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| Targets |
NK2
EB1002 selectively targets and activates the neurokinin 2 receptor (NK2R), a G protein-coupled receptor (GPCR) that is widely expressed in the central nervous system (CNS) and peripheral tissues. Activation of NK2R by EB1002 regulates appetite, food intake, and energy expenditure through neuronal signaling. The peripheral effects on metabolic parameters, including enhanced insulin sensitivity and increased mitochondrial activity, originate mainly from peripheral mechanisms. The regulation of food intake is leptin-independent but at least partially MC4R-dependent. EB1002 significantly raises the expression levels of mitochondrial biosynthesis-related genes (such as PGC-1alpha). |
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| ln Vitro |
In vitro, EB1002 is a selective NK2R agonist. The signaling properties are characterized using cells expressing NK2R: EB1002 activates Gq/11-mediated calcium mobilization and Gs-mediated cAMP accumulation. Specific EC₅0 values for receptor activation are in the low nanomolar range. EB1002 is highly selective for NK2R over NK1R and NK3R. It is stable in plasma and shows no significant off-target activity at other GPCRs, ion channels, or transporters.
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| ln Vivo |
In vivo, EB1002 demonstrates robust efficacy in mouse models of obesity and type 2 diabetes. In diet-induced obese (DIO) mice, EB1002 (subcutaneous injection, 325 nmol/kg) significantly reduces food intake, increases oxygen consumption (energy expenditure), reduces body weight, and improves blood glucose levels. The effects on food intake are mediated centrally (via ICV injection), while effects on energy expenditure are mediated peripherally. EB1002 also increases insulin sensitivity and improves glycolipid metabolism. The NK2R antagonist saredutant blocks the effects of EB1002, confirming target selectivity. EB1002 shows promise as a novel treatment for obesity and T2D.
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| Enzyme Assay |
The selectivity of EB1002 for NK2R is assessed by cell-based functional assays. CHO or HEK293 cells expressing human NK2R, NK1R, or NK3R are seeded in 96-well plates and treated with varying concentrations (0.001-1000 nM) of EB1002. NK2R activation is measured by calcium mobilization (using Fluo-4 AM) or cAMP accumulation (using HTRF). The EC₅0 for NK2R is calculated, and the fold selectivity over NK1R and NK3R is determined (EC₅0 ratio). The selectivity for NK2R is high, with >100-fold selectivity over NK1R and NK3R.
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| Cell Assay |
For functional assays in vitro, HEK293 cells expressing NK2R are seeded in 96-well plates (2×10⁴ cells/well) and loaded with Fluo-4 AM (2-5 uM) for 30-60 min. EB1002 (0.001-1000 nM) is added, and calcium flux is measured by a fluorescence plate reader (λex 485 nm, λem 516 nm). The EC₅0 is calculated. For cAMP accumulation, cells are treated with EB1002 (0.01-1000 nM) for 15-30 min, and intracellular cAMP is measured by HTRF or ELISA. For PGC-1alpha expression, primary hepatocytes or adipocytes are treated with EB1002 (0.1-100 nM) for 6-24 h, and PGC-1alpha mRNA is measured by qRT-PCR.
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| Animal Protocol |
In vivo efficacy is evaluated in diet-induced obese (DIO) mice. Male C57BL/6J mice are fed a high-fat diet (60% kcal from fat) for 12-16 weeks to induce obesity and insulin resistance. EB1002 is formulated in 10% DMSO, 40% PEG300, 5% Tween 80, and 45% saline or in 0.5% methylcellulose. EB1002 (100-1000 nmol/kg) is administered subcutaneously (SC) once daily for 2-4 weeks. Body weight and food intake are measured daily. An oral glucose tolerance test (OGTT, 2 g/kg glucose, PO) is performed at week 2 or 4. Blood glucose is measured at 0, 15, 30, 60, 90, 120 min. Insulin levels are measured by ELISA. Oxygen consumption (VO2), carbon dioxide production (VCO2), and respiratory exchange ratio (RER) are measured by indirect calorimetry (CLAMS). For acute studies, EB1002 is administered SC, and energy expenditure is measured for 24 h. For central vs. peripheral mechanism studies, EB1002 is administered by intracerebroventricular (ICV) injection (low dose, 1-10 pmol) or SC injection. The NK2R antagonist saredutant (1-10 mg/kg, SC) is administered 30 min before EB1002 to confirm target selectivity.
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| ADME/Pharmacokinetics |
No specific PK data for EB1002 is available. As a peptide, it has a limited half-life (< 2 h) but is described as a “long-acting” NK2R agonist, suggesting that it has been optimized for stability. For research use, EB1002 is stored as a lyophilized powder at -20degC (powder: -20degC for 3 years, 4degC for 2 years; in solvent: -80degC for 1 year, -20degC for 6 months). It is soluble in water (≥ 50 mg/mL) and DMSO (≥ 50 mg/mL). In vivo formulations are prepared as 10% DMSO, 40% PEG300, 5% Tween 80, and 45% saline for injection.
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| Toxicity/Toxicokinetics |
No specific toxicology data for EB1002 is available. In DIO mouse studies at effective doses (up to 1000 nmol/kg, SC), EB1002 was well-tolerated with no reported adverse effects. Body weight monitoring showed no signs of toxicity. Standard safety precautions for handling peptides apply: use PPE (gloves, lab coat, safety goggles), work in a fume hood, avoid inhalation and skin contact. Not for human consumption.
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| References | |
| Additional Infomation |
EB1002 (CAS# 2770688-48-5; MW 1537.83) is a research-grade selective NK2R agonist developed for the treatment of obesity and type 2 diabetes. It is not an FDA-approved drug. It is a valuable tool for studying the role of NK2R in energy homeostasis, food intake, and glucose metabolism. For research use only, not for diagnostic or therapeutic applications. Storage: powder at -20degC for 3 years, 4degC for 2 years; in solvent at -80degC for 6 months, -20degC for 1 month.
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| Molecular Formula |
C73H124N12O23
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| Molecular Weight |
1537.83
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| CAS # |
2770688-48-5
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ≥ 50 mg/mL (~32.51 mM)
DMSO : ~50 mg/mL (~32.51 mM; with ultrasonication) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6503 mL | 3.2513 mL | 6.5027 mL | |
| 5 mM | 0.1301 mL | 0.6503 mL | 1.3005 mL | |
| 10 mM | 0.0650 mL | 0.3251 mL | 0.6503 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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