Cagriniltide
Em Estoque e Pronto para Envio dos EUA
Frete GRATIS em pedidos acima de US$200
Checkout seguro via processador de pagamento criptografado
Apenas para Uso em Pesquisa
Estes produtos sao destinados exclusivamente a pesquisa laboratorial e nao se destinam ao uso medico. Nao sao aprovados pela FDA para diagnosticar, tratar, curar ou prevenir qualquer doenca. Ao adquirir, voce certifica que os produtos serao utilizados exclusivamente para pesquisa e nao para consumo humano ou animal.
Resumo da Pesquisa
19 Citacoes PubMedVisao Geral da Pesquisa Cagriniltide (AM833/NN1213) is a long-acting acylated analogue of human amylin — a 37-aminoacido pancreatic hormone co-secreted with insulin que regula satiety and glucose homeostasis. Native human amylin is unstable, prone to amyloid fibril formation, and has a muito short meia-vida. The first-generation analogue, pramlintide, requer multiplos(as) daily injections.[2] Cagriniltide overcomes these limitations through C20 fatty diacid acylation (via γ-glutamic acid spacer at Lysine 1), que binds serum albumin, extending the meia-vida to 159–195 hours and enabling once-dosagem semanal. Proline substitutions (Pro21, Pro27) and specific aminoacido changes (N14E, V17R) prevent fibril formation and stabilize o peptideo's alpha-helix.[3] O(a) principal therapeutic strategy envolve co-administration with semaglutide (branded as CagriSema). While GLP-1 agonists target incretin pathways, cagriniltide direciona distinct amylin and calcitonin receptors no(a) hindbrain, activating non-overlapping satiety pathways for synergistic perda de peso of up to 22.7% — significantly exceeding qualquer monotherapy.[5][11]
Cagriniltide — Dados de Pesquisa em Resumo
| Propriedade | Valor |
|---|---|
| Citacoes PubMed Referenciadas | 19 |
| Pesquisadores Colaboradores | 3 |
| Condicoes de Armazenamento | Liofilizado: -80°C (2 anos) ou -20°C (1 ano); Reconstituído: -80°C (6 meses) ou -20°C (1 mês); alíquote para prevenir degradação. |
| Padrao de Pureza | ≥99% (HPLC verified, 3rd-party COA) |
| Apenas para Uso em Pesquisa | Nao destinado ao consumo humano. Apenas para uso em pesquisa. |
Visao Geral
Visao Geral da Pesquisa
Cagriniltide (AM833/NN1213) is a long-acting acylated analogue of human amylin — a 37-aminoacido pancreatic hormone co-secreted with insulin que regula satiety and glucose homeostasis. Native human amylin is unstable, prone to amyloid fibril formation, and has a muito short meia-vida. The first-generation analogue, pramlintide, requer multiplos(as) daily injections.[2]
Cagriniltide overcomes these limitations through C20 fatty diacid acylation (via γ-glutamic acid spacer at Lysine 1), que binds serum albumin, extending the meia-vida to 159–195 hours and enabling once-dosagem semanal. Proline substitutions (Pro21, Pro27) and specific aminoacido changes (N14E, V17R) prevent fibril formation and stabilize o peptideo's alpha-helix.[3]
O(a) principal therapeutic strategy envolve co-administration with semaglutide (branded as CagriSema). While GLP-1 agonists target incretin pathways, cagriniltide direciona distinct amylin and calcitonin receptors no(a) hindbrain, activating non-overlapping satiety pathways for synergistic perda de peso of up to 22.7% — significantly exceeding qualquer monotherapy.[5][11]
Mecanismo de Acao
Mecanismo de Acao
Cagriniltide functions como um(a) non-selective dual agonist of ambos(as) calcitonin receptors (CTR) and amylin receptors (AMY1R, AMY2R, AMY3R) — heterodimers of CTR with RAMPs 1, 2, or 3.[3][12]
Receptor Targets & Binding
| Target | Interaction | Evidence |
|---|---|---|
| Calcitonin Receptor (CTR) | Non-selective agonist; class B1 GPCR; EC50 62 pM | Kruse et al. (2021); Cao et al. (2025) cryo-EM[3][9] |
| AMY1R (CTR+RAMP1) | Potent agonist; "bypass" conformation binding | RAMP1/3 KO abolishes weight-loss effects[8] |
| AMY3R (CTR+RAMP3) | Potent agonist; EC50 49 pM (hAMY3R) | Carvas et al. (2025): essencial para efficacy[8][13] |
| CGRPR / AM1R / AM2R | No or muito baixo(a) activity — selective for amylin/calcitonin axis | Fletcher et al. (2021)[12] |
Sinalizacao a Jusante
| Pathway | Effect | Consequence |
|---|---|---|
| Gs / Adenylyl Cyclase / cAMP | Gs-protein ativacao → adenylyl cyclase → intracellular cAMP accumulation | Primary cascata de sinalizacao for satiety[9] |
| Neuronal cFos (AP/NTS/LPBN) | Induces cFos expression in area postrema, nucleus of solitary tract, lateral parabrachial nucleus | Satiety signaling; 57% fewer AP neurons in RAMP1/3 KO[8] |
| Gastric Emptying | Delays gastric emptying → prolonged postprandial fullness | Reduced caloric intake; may affect oral drug absorcao |
| Glucagon Suppression | Suppresses postprandial glucagon from pancreatic α-cells | Improved glycemic control sem hipoglicemia risk[6] |
Unique Binding Characteristics
| Property | Cagriniltide | Salmon Calcitonin |
|---|---|---|
| Receptor Conformation | "Bypass" (stabilized by ionic lock N14E–V17R) | "CT-like" conformation |
| Residence Time | 3–6 minutes (rapid dissociation) | 45–60 minutes (slow dissociation) |
| Desensibilizacao | Prevents receptor downregulacao → sustained perda de peso | Causes receptor downregulacao → weight regain |
RAMP Dependence: Carvas et al. (2025) demonstrated que the weight-lowering and anorectic effects of cagriniltide are strictly dependente de AMY1R and AMY3R — knockout of RAMP1 and RAMP3 aboliu completamente drug efficacy, with 57% fewer neurons ativou no(a) area postrema.[8]
Aplicacoes de Pesquisa
Aplicacoes de Pesquisa
Cagriniltide is atualmente evaluated in late-stage ensaios clinicos across 4+ research domains:
- Obesity & Weight Management — CagriSema (cagriniltide + semaglutide) alcancou 20.4–22.7% perda de peso in Phase 3 REDEFINE 1 trial (n=3,417), significantly outperforming semaglutide monotherapy (15–16%) and cagriniltide monotherapy (11.8%). Targets the "perda de peso plateau" seen with single-agent GLP-1 therapy.[5]
- Type 2 Diabetes — REIMAGINE 2 trial (n=2,728) demonstrated HbA1c reduction of 1.91% with CagriSema vs 1.76% with semaglutide alone (superiority); 73.5% alcancou HbA1c <6.5%. Phase 2 data showed HbA1c reduction of -2.2%.[6][4]
- Reducao do Risco Cardiovascular — REDEFINE 1 analise post-hoc showed systolic pressao arterial diminuiu -10.9 mmHg with CagriSema vs -2.1 mmHg placebo. Significant reduction in hsCRP inflammatory markers. Dedicated REDEFINE 3 MACE outcomes trial is ongoing.[7]
- Combination Therapy for Resistant Phenotypes — Research explores utility for subjects failing GLP-1 monotherapy or requiring bariatric-surgery-level controle de peso. Theoretical combinations with next-generation incretin agonists under investigation.[14]
- Receptor Pharmacology — Cryo-EM structural biology of dual AMYR/CTR agonism; RAMP-dependent signaling; "bypass" vs "CT-like" receptor conformations; rapid-dissociation kinetics preventing dessensibilizacao.[9][10]
Caracteristicas Bioquimicas
| Propriedade | Valor |
|---|---|
| Molecular Formula | C₁₉₄H₃₁₂N₅₄O₅₉S₂ |
| Molecular Weight | 4409.01 Da |
| CAS Number | 1415456-99-3 |
| PubChem CID | 171397054 |
| Sequence (1-Letter) | K(Eicosanedioic acid-γ-Glu)-CNTATCATQRLAEFLRHSSNNFGPILPPTNVGSNTP-NH₂ |
| Sequence (3-Letter) | {Eicosanedioic acid-γ-Glu}-Lys-Cys-Asn-Thr-Ala-Thr-Cys-Ala-Thr-Gln-Arg-Leu-Ala-Glu-Phe-Leu-Arg-His-Ser-Ser-Asn-Asn-Phe-Gly-Pro-Ile-Leu-Pro-Pro-Thr-Asn-Val-Gly-Ser-Asn-Thr-Pro-NH₂ |
| Structure | 37-aminoacido lipidated amylin analogue; C20 fatty diacid via γ-Glu spacer at Lys1; Cys2–Cys7 ponte dissulfeto; Pro21/Pro27 anti-fibrillation substitutions; N14E/V17R ionic lock |
| Origin | Engineered from human amylin scaffold by Novo Nordisk A/S |
| Classification | Long-Acting Amylin Analogue / DACRA / Research Peptide |
| Half-Life | ~159–195 hours (human); ~24h (rat), ~50h (rabbit), ~76h (dog), ~115h (minipig) |
| Bioavailability | ~40% subcutaneo(a) (rat) |
Identificadores
| Purity Standard | |
|---|---|
| Synonyms | |
| InChI Key | |
| Developer |
Resumo da Pesquisa Pre-clinica
Resumo da Pesquisa Pre-clinica
Key Preclinical Studies
| Estudo | Modelo | Principais Achados | Ref |
|---|---|---|---|
| Carvas et al. (2025) | 129S2/SvEv mice — WT vs RAMP1/3 KO; 3–300 nmol/kg SC | 30 nmol/kg: 24h food intake ↓51%; WT lost -3.4g (-6.6%), KO had no effect; 57% fewer AP neurons ativou in KO | [8] |
| Kruse et al. (2021) | Male SD rats — 0.1–30 nmol/kg SC; PK: 10 nmol/kg IV/SC | Food intake reduziu for varios(as) days at 1–10 nmol/kg; T½ 20h (IV), 27h (SC) | [3] |
| Dahl et al. (2024) | Rats — 30 nmol/kg single SC injection | Food intake reduziu 85% at 0–24h and 84% at 24–48h; EC50: hAMY3R 49 pM, hCTR 62 pM | [13] |
Clinical / Human Studies
| Ensaio | Desenho | Key Results | Outcome |
|---|---|---|---|
| REDEFINE 1 NCT05567796 | Phase 3; n=3,417; 68-week RCT; CagriSema 2.4/2.4mg vs sema vs cagri vs placebo | Weight loss: 22.7% (CagriSema) vs 15–16% (sema) vs 11.8% (cagri); SBP -10.9 mmHg; GI AEs 79.6% | SUCCESS[5] |
| REDEFINE 2 NCT05394519 | Phase 3; n=1,206; 68-week RCT in T2D; CagriSema vs placebo | Weight loss: 13.7% vs 3.4%; 73.5% alcancou HbA1c <6.5% vs 15.9% | SUCCESS[6] |
| REIMAGINE 2 NCT06065540 | Phase 3; n=2,728; 68-week active-controlled; CagriSema vs sema 2.4mg | HbA1c: -1.91% vs -1.76% (superiority); weight: 14.2% vs 10.2% | SUCCESS |
| Phase 2 T2D | n=92; 32-week; CagriSema vs sema vs cagri | HbA1c: -2.2% (CagriSema) vs -1.8% vs -0.9%; weight: -15.6% vs -5.1% vs -8.1% | SUCCESS[4] |
| Phase 2 Obesity | n=706; 26-week dose-finding; cagri (0.3–4.5mg) vs liraglutide vs placebo | 4.5mg: 10.8% loss; 2.4mg: 8.9%; liraglutide 3.0mg: 9.0% | SUCCESS[2] |
| Phase 1b | n=95; 20-week; cagri 2.4mg + sema 2.4mg | Weight loss: 17.1% vs 9.8% (sema alone) | SUCCESS[1] |
Os produtos oferecidos neste site são fornecidos apenas para estudos in vitro. Estudos in vitro (do latim: em vidro) são realizados fora do corpo. Estes produtos não são medicamentos ou fármacos e não foram aprovados pelo FDA dos EUA para prevenir, tratar ou curar qualquer condição médica, enfermidade ou doença. A introdução corporal de qualquer tipo em humanos ou animais é estritamente proibida por lei.
Apenas para Pesquisa Laboratorial. Não se destina ao uso humano, uso médico, uso diagnóstico ou uso veterinário.
TODOS OS ARTIGOS E INFORMAÇÕES SOBRE PRODUTOS FORNECIDOS NESTE SITE SÃO APENAS PARA FINS INFORMATIVOS E EDUCACIONAIS.
Autores e Atribuicao
✍️ Autor do Artigo
Thomas Kruse
Thomas Kruse is a lead scientist at Novo Nordisk A/S in Måløv, Denmark. He played a central role no(a) chemical development and structural engineering of cagriniltide, leading a estrutura-activity relationship (SAR) efforts to create a long-acting, estavel amylin analog que ativa ambos(as) amylin receptors e o(a) calcitonin receptor enquanto overcoming the instability and fibrillation issues of native human amylin. His key publications include "Development of Cagrilintide, a Long-Acting Amylin Analogue" (2021, Journal of Medicinal Chemistry) and "NN1213 – A Potent, Long-Acting, and Selective Analog of Human Amylin" (2024, Journal of Medicinal Chemistry). Thomas Kruse is being referenced as one do(a) leading scientists envolveu in cagriniltide research. De forma alguma este(a) médico(a)/cientista endossa ou defende a compra, venda ou uso deste produto por qualquer motivo. Não existe afiliação ou relação, implícita ou de outra forma, entre a Pure US Peptide e este(a) médico(a).
Ver Perfil Completo do Pesquisador →🎓 Autor de Revista Cientifica
W. Timothy Garvey, MD
W. Timothy Garvey, MD is a professor no(a) Department of Nutrition Sciences no(a) University of Alabama at Birmingham. He served as principal investigator para o(a) pivotal Phase 3 REDEFINE program evaluating cagriniltide combined with semaglutide (CagriSema) for perda de peso. His landmark trial demonstrated 22.7% perda de peso with CagriSema in 3,417 adults with overweight or obesidade, along with significant cardiovascular benefits incluindo 10.9 mmHg systolic pressao arterial reduction. His key publications include "Coadministered Cagrilintide and Semaglutide in Adults with Overweight or Obesity" (2025, New England Journal of Medicine) and "CagriSema Reduces Blood Pressure in Adults With Overweight or Obesity: REDEFINE 1" (2026, Hypertension). W. Timothy Garvey is being referenced as one do(a) leading scientists envolveu in cagriniltide research. De forma alguma este(a) médico(a)/cientista endossa ou defende a compra, venda ou uso deste produto por qualquer motivo. Não existe afiliação ou relação, implícita ou de outra forma, entre a Pure US Peptide e este(a) médico(a).
Ver Perfil Completo do Pesquisador →W. Timothy Garvey, MD is being referenced as one of the leading scientists involved in the research and development of Cagriniltide. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Pure US Peptide and this doctor. The purpose of citing the doctor is to acknowledge, recognize, and credit the exhaustive research and development efforts conducted by the scientists studying this peptide.
🔬 Pesquisador Colaborador
David C.W. Lau, MD, PhD
David C.W. Lau, MD, PhD is based no(a) Julia McFarlane Diabetes Research Centre and Libin Cardiovascular Institute of Alberta, University of Calgary Cumming School of Medicine. He led the Phase 2 dose-finding study and Phase 1b safety/tolerability trials que estabeleceu a dose-dependente perda de peso effects of cagriniltide monotherapy e seu(sua) perfil de seguranca quando co-administered with semaglutide. His key publications include "Once-weekly cagrilintide for controle de peso in people with overweight and obesidade" (2021, The Lancet) and "Safety, tolerability, pharmacokinetics, and pharmacodynamics of concomitant administration of cagrilintide with semaglutide" (2021, The Lancet). David C.W. Lau is being referenced as one do(a) leading scientists envolveu in cagriniltide research. De forma alguma este(a) médico(a)/cientista endossa ou defende a compra, venda ou uso deste produto por qualquer motivo. Não existe afiliação ou relação, implícita ou de outra forma, entre a Pure US Peptide e este(a) médico(a).
Ver Perfil Completo do Pesquisador →David C.W. Lau, MD, PhD is being referenced as one of the leading scientists involved in the research and development of Cagriniltide. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Pure US Peptide and this doctor. The purpose of citing the doctor is to acknowledge, recognize, and credit the exhaustive research and development efforts conducted by the scientists studying this peptide.
Citacoes Referenciadas
Enebo LB, et al. Safety, tolerability, pharmacokinetics, and pharmacodynamics of concomitant administration of multiplos(as) doses of cagrilintide with semaglutide 2.4 mg for controle de peso: a randomised, controlled, phase 1b trial. Lancet, 397(10286), 1736-1748, 2021.
PubMedLau DCW, et al. Once-weekly cagrilintide for controle de peso in people with overweight and obesidade: a multicentre, randomised, duplo-cego, controlado por placebo and active-controlled, dose-finding phase 2 trial. Lancet, 398(10317), 2160-2172, 2021.
PubMedKruse T, et al. Development of Cagrilintide, a Long-Acting Amylin Analogue. Journal of Medicinal Chemistry, 64(15), 11183-11194, 2021.
PubMedFrias JP, et al. Efficacy and safety of co-administered uma vez por semana cagrilintide 2.4 mg with uma vez por semana semaglutide 2.4 mg in diabetes tipo 2: a multicentre, randomised, duplo-cego, active-controlled, phase 2 trial. Lancet, 402(10403), 720-730, 2023.
PubMedGarvey WT, et al. Coadministered Cagrilintide and Semaglutide in Adults with Overweight or Obesity. New England Journal of Medicine, 393(7), 635-647, 2025.
PubMedDavies MJ, et al. Cagrilintide–Semaglutide in Adults with Overweight or Obesity and Type 2 Diabetes. New England Journal of Medicine, 393(7), 648-659, 2025.
PubMedVerma S, et al. CagriSema Reduces Blood Pressure in Adults With Overweight or Obesity: REDEFINE 1. Hypertension, 83(2), e26055, 2026.
PubMedCarvas AO, et al. Cagrilintide lowers bodyweight through brain amylin receptors 1 and 3. EBioMedicine, 118, 105836, 2025.
PubMedCao J, et al. Structural and dynamic features of cagrilintide binding to calcitonin and amylin receptors. Nature Communications, 16, 3389, 2025.
PubMedGu YM, et al. Structural and mechanistic insights into dual ativacao of cagrilintide in amylin and calcitonin receptors. Acta Pharmacologica Sinica, 47(1), 162-172, 2026.
PubMedWang Y, Feng Z, Yu L. The next frontier in metabolic health: Cagrilintide-Semaglutide e o(a) evolving landscape of therapies. The Innovation Medicine, 3(3), 100150, 2025.
PubMedFletcher MM, et al. AM833 Is a Novel Agonist of Calcitonin Family G Protein-Coupled Receptors: Pharmacological Comparison with Six Selective and Nonselective Agonists. JPET, 377(3), 417-440, 2021.
PubMedDahl K, et al. NN1213 – A Potent, Long-Acting, and Selective Analog of Human Amylin. Journal of Medicinal Chemistry, 67(14), 11688–11700, 2024.
PubMedBecerril S, Frühbeck G. Cagrilintide plus semaglutide for obesidade management. Lancet, 397(10286), 1687-1689, 2021.
PubMedD'Ascanio AM, et al. Cagrilintide: A Long-Acting Amylin Analog para o(a) Treatment of Obesity. Cardiology in Review, 32(1), 83-90, 2024.
PubMedMikhail N, Wali S. Cagrilintide Combined with Semaglutide: A New Approach for Treatment of Obesity and Type 2 Diabetes. Clinical Trials and Clinical Research, 2(5), 2023.
PubMedHales CM. Expanding the Treat-to-Target Toolbox for Obesity and Diabetes Care. New England Journal of Medicine, 393(7), 712-714, 2025.
PubMedGadde KM, Allison DB. Long-acting amylin analogue for reducao de peso. Lancet, 398(10317), 2132-2134, 2021.
PubMedDehestani B, et al. Amylin como um(a) Future Obesity Treatment. Journal of Obesity & Metabolic Syndrome, 30(4), 320-325, 2021.
PubMedAviso de Uso em Pesquisa
Apenas para Uso em Pesquisa (RUO). Nao destinado ao consumo humano, uso clinico, ou como medicamento, alimento, cosmetico ou dispositivo medico. Este produto nao foi avaliado pelo FDA e e fornecido exclusivamente para pesquisa laboratorial in vitro por profissionais qualificados.
Certificado de Analise
Each lot is independently tested by accredited third-party laboratories (ISO 17025) at 99%+ purity.
Ultimo Relatorio de Laboratorio
Armazenamento e Manuseio
Resumo
Liofilizado: -80°C (2 anos) ou -20°C (1 ano); Reconstituído: -80°C (6 meses) ou -20°C (1 mês); alíquote para prevenir degradação.
Pó Liofilizado
Store at -80°C por até 2 years or -20°C por até 1 year. Keep sealed, away from moisture and light, preferably under inert gas (N₂).
Solução Reconstituída
Store at -80°C por até 6 months or -20°C por até 1 month. Aliquot stock solutions para prevenir freeze-thaw cycles que degrade o peptideo.
Manuseio
White to off-white powder. Purity: ≥95–99.97% by HPLC/UPLC. Identity: LC-MS (~4409.01 Da). Physical stability: Thioflavin T (ThT) assay confirma >40 hours fibril-free under stress conditions.
“Resumo da Pesquisa Pre-clinica Key Preclinical Studies Estudo Modelo Principais Achados Ref Carvas et al.”
