I-Tesamorelin API
I-Tesamorelin iyisidakamizwa se-peptide yokwenziwa, igama eligcwele yi-ThGRF(1-44)NH₂, okuyi-hormone yokukhula ekhulula i-hormone (GHRH) analog. Ishukumisa i-anterior pituitary ukuze ikhiphe i-hormone yokukhula (GH) ngokulingisa isenzo se-GHRH engapheli, ngaleyo ndlela ikhulise ngokungaqondile izinga le-insulin-like growth factor 1 (IGF-1), ilethe uchungechunge lwezinzuzo kumetabolism kanye nokulungiswa kwezicubu.
Njengamanje, i-Tesamorelin ivunyelwe yi-FDA yokwelashwa kwe-lipodystrophy ehlobene ne-HIV, ikakhulukazi ekunciphiseni ukuqoqwa kwamafutha e-visceral esiswini (izicubu ze-visceral adipose, i-VAT). Kuye kwacwaningwa kabanzi nge- **anti-aging, metabolic syndrome, isifo sesibindi esinamafutha angenalo utshwala (NAFLD/NASH)** kanye neminye imikhakha, ebonisa amathemba okufaka isicelo abanzi.
Indlela yokwenza
I-Tesamorelin iyi-peptide ye-44-amino acid enesakhiwo esifana kakhulu ne-GHRH yemvelo. Indlela yokusebenza yayo yile:
Yenza kusebenze i-GHRH receptor (GHRHR) ukuze ushukumise i-anterior pituitary ukuthi ikhulule i-GH.
Ngemuva kokuthi i-GH iphakanyisiwe, isebenza esibindi nezicubu ezizungezile ukuze kwandiswe i-IGF-1 synthesis.
I-GH ne-IGF-1 ngokubambisana babamba iqhaza ku-fat metabolism, amaprotheni synthesis, ukulungiswa kwamaseli kanye nokugcinwa kwamathambo.
Isebenza kakhulu ekuwohlokeni kwamafutha e-visceral (ukuhlanganisa amafutha) futhi inomthelela omncane kumafutha angaphansi kwesikhumba.
Uma kuqhathaniswa nomjovo oqondile we-GH, i-Tesamorelin ikhuthaza ukugcinwa kwe-GH ngokusebenzisa izindlela ezingapheli, eziseduze nesigqi somzimba futhi igwema ukusabela okubi okubangelwa i-GH ngokweqile, njengokugcinwa kwamanzi nokumelana ne-insulin.
Ucwaningo kanye nempumelelo yomtholampilo
Ukusebenza kwe-Tesamorelin kuqinisekiswe ngezivivinyo eziningi zemitholampilo, ikakhulukazi kulezi zindawo ezilandelayo:
1. I-lipodystrophy ehlobene ne-HIV (izinkomba ezigunyazwe yi-FDA)
I-Tesamorelin inganciphisa kakhulu i-VAT yesisu (isilinganiso sokuncipha kwe-15-20%);
Khulisa amazinga e-IGF-1 futhi uthuthukise isimo somzimba womzimba;
Thuthukisa isimo somzimba futhi unciphise umthwalo ongokwengqondo ohambisana nokwabiwa kabusha kwamafutha;
Ayithinti kakhulu ungqimba lwamafutha angaphansi kwesikhumba, ukuminyana kwamathambo noma imisipha.
2. I-steatohepatitis engeyona utshwala (NASH) kanye ne-fibrosis yesibindi
Ukuhlolwa kwemitholampilo kubonise ukuthi i-Tesamorelin inganciphisa okuqukethwe kwamafutha esibindi (imaging ye-MRI-PDFF);
Kulindeleke ukuthi kuthuthukiswe ukuzwela kwe-insulin ye-hepatocyte;
Isebenza kakhulu ezigulini ezine-HIV ne-NAFLD, futhi inokuvikelwa okungaba khona kwe-broad-spectrum metabolism.
3. I-Metabolic syndrome kanye nokumelana ne-insulin
I-Tesamorelin inciphisa kakhulu amazinga e-triglyceride nokukhuluphala kwesisu;
Ithuthukisa inkomba ye-HOMA-IR futhi isiza ekuthuthukiseni ukumelana ne-insulin;
Ucwaningo luye lwabonisa ukuthi lungathuthukisa amandla e-muscle amaprotheni synthesis, okuzuzisa asebekhulile noma ukululama kwezifo ezingapheli.
Ukukhiqizwa kwe-API nokulawulwa kwekhwalithi
I-Tesamorelin API ehlinzekwa yi-Gentolex Group yethu isebenzisa ubuchwepheshe obuthuthukisiwe besigaba se-peptide synthesis (SPPS) futhi ikhiqizwa ngaphansi kwemvelo ye-GMP. Inezici ezilandelayo:
Ubumsulwa ≥99% (HPLC)
Ayikho i-endotoxin, insimbi esindayo, ukutholwa kwe-solvent eyinsalela efanelekile
Ukulandelana kwe-amino acid nokuqinisekiswa kwesakhiwo nge-LC-MS/NMR
Nikeza ukukhiqizwa okwenziwe ngendlela oyifisayo kuleveli yegremu kuya kwekhilogremu