Taspoglutide

Taspoglutide is a pharmaceutical drug, a glucagon-like peptide-1 agonist (GLP-1 agonist), under investigation for treatment of type 2 diabetes being codeveloped by Ipsen and Roche.

Designed for biological research and industrial applications, not intended for individual clinical or medical purposes.
Taspoglutide(CAS 275371-94-3)

CAT No: 10-101-176

CAS No:275371-94-3

Synonyms/Alias:275371-94-3;SCHEMBL2899791;Taspoglutide trifluoroacetate salt;DB14027;DA-67943;ITM077; R1583; BIM51077;F85503;

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cGMP Peptide
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  • IND and NDA support
  • Drug master files (DMF) filing
M.F/Formula
C152H232N40O45
M.W/Mr.
3339.7
Sequence
One Letter Code:HXEGTFTSDVSSYLEGQAAKEFIAWLVKXR
Three Letter Code:H-His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Aib-Arg-NH2
Labeling Target
Glucagon-like peptide 1 (GLP-1) receptor
Application
Taspoglutide is developed for treatment of type 2 diabetes
Activity
Agonist
Areas of Interest
Metabolic Disease

Taspoglutide is a synthetic peptide analog belonging to the class of glucagon-like peptide-1 (GLP-1) receptor agonists, designed to mimic the activity of endogenous incretin hormones. Characterized by its extended half-life and structural modifications that enhance receptor affinity, Taspoglutide offers a unique profile for research and development in metabolic regulation. Its molecular architecture supports robust receptor activation, translating to pronounced physiological effects in preclinical models. As a tool compound, it is widely recognized for its ability to modulate glucose homeostasis and promote satiety, making it a valuable asset in the exploration of metabolic pathways and energy balance. The peptide's stability and bioactivity have made it a subject of interest across various scientific disciplines, particularly those investigating the mechanisms underlying metabolic disorders and peptide-based therapeutics.

Metabolic Disease Research: Taspoglutide serves as a pivotal agent in the study of metabolic diseases, particularly for elucidating the complex signaling pathways involved in glucose regulation and insulin secretion. By acting as a GLP-1 receptor agonist, it enables researchers to dissect the downstream effects of incretin signaling, providing insights into pancreatic beta-cell function, insulinotropic activity, and glucagon suppression. Its application in in vitro and in vivo models facilitates the identification of molecular targets and the evaluation of novel therapeutic strategies aimed at improving glycemic control. The use of this peptide in metabolic research not only advances the understanding of disease mechanisms but also supports the discovery of next-generation peptide analogs with improved pharmacological profiles.

Appetite and Weight Regulation Studies: As an incretin mimetic, Taspoglutide has proven instrumental in research focused on appetite suppression and weight management. Through activation of central and peripheral GLP-1 receptors, it influences satiety centers in the brain and modulates gastrointestinal motility, leading to reduced food intake in experimental settings. Scientists utilize this compound to investigate the neuroendocrine regulation of hunger and satiety, as well as to explore the interplay between gut hormones and energy expenditure. Its ability to induce weight loss in preclinical models makes it a reference molecule for comparative studies evaluating the efficacy of emerging anti-obesity agents.

Cardiovascular Function Investigation: The impact of GLP-1 receptor agonists on cardiovascular health has garnered significant attention, and Taspoglutide is frequently employed in studies assessing cardiac and vascular function. By modulating endothelial function, reducing oxidative stress, and influencing myocardial metabolism, it provides a framework for understanding the cardioprotective potential of incretin-based therapies. Experimental use of this peptide extends to models of atherosclerosis, hypertension, and ischemic injury, where its effects on vascular remodeling and inflammatory pathways are systematically evaluated. These investigations contribute to a broader comprehension of how metabolic peptides can modulate cardiovascular risk factors beyond glycemic control.

Beta-cell Preservation and Regeneration: Preservation of pancreatic beta-cell mass is a central theme in diabetes research, and Taspoglutide has emerged as a valuable tool for probing the mechanisms of beta-cell survival and regeneration. Its ability to stimulate beta-cell proliferation, reduce apoptosis, and enhance insulin biosynthesis is leveraged in studies aiming to prevent or reverse beta-cell dysfunction. Researchers employ it in cellular and animal models to identify signaling cascades that promote islet cell health, facilitating the development of therapeutic interventions that target beta-cell preservation. The insights gained from these studies have implications for the design of regenerative strategies in metabolic diseases.

Pharmacological Screening and Drug Development: In the domain of drug discovery, Taspoglutide is utilized as a reference compound for the screening of novel GLP-1 receptor agonists and related peptides. Its well-characterized pharmacodynamic and pharmacokinetic properties enable comparative analyses, guiding the optimization of lead candidates with improved efficacy and safety profiles. The peptide's role in high-throughput screening assays and structure-activity relationship studies accelerates the identification of promising compounds for further development. By serving as a benchmark in pharmacological research, it supports the advancement of innovative therapies targeting metabolic and endocrine disorders. Through these diverse applications, Taspoglutide continues to drive scientific progress in metabolic research, offering a versatile platform for the exploration of peptide-based modulation of physiological processes.

Source#
Synthetic
InChI
InChI=1S/C152H232N40O45/c1-20-78(10)119(145(233)168-81(13)125(213)174-105(63-87-66-162-92-39-28-27-38-90(87)92)134(222)176-101(59-75(4)5)135(223)187-117(76(6)7)143(231)173-95(41-30-32-56-154)142(230)192-152(18,19)148(236)184-93(122(157)210)42-33-57-161-150(158)159)189-136(224)103(60-84-34-23-21-24-35-84)177-131(219)99(50-54-115(206)207)172-130(218)94(40-29-31-55-153)170-124(212)80(12)166-123(211)79(11)167-129(217)98(47-51-110(156)199)169-111(200)68-163-127(215)96(48-52-113(202)203)171-132(220)100(58-74(2)3)175-133(221)102(62-86-43-45-89(198)46-44-86)178-139(227)107(70-193)181-141(229)109(72-195)182-144(232)118(77(8)9)188-138(226)106(65-116(208)209)179-140(228)108(71-194)183-147(235)121(83(15)197)190-137(225)104(61-85-36-25-22-26-37-85)180-146(234)120(82(14)196)186-112(201)69-164-128(216)97(49-53-114(204)205)185-149(237)151(16,17)191-126(214)91(155)64-88-67-160-73-165-88/h21-28,34-39,43-46,66-67,73-83,91,93-109,117-121,162,193-198H,20,29-33,40-42,47-65,68-72,153-155H2,1-19H3,(H2,156,199)(H2,157,210)(H,160,165)(H,163,215)(H,164,216)(H,166,211)(H,167,217)(H,168,233)(H,169,200)(H,170,212)(H,171,220)(H,172,218)(H,173,231)(H,174,213)(H,175,221)(H,176,222)(H,177,219)(H,178,227)(H,179,228)(H,180,234)(H,181,229)(H,182,232)(H,183,235)(H,184,236)(H,185,237)(H,186,201)(H,187,223)(H,188,226)(H,189,224)(H,190,225)(H,191,214)(H,192,230)(H,202,203)(H,204,205)(H,206,207)(H,208,209)(H4,158,159,161)/t78-,79-,80-,81-,82+,83+,91-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,117-,118-,119-,120-,121-/m0/s1
InChI Key
WRGVLTAWMNZWGT-VQSPYGJZSA-N
BoilingPoint
N/A
Melting Point
N/A

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