1kits (10Vials) .
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▎ Nukae Nye Retatrutide?
Retatrutide nye atike yeye aɖe si wotu ɖe peptide dzi si le triple receptor agonists ƒe hatsotso si tɔa ŋku GLP-1R/GIPR/GCGR, si me amino acid 39 le la me. Lãmetsi siwo le abe insulin ene siwo le dɔgboa me (abe GIP ene) ye ʋãe wòwɔ eƒe wɔwɔme eye to eƒe wɔwɔme ƒe nyonyome dzi la, ate ŋu ana GLP-1 xɔla (GLP-1R), GIP xɔla (GIPR), kple glucagon xɔla (GCGR) nawɔ dɔ le ɣeyiɣi ɖeka me. GLP-1R ƒe dɔwɔwɔ doa insulin ƒe dodo ɖe ŋgɔ, xea mɔ na sukli ƒe dodo, eɖea sukli ƒe agbɔsɔsɔ le ʋu me dzi kpɔtɔna, ehea dɔgboa ƒe ƒuƒlu ɖe megbe, eye wòɖea nuɖuɖu ƒe dzodzro dzi kpɔtɔna; GIPR ƒe dɔwɔwɔ doa ŋusẽ insulin ƒe dodo ƒe ŋusẽkpɔɖeamedzi, egaɖea sukli ƒe agbɔsɔsɔ le ʋu me dzi kpɔtɔna, eye wòwɔa akpa aɖe le suklidɔ si me ʋumemi le hã me; GCGR ƒe dɔwɔwɔ doa ŋusẽzazã ɖe ŋgɔ, enaa aklã me sukli ƒe dzɔdzɔ ƒe mɔxexe ɖe enu, eye wòɖea aklã me ami ƒe sisi dzi kpɔtɔna.
▎ Retatrutide ƒe Dɔwɔɖoɖo
Dzɔtsoƒe: PubChem |
Tsitretsitsi: YA⊃1;QGTFTSDYSI-L⊃2;LDKK4AQA⊃1;AFIEYLLEGGPSSGAPPPS⊃3; Molekyulãwo ƒe Mɔfiame: C 221H 342N 46O68 Molekyulã ƒe Kpekpeme: 4731 g/mol CAS ƒe xexlẽdzesi: 2381089-83-2 PubChem ƒe CID: 171390338 Nya siwo sɔ kple wo nɔewo:LY3437943 |
▎ Retatrutide ƒe Numekuku
Nukae nye numekuku si Retatrutide wɔ?
Numekuku si wowɔ tso Retatrutide ŋu do ƒome kplikplikpli kple xexeame katã ƒe nya siwo le sesẽm ɖe edzi le lolo akpa kple lãmenugbagbeviwo ƒe dɔwɔwɔ ŋu, kpakple seɖoƒe siwo le atike siwo wozãna tsɔ daa dɔe ŋu: lolo akpa kple lãmenugbagbeviwo ƒe dɔwɔwɔ nye afɔku gã aɖe na dukɔa ƒe lãmesẽ, eye wobu akɔnta be xexeame katã ƒe lolo akpa ƒe xexlẽme aɖo biliɔn 4.005 le ƒe 2035 me eye lãmenugbagbeviwo ƒe dɔwɔwɔ ŋuti dɔnɔwo ƒe xexlẽme adzi ɖe edzi va ɖo 592 miliɔn, si wɔnɛ be wozãa ga gbogbo aɖe ɖe xexeame katã ƒe lãmesẽnyawo ŋu le lãmenugbagbeviwo ƒe dɔwɔwɔ ta. Multi-target receptor agonist peptides do abe egbɔkpɔnu ene, si te ŋu xea mɔ na lolo akpa, daa lãmenugbagbeviwo ƒe dɔwɔwɔ, eye wòƒoa asa na atike siwo li xoxo ƒe aɖi ƒe nugbegblẽ le ame ŋu, si wɔe be wozu nuwɔna le lolo akpa kple lãmenugbagbeviwo ƒe dɔwɔwɔ ƒe atikewɔwɔwo toto vɛ me.
Nukae nye Retatrutide ƒe dɔwɔwɔ ƒe mɔnu?
Ŋusẽ ƒe asitɔtrɔ le lãmenugbagbeviwo ŋu to multi-receptor activation me
Retatrutide nye atike etɔ̃ siwo xɔa dɔlékuiwo si tɔa ŋku insulinotropic polypeptide xɔla si nɔa te ɖe sukli dzi (GIPR), sukli si le abe peptide-1 xɔla (GLP-1R), kple suklixɔla (GCGR). Enaa ŋusẽ ƒe xɔla etɔ̃ siawo wɔa dɔ le ɣeyiɣi ɖeka me, eye wòɖɔa ŋusẽ ƒe asitɔtrɔ le lãmenugbagbeviwo ŋu to mɔ vovovowo dzi.
GIPR agonist ƒe dɔwɔwɔ:
GIP nye lãmetsi si ɖea insulin le dɔgboa me si dɔgboa me K lãmenugbagbeviwo ɖena dona eye wòdona le nuɖuɖu vɔ megbe. Retatrutide nana GIPR wɔa dɔ, si doa insulin ƒe dodo ɖe ŋgɔ, enaa insulin ƒe dɔwɔwɔ dzina ɖe edzi, eye wòtoa esia me kpena ɖe ŋutilãa ŋu wòxɔa sukli nyuie wu hezãnɛ, si wɔnɛ be sukli ƒe agbɔsɔsɔ dzi ɖena kpɔtɔna le ʋu me. Tsɔ kpe ɖe eŋu la, GIP ate ŋu akpɔ ŋusẽ ɖe ami ƒe asitɔtrɔ dzi to ami ƒe dɔwɔwɔ dzi kpɔkpɔ kple ami ƒe ƒuƒoƒo dzi ɖeɖe kpɔtɔ me [1]..
GLP-1R agonist ƒe dɔwɔwɔ:
GLP-1 nye peptide lãmetsi si dɔgboa me L lãmenugbagbeviwo ɖena dona. Ne Retatrutide na GLP-1R wɔ dɔ vɔ la, ewɔa viɖe vovovowo. Ate ŋu aʋã insulin ƒe dodo le mɔ si nɔa te ɖe sukli ƒe agbɔsɔsɔ dzi nu, si ana sukli ƒe agbɔsɔsɔ naɖiɖi le ʋu me. Ate ŋu ahe dɔgboa ƒe tsi ƒuƒlu ɖe megbe, ana ame naɖi ƒo, eye wòaɖe nuɖuɖu dzi akpɔtɔ. GLP-1R agonistism ate ŋu awɔ dɔ ɖe lãmeka siwo le titina hã dzi, si ana nuɖuɖu ƒe dzodzro kple ŋusẽ nada asɔ, si ana wòakpe ɖe ame ƒe lolo dzi ɖeɖe kpɔtɔ ŋu [2]..
GCGR agonist ƒe ŋusẽkpɔɖeamedziwo:
Zi geɖe la, glucagon dzia sukli ƒe agbɔsɔsɔ ɖe ʋu me ɖe edzi, gake le Retatrutide ƒe ŋusẽkpɔɖeamedzi te la, GCGR agonistism wɔa dɔ vovovowo. Edoa glycogenolysis kple gluconeogenesis ɖe ŋgɔ le aklã me. Le Retatrutide ƒe ŋusẽkpɔɖeamedzi ƒokpli nu la, ŋutilãa mekpɔa sukli ƒe agbɔsɔsɔ si le ʋu me ƒe dzidziɖedzi bɔbɔe o ke boŋ eɖɔa ŋusẽ ƒe asitɔtrɔ ɖo be ami ƒe gbagbã nadzi ɖe edzi, si wɔnɛ be eƒe lolome dzi ɖena kpɔtɔna eye wònaa lãmenugbagbeviwo ƒe dɔwɔwɔ nyona ɖe edzi. GCGR agonistism ate ŋu akpɔ ŋusẽ ɖe aklã me ʋumemi ƒe asitɔtrɔ hã dzi, si aɖe aklã me ami ƒe ƒoƒo ɖe lãme na ame dzi akpɔtɔ [3]..
Ŋusẽkpɔɖeamedzi ɖe Suklidɔ ƒe Lãmetsiŋusẽ ƒe Dɔwɔnawo Dzi
To Retatrutide ƒe dɔwɔwɔ ɖe lãmenugbagbevi etɔ̃ siwo míeyɔ va yi dzi le ɣeyiɣi ɖeka me la, ekpɔa ŋusẽ ɖe ŋutilã ƒe dɔwɔwɔ geɖe siwo do ƒome kple lãmenugbagbeviwo ƒe dɔwɔwɔ dzi.
Ʋumesukli ƒe agbɔsɔsɔ dzi kpɔkpɔ:
To GIPR kple GLP-1R ƒe dɔwɔwɔ be woado insulin ƒe dodo ɖe ŋgɔ, kple GCGR ƒe ɖoɖowɔwɔ nyuie me la, Retatrutide ate ŋu aɖe sukli ƒe agbɔsɔsɔ le ʋu me dzi akpɔtɔ. Eƒe suklidɔ dzi ɖeɖe kpɔtɔ ƒe ŋusẽkpɔɖeamedzi dzena ne suklidɔ dzi ɖe edzi, evɔ anɔ eme be mahe suklidɔ ƒe ɖiɖi vɛ ne sukli ƒe agbɔsɔsɔ le ʋu me sɔ o, si ɖea vi na suklidɔlélawo ƒe ʋumesukli dzi ɖeɖe kpɔtɔ [4]..
Kpekpeme dzi kpɔkpɔ:
Retatrutide ɖee fia be ewɔa dɔ nyuie ŋutɔ le kpekpeme dzi kpɔkpɔ me. To GLP-1R ƒe dɔwɔwɔ me la, enaa dɔgboa me tsi ƒuƒlu blewu, enaa ame ƒe dzidzeme dzina ɖe edzi, eye wòɖea nuɖuɖu si woɖuna dzi kpɔtɔna; to ami ƒe asitɔtrɔ le lãmenugbagbeviwo ŋu dzi wɔwɔ me la, edoa ami ƒe gbagbã kple ŋusẽzazã ɖe ŋgɔ, si wɔnɛ be wòlolona dzi ɖena kpɔtɔna. Dɔdamɔnu dodokpɔwo ɖee fia be dɔnɔ siwo lolo akpa alo lolo akpa siwo wotsɔ Retatrutide da dɔ na la ƒe lolo dzi ɖena kpɔtɔna ŋutɔ le ɣeyiɣi aɖe me [5,6]..
Lãmetsiŋusẽ ƒe ɖoɖowɔwɔ:
Retatrutide zazã nana dɔnɔwo ƒe ʋumemi ƒe agbɔsɔsɔme nyona ɖe edzi. Eɖea triglyceride (TG), lipoprotein cholesterol si mebɔ o (LDL-C), kple lipoprotein cholesterol si mebɔ o ŋutɔ (VLDL-C) ƒe agbɔsɔsɔ dzi kpɔtɔna, eye wògakpɔa apolipoprotein ƒe agbɔsɔsɔ dzi, abe apolipoprotein B (apoB) kple apolipoprotein C -III (apoC-III) ƒe agbɔsɔsɔ dzi ɖeɖe kpɔtɔ ene, si wɔnɛ be lipoprotein ƒe akpa siwo do ƒome kplii ƒe xexlẽme dzi ɖena kpɔtɔna kple ʋukawo ƒe ʋuʋu kple dzitodzitowo ƒe lãmesẽ dodo ɖe ŋgɔ [7]..
Aklã me ʋumemi ƒe asitɔtrɔ le lãme na ame ƒe nyonyo:
Le dɔnɔ siwo ŋu aklãdɔ si me ami mele o (NAFLD) si do ƒome kple lãmenugbagbeviwo ƒe dɔwɔwɔ ƒe dɔmawɔmawɔ nyuie gome la, Retatrutide ɖea aklã me ami dzi kpɔtɔna ŋutɔ. Le dɔdamɔnu dodokpɔ siwo sɔ me la, dɔnɔ siwo wotsɔ Retatrutide ƒe agbɔsɔsɔme vovovowo da dɔe la ɖe aklã me ami ƒe agbɔsɔsɔ dzi ɖe kpɔtɔ ŋutɔ ne wotsɔe sɔ kple gɔmedzedzea, si ɖee fia be Retatrutide kpɔa ŋusẽ nyui ɖe aklã me ami ƒe asitɔtrɔ dzi le ɖoɖowɔwɔ me, si ɖea vi na aklã ƒe dɔwɔwɔ nyuie wu [3]..

Nɔnɔmetata 1 Retatrutide ƒe dɔwɔwɔ ƒe mɔnuwo [8] ..
Nukae nye Retatrutide ƒe dɔwɔwɔwo?
Lolo akpa ƒe atikewɔwɔ:
Lolo akpa va zu xexeame katã ƒe dukɔa ƒe lãmesẽnya vevi aɖe, si do ƒome kplikplikpli kple dɔléle vovovo siwo nɔa anyi didi ƒe gɔmedzedze kple woƒe ŋgɔyiyi. Retatrutide ɖee fia be ewɔa dɔ ɖe ame dzi ŋutɔ le lolo akpa dada me. Dɔnɔ lolo akpa siwo wotsɔ Retatrutide da dɔe la ƒe kpekpeme dzi ɖe kpɔtɔ ŋutɔ. Le kwasiɖa 48 ƒe Akpa 2 ƒe lolo akpa ŋuti numekuku me la, dɔnɔ siwo wotsɔ Retatrutide 8mg kple 12mg da dɔ na la ƒe kpekpeme dzi ɖe kpɔtɔ 22.8% kple 24.2%. Le Akpa 2 lia ƒe dodokpɔ bubu si me wozã ŋku eve le, si wowɔ le vome, si me wozã atike si wotsɔ ɖɔa amee le me la, dɔnɔ siwo le atike ƒe agbɔsɔsɔme vovovowo ƒe hatsotsowo me ƒe lolome dzi ɖe kpɔtɔ le mɔ vovovowo nu le kwasiɖa 24 kple kwasiɖa 48 me. 12mg ƒuƒoƒoa kpɔ kpekpeme dzi ɖe kpɔtɔ 24.2% le kwasiɖa 48 me, gake placebo ƒuƒoƒoa ya kpɔ -2.1% ƒe ɖiɖi ko. Retatrutide ɖea ŋutilã ƒe kpekpeme dzi kpɔtɔna nyuie le dɔnɔ siwo lolo akpa me, si nye dɔwɔnu yeye sẽŋu aɖe si woatsɔ ada lolo akpa. Menye ɖeko retatrutide zazã na lolo akpa ɖea ame ƒe kpekpeme dzi kpɔtɔna ko o, ke ate ŋu ana lãmesẽnya bubu siwo do ƒome kple lolo akpa hã nanyo ɖe edzi, abe ƒunukpeƒetetedɔ dzi ɖeɖe kpɔtɔ kple ƒunukpeƒedɔléle siwo do ƒome kple lolo akpa ƒe dzesiwo dzi ɖeɖe kpɔtɔ to lolo dzi ɖeɖe kpɔtɔ me ene; lolo dzi ɖeɖe kpɔtɔ ate ŋu akpe ɖe ame ŋu hã be kuxi siwo dona tso lolo akpa abe alɔ̃dɔdɔ ƒe gbɔgbɔtsixetsixe ene nanyo ɖe edzi [3,6]..
Atikewɔwɔ ƒomevi 2 lia si ku ɖe lãmenugbagbeviwo ƒe dɔwɔwɔ ŋu:
Lãmetsiŋusẽ ƒe dɔwɔwɔ ƒomevi 2 nye lãmenugbagbeviwo ƒe dɔwɔwɔ ƒe dɔléle si bɔ si nɔa anyi didi si ƒe dzesi enye insulin ƒe dɔlélenutsiŋutete kple insulin ƒe dodo si mesɔ gbɔ o. Asixɔxɔ si ate ŋu anɔ retatrutide ŋu le lãmenugbagbeviwo ƒe dɔwɔwɔ ƒomevi 2 dada me. Edoa ŋusẽ insulin ƒe dodo to GLP-1 xɔla ƒe dɔwɔwɔ me, enaa insulin ƒe dɔlélenutsiŋutete nyona ɖe edzi, eye wòɖea sukli ƒe agbɔsɔsɔ le ʋu me dzi kpɔtɔna. Eƒe kpekpeme dzi ɖeɖe kpɔtɔ ƒe ŋusẽkpɔɖeamedziwo hã kpena ɖe dɔnɔ siwo ƒe lãmenugbagbeviwo ƒe dɔwɔwɔ ƒomevi 2 ƒe nɔnɔme nyona ɖe edzi, elabena lolo akpa nye afɔku vevi aɖe na lãmenugbagbeviwo ƒe dɔwɔwɔ ƒomevi 2, eye lolo dzi ɖeɖe kpɔtɔ ate ŋu ana insulin ƒe dɔwɔwɔ nanyo ɖe edzi, si akpe ɖe ame ŋu geɖe wu le ʋumesukli ƒe dɔwɔwɔ dzi ɖuɖu me. Le numekuku siwo ku ɖe dɔnɔ siwo ƒe lãmenugbagbeviwo ƒe dɔwɔwɔ ƒomevi 2 ŋu me la, Retatrutide na woƒe lolo dzi ɖe kpɔtɔ ŋutɔ eye hemoglobin A1c (HbA1c) ƒe agbɔsɔsɔ dzi ɖe kpɔtɔ ŋutɔ, eye HbA1c dzi ɖe kpɔtɔ 1.64% ne wotsɔe sɔ kple atike si wotsɔ ɖɔa amee. Esia ɖee fia be menye ɖeko Retatrutide kpɔa ʋumesukli ƒe agbɔsɔsɔ dzi nyuie ko o, ke enaa dɔnɔ siwo ƒe lãmenugbagbeviwo ƒe dɔwɔwɔ ƒomevi 2 ƒe nɔnɔme bliboa hã nyona ɖe edzi to mɔnu vovovowo dzi, siwo dome lolo dzi ɖeɖe kpɔtɔ hã le, si wɔnɛ be woƒe agbenɔnɔ nyona ɖe edzi [6]..
Aklãdɔ si me ami mele o (NAFLD) dada:
NAFLD nye aklã ƒe abi si lãmenugbagbeviwo ƒe nuteɖeamedzi hena vɛ si do ƒome kplikplikpli kple insulin ƒe dɔlélenutsiŋutete kple domenyiŋusẽfianu ƒe dɔlélenutsiŋutete, si lɔ nɔnɔme vovovo siwo dometɔ aɖewoe nye aklã bɔbɔe si me ami mele o, steatohepatitis si me aha mele o, kple aklãdɔ si do ƒome kplii ɖe eme. Retatrutide ɖe ŋutete si ŋugbe wodo fia le NAFLD dada me. Le dodokpɔ si wowɔ le vome, si me wozã atike eve le, si me wokpɔ gome le siwo me ami ƒe aklãdɔ si do ƒome kple lãmenugbagbeviwo ƒe dɔwɔwɔ ƒe dɔmawɔmawɔ nyuie eye aklã me ami ƒe agbɔsɔsɔ ≥10% le, le kwasiɖa 24 me la, tɔtrɔ si le aklã me ami ƒe agbɔsɔsɔ le mama dedie nu tso gɔmedzedzea me to vovo ŋutɔ le Retatrutide ƒe agbɔsɔsɔme ƒe hatsotsowo katã me: -81.4% le 8mg ƒuƒoƒoa me, -82.4% le 12 mg me ƒuƒoƒoa me, kple +0.3% le placebo ƒuƒoƒoa me. Esia ɖee fia be Retatrutide ate ŋu aɖe ami si le aklã me dzi akpɔtɔ nyuie, si le vevie ŋutɔ na NAFLD dɔnɔwo ƒe aklãdɔléle ƒe nyonyo. Edo ŋugbe be enye atikewɔmɔnu yeye na NAFLD, si ate ŋu ana dɔlélea ƒe ŋgɔyiyi nagbɔdzɔ eye wòaɖe kuxi sesẽwo abe ʋumenugbagbeviɣidɔ ene ƒe afɔkua dzi akpɔtɔ [3]..
Nyanuwuwuw
Retatrutide ɖe ŋutete si ŋugbe wodo fia le NAFLD dɔnɔwo ƒe aklãdɔléle ƒe nɔnɔme nyonyo me, ewɔa dɔ to mɔnu vovovowo dzi siwo dometɔ aɖewoe nye ŋusẽ ƒe asitɔtrɔ, insulin ƒe dɔlélenutsiŋutete ƒe nyonyome, dɔlékuiwutikewo ƒe ŋusẽkpɔɖeamedzi, kple ʋumemi ƒe asitɔtrɔ.
Le Agbalẽŋlɔla La Ŋu
Nusiwo míeyɔ ɖe etame la katã nye esiwo ŋu Cocer Peptides wɔ numekuku le, trɔ asi le wo ŋu eye woƒo wo nu ƒu.
Dzɔdzɔmeŋutinunya ƒe Agbalẽŋlɔla
Rosenstock, J nye agbalẽnyala ɖedzesi aɖe si ƒe dɔwɔwɔ do ƒome kplikplikpli kple dɔwɔƒe xɔŋkɔ geɖewo, siwo dometɔ aɖewoe nye Texas Yunivɛsiti ƒe Southwestern Medical Center, Texas Yunivɛsiti Dallas, kple Canada VIGOR Centre. Eƒe numekukuwo ku ɖe akpa geɖewo abe Endocrinology & Diabetes, General & Internal Medicine, Cardiovascular System & Cardiology, Pharmacology & Pharmacy, kple Research & Experimental Medicine ŋu. Eƒe akpa ɖedzesi siwo wòwɔ na agbalẽnyalawo ƒe habɔbɔa na wokpɔ ŋudzedze ɖe eŋu le afisiafi, abe alesi wòdze le eƒe tiatia enuenu be enye 'Numekula si Woyɔ Vevie le Atikewɔwɔ ƒe Dɔwɔnyawo me' tso ƒe 2017 va ɖo ƒe 2024 me, si te gbe ɖe eƒe nɔƒe vevi kple ŋusẽkpɔɖeamedzi deto si wòkpɔ le atikewɔnyawo ŋuti numekuku me dzi. Woŋlɔ Rosenstock J ŋkɔ ɖe nyayɔyɔ ƒe nyatakaka me [4].
▎ Nyayɔyɔ Siwo Sɔ
[1] Brzozowska P, Frańczuk A, Nowinńska B, kple ame bubuwo. Retatrutide - tɔtrɔ kpata si woto vɛ nyitsɔ laa ƒe GLP agonist - agbalẽwo me dzodzro[J]. Dzedzeme le Kamedefefe me, 2024.DOI: 10.12775 / qs.2024.15.52125.
[2] Doggrell S A. Retatrutide si ɖe ŋugbedodo fia le lolo akpa (kple lãmenugbagbeviwo ƒe dɔwɔwɔ ƒomevi 2)[J]. Eŋutinunyalawo ƒe Nukpɔsusu Le Numekuku Atikewo Ŋu, 2023,32 (11): 997-1001.DOI: 10.1080/13543784.2023.2283020.
[3] Sanyal A. J., Kaplan L. M., Frias J. P., kple ame bubuwo. Triple hormone receptor agonist Retatrutide na aklãdɔ si do ƒome kple lãmenugbagbeviwo ƒe dɔwɔwɔ ƒe dɔmawɔmawɔ nyuie: afɔɖeɖe 2a dodokpɔ si wowɔ le vome[J]. Dzɔdzɔme Atikewɔwɔ, 2024, 30: 2037-2048.DOI: 10.1038 / s41591-024-03018-2.
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NYATAKAKAWO KPLE NUSIWO WOTSƆ ƑE NYATAKAKA SIWO KAtã WOÐO LE NYATAKAKADZRAÐOƑE SIA ME LA KPLE NYATAKAKAWO ƑE MAKAKAKA KPLEE NUFIAFIA ƑE TAÐOÐOWO KO.
Wotrɔ asi le atike siwo wona le nyatakakadzraɖoƒe sia ŋu na numekuku le vitro ɖeɖeko. Wowɔa numekuku le vitro (Latingbe me: *le ahuhɔ̃e me*, si gɔmee nye le ahuhɔ̃e me) le amegbetɔ ƒe ŋutilã godo. Atike siawo menye atikewo o, United States ƒe Nuɖuɖu Kple Atike Ŋuti Dɔwɔƒe (FDA) meda asi ɖe wo dzi o, eye mele be woazã wo atsɔ axe mɔ ɖe atikewɔwɔ, dɔléle, alo dɔléle aɖeke nu, adae, alo adae o. Se de se vevie be woatsɔ atike siawo ade amegbetɔ alo lãwo ƒe ŋutilã me le mɔ ɖesiaɖe nu.