Tesamorelin

HCID 16137828CAS 218949-48-5
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기본 정보

표준 SMILES
CC/C=C/CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O)[C@@H](C)CC)C(C)C)[C@@H](C)O)[C@@H](C)CC
InChIKey
QBEPNUQJQWDYKU-BMGKTWPMSA-N
분자식
C221H366N72O67S
평균 분자량
5,136 g/mol
단동위원소 질량
5,132.71664025

개요

Tesamorelin is a stabilized synthetic peptide analogue of the hypothalamic peptide, Growth Hormone Releasing Hormone (GHRH) indicated for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy. Lipodystrophy is a metabolic condition characterized by insulin resistance, fat redistribution, and hyperlipidemia associated with antiretroviral therapy for HIV infection.

이름 및 식별자

우선 이름
Tesamorelin
IUPAC
(4S)-4-[[2-[[(2S)-5-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-3-carboxy-2-[[(2S)-2-[[(2S)-2-[[(E)-hex-3-enoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]-3-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoyl]amino]-3-carboxypropanoyl]amino]-3-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-5-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
영어명
Tesamorelin
분자식
C221H366N72O67S
분자량
5135.86

이름 및 동의어

Tesamorelin218949-48-5TH9507MQG94M5EEODTXSID00583207TH 9507tesamorelinatesamorelinetesamorelinumTH-9507CHEBI:63626GHRH(1-44)
이름 더 보기
Adipotide/FTTPtesamorelTesamorelin 5mg/10mg/20mgTSM2D06655TirelinTimorelinTesamoreli APITesamorelin 8866
RefChem:57140N-((3E)-1-oxo-3-hexenyl)Somatoliberin (human pancreatic islet)DTXCID30533972H01AC06Egrifta804475-66-9UNII-MQG94M5EEOTesamorelin [USAN:INN]

데이터베이스 식별자

CAS
218949-48-5
PubChem CID
16137828
DTXSID
DTXSID00583207
ChEMBL
CHEMBL1237026

물성

구조 계산 물성

XLogP
-23.3
극성 표면적
2,360 Ų
수소 결합 공여자 수
83
수소 결합 수용자 수
76
회전 가능 결합 수
187
무거운 원자 수
361

실험 및 물리화학적 성질

Biologics · 3건

Biologic product (Egrifta) -> FDA Purple Book

Biologic product (Egrifta SV) -> FDA Purple Book

Biologic product (Egrifta WR) -> FDA Purple Book

물리화학적 성질

저장 조건
2 · 2-8°C Refrigerator

안전 및 규제

독성 정보

Hepatotoxicity · 1건

In clinical trials in patients with HIV-associated lipodystrophy, tesamorelin therapy was not associated with de novo elevations in serum enzymes and, in some studies, was associated with decreases in preexisting ALT elevations, possibly mediated by improvements in nonalcoholic fatty liver. Instances of clinically apparent liver injury attributable to tesamorelin use have not been reported.

화학 및 산업

약리 정보

ATC Code · 2건

H - Systemic hormonal preparations, excl. sex hormones and insulins

QH - Systemic hormonal preparations, excl. sex hormones and insulin

PharmacodynamicsTesamorelin stimulates growth hormone secretion, and subsequently increases IGF-1 and IGFBP-3 levels.
Mechanism of Action · 1건

By acting on the pituitary cells in the brain, tesamorelin stimulates production and release of the endogenous hormone (hGRF). Tesamorelin therapy predisposes the patient to glucose intolerance and can also increase the risk of type 2 diabetes, so the drug is contraindicated in pregnancy.

Biological Half-Life26 and 38 minutes in healthy subjects and HIV-infected patients, respectively.
Metabolism/MetabolitesNo formal metabolism studies have been performed in humans.
FDA Pharmacological Classification · 5건

MQG94M5EEO

TESAMORELIN

Physiologic Effects [PE] - Increased GHRH Activity

Established Pharmacologic Class [EPC] - Growth Hormone Releasing Factor Analog

Tesamorelin is a Growth Hormone Releasing Factor Analog. The physiologic effect of tesamorelin is by means of Increased GHRH Activity.

공급사50 곳

上海沛灵生物科技有限公司13127581762 13127581762 · [email protected]
Ningbo Qingteng Plastic Cost.,Ltd.+86-15028138352 +86-19322619905 · [email protected]
LIDE PHARMACEUTICALS LIMITED+852-55945652 · [email protected]
深圳市铭康生物技术有限公司18682083212 · [email protected]
曼顿生物科技（深圳）有限公司+86-75589664337 +86-15112661142 · [email protected]

추가 설명

정의FDA Pharm Classes: Tesamorelin is a Growth Hormone Releasing Factor Analog. The physiologic effect of tesamorelin is by means of Increased GHRH Activity.

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