using it few days ago at about 2.8 ml dosage. My original plan was to use 2 ml/day, but my protocol has weekly usage of dutasteride ethosomes gel and minoxidil ethosomes gel, so as I'm jumping these four days in the 14 days cycle (pen microneedling cycle), I'm compensating these missing days by increasing the dosage (volume).

This compound is equally interesting and cheap, so I would like to give a further try at 0.5% concentration with the supposedly enhanced dermal delivery of the ethosomes.

There are no info on metabolism and half life. The logp is 2.3 and very likely it should undergo glucoronidation and sulphonation before elimination, like similar phenols. Closest compound is resorcinol that goes this route (70%-30%), and it has a dermal half life of 14h, but it is water soluble, so I think atraric acid could last more.

I have found atraric acid has been recently reported working in vitro as an antinflammatory on macrophages cell line as decreases Cox2 via NF-KB (an by AR inhibition when there is DHT?), that is good for PGD2 decrease, but for sure it decreased in vitro thePGE2 and this is not good...
Here the in vitro study.

Atraric Acid Exhibits Anti-Inflammatory Effect in Lipopolysaccharide-Stimulated RAW264.7 Cells and Mouse Models

Lichens, composite organisms resulting from the symbiotic association between the fungi and algae, produce a variety of secondary metabolites that exhibit pharmacological activities. This study aimed to investigate the anti-inflammatory activities of the secondary metabolite atraric acid...

www.mdpi.com

 

[FollicleGuardian]

Got the powder few days ago and made the ethosomes gel, 100 ml batch, in combination with estriol.
Component A (2X strength)
3% refined lecithin (97% fosfolipids, 40% phosphatidyl choline
0.2% Phytosterols (approx 10% of ethanol soluble phospholipids)
Atraric acid 1%
Estriol 0.2%
30% Ethanol
15% Butylene glycol
Deionized water 55%
Ethosomes made by cold method , by dissolving all the actives and lecithin in ethanol-butylene glycol. Used ultrasonic bath for getting fully dispersed the lecithin, as it has a some phospholipids that won't dissolve in ethanol; Phytosterols are not the easiest stuff to be dissolved and require sonication for full dissolution. Then slow water addition under magnetic stirring, followed by sonication in a bath to getting ethosomes size reduction.

Component B (gel 2X strength)
Ethanol 30%
Butylene glycol 15%
Tromethamine (Tris base buffer), 0.53%. Dosage taken by the Lubrizol application guide for Pemulen gel neutralisation as it is acidic.
Pemulen Tr2 0.2%
Deionized water 55%


Component A and B mixed in equal volume to make the gel at target concentrations, so half of everything, with the exception for the base vehicle that is the same for both the components.

Started using it few days ago at about 2.8 ml dosage. My original plan was to use 2 ml/day, but my protocol has weekly usage of dutasteride ethosomes gel and minoxidil ethosomes gel, so as I'm jumping these four days in the 14 days cycle (pen microneedling cycle), I'm compensating these missing days by increasing the dosage (volume).

This compound is equally interesting and cheap, so I would like to give a further try at 0.5% concentration with the supposedly enhanced dermal delivery of the ethosomes.

There are no info on metabolism and half life. The logp is 2.3 and very likely it should undergo glucoronidation and sulphonation before elimination, like similar phenols. Closest compound is resorcinol that goes this route (70%-30%), and it has a dermal half life of 14h, but it is water soluble, so I think atraric acid could last more.

I have found atraric acid has been recently reported working in vitro as an antinflammatory on macrophages cell line as decreases Cox2 via NF-KB (an by AR inhibition when there is DHT?), that is good for PGD2 decrease, but for sure it decreased in vitro thePGE2 and this is not good...
Here the in vitro study.

Atraric Acid Exhibits Anti-Inflammatory Effect in Lipopolysaccharide-Stimulated RAW264.7 Cells and Mouse Models

Lichens, composite organisms resulting from the symbiotic association between the fungi and algae, produce a variety of secondary metabolites that exhibit pharmacological activities. This study aimed to investigate the anti-inflammatory activities of the secondary metabolite atraric acid...

www.mdpi.com

Thanks for the update!

 

[MrOscar]

Type 2 5AR inhibition by atraric acid in vitro with about half of the potency of finasteride.The finasteride IC50 measured in this study is about 8X lower than the known value. Anyway, it works as internal reference standard.

Hereby the link to the study:

Determinación in vitro del efecto de algunas sustancias liquénicas seleccionadas sobre el receptor de andrógenos, la enzima 5alfa-reductasa y la aromatasa para valorarlos como posibles prototipos de fármacos para el tratamiento de desórdenes dependie

repositorio.unal.edu.co