Eloralintide
Based on 1 Customer Validation
Eloralintide (LY-3841136) is an amylin receptor agonist with human AMY1R EC50 23.9 pM and human AMY3R EC50 253.8 pM. Eloralintide induces decreased appetite, reduced food intake, body weight and fat mass loss, prolonged plasma calcium2+ reduction, and weak conditioned taste avoidance. Eloralintide can be used for the research of obesity.
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- Pureté : 99.97%
- CAS No.: 2883634-40-8
- Formule: C201H319N49O65S2
- Masse moléculaire:4526.10
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Stockage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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NN1213 acetateAmylin Receptor Agonist -
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Activité biologique
Description
In Vitro
Eloralintide acts as an agonist of both rat and human amylin receptors (AMYRs) and calcitonin receptors (CTRs)[2].
Eloralintide selectively activates human AMY1R (EC50 = 23.9 pM) with 11- to 12-fold greater potency than human AMY3R and CTR, and acts as a full agonist at all three human receptors[3].
Eloralintide binds human AMY1R (Ki = 478.1 pM) with 8-fold greater affinity than human AMY3R and CTR[3].
Eloralintide selectively activates rat AMY1R (EC50 = 5.4 pM) with 3-fold greater potency than rat AMY3R and 45-fold greater potency than rat CTR, and acts as a full agonist at all three rat receptors[3].
Eloralintide binds rat AMY1R (Ki = 48.1 pM) with 3-fold greater affinity than rat AMY3R and 109-fold greater affinity than rat CTR[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Eloralintide (0.1-100 nmol/kg; s.c.; Q3D; 13-15 days) dose-dependently reduces food intake and body weight in diet-induced obese male Long Evans rats, primarily via fat mass loss, with an ED50 of 0.8 nmol/kg for fat mass loss[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Long Evans (male, diet-induced obese)[3]
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Dosage:0.1 nmol/kg; 0.3 nmol/kg; 1 nmol/kg; 3 nmol/kg; 10 nmol/kg; 30 nmol/kg; 100 nmol/kg (13 days); 1 nmol/kg; 10 nmol/kg; 100 nmol/kg (15 days)
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Administration:s.c.; Q3D; 13 days; 15 days
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Result:Induced dose-proportional reductions in food intake and body weight.
Reduced mean body weight by -12.3% from baseline at day 13 post-dose at 100 nmol/kg Q3D.
Caused fat mass to account for 85%, 77%, and 68% of total body weight loss at doses of 10, 30, and 100 nmol/kg Q3D, respectively.
Achieved an ED50 of 0.8 nmol/kg for fat mass loss, which was significantly lower than that of cagrilintide.
Reduced mean body weight by -11.0% from baseline at day 15 post-dose at 100 nmol/kg Q3D in head-to-head study, with fat mass accounting for 80% of total body weight loss.
Caused significantly less lean mass loss than cagrilintide at 100 nmol/kg Q3D.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2883634-40-8
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Appearance Solid
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Masse moléculaire 4526.10
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Formule C201H319N49O65S2
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Color White to off-white
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Synonyms
LY-3841136
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Sequence
{γGlu}-Cys-Asn-Thr-Ala-Thr-Cys-Ala-Thr-Gly-{Orn}-Leu-Ala-Glu-{(α-Me-Phe)}-Leu-Val-Arg-Ser-Ser-Asn-{(N-Me-Asn)}-Phe-Gly-Pro-{Lys(γGlu-γGlu-C20 diacid)}-Leu-Pro-Pro-Thr-Glu-Val-Gly-Ser-Asn-Thr-Tyr-NH2 (Methylene bridge: Cys2-Cys7)
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Sequence Shortening
{γGlu}-CNTATCATG-{Orn}-LAE-{(α-Me-Phe)}-LVRSSN-{(N-Me-Asn)}-FGP-{Lys(γGlu-γGlu-C20 diacid)}-LPPTEVGSNTY-NH2 (Methylene bridge: Cys2-Cys7)
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (22.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (0.55 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (0.55 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Pureté et documentation
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Fiche technique (300 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Bhattachar S, et al. Eloralintide, a selective, long-acting amylin receptor agonist for treatment of obesity: Phase 1 proof of concept. Diabetes Obes Metab. Published online January 20, 2026. [Content Brief]
[3]. Briere DA, et al. Eloralintide (LY3841136), a novel amylin receptor agonist for the treatment of obesity: From discovery to clinical proof of concept. Mol Metab. 2025 Dec;102:102271. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.2209 mL | 1.1047 mL | 2.2094 mL | 5.5235 mL |
| 5 mM | 0.0442 mL | 0.2209 mL | 0.4419 mL | 1.1047 mL | |
| 10 mM | 0.0221 mL | 0.1105 mL | 0.2209 mL | 0.5524 mL | |
| 15 mM | 0.0147 mL | 0.0736 mL | 0.1473 mL | 0.3682 mL | |
| 20 mM | 0.0110 mL | 0.0552 mL | 0.1105 mL | 0.2762 mL |
Eloralintide Related Classifications
HY-P10798 Related Classifications
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