Size | Price | Stock | Qty |
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1mg |
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5mg |
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Other Sizes |
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Targets |
EC50 (for human): 5.79 (GCGR), 0.0643 (GIPR), 0.775 nM (GLP-1R) [1]. EC50 (for mouse): 2.32 (GCGR), 0.191 (GIPR), 0.794 nM (GLP-1R) [1]. Ki (for human): 5.6 (GCGR), 0.057 (GIPR), 7.2 nM (GLP-1R) [1]. Ki (for mouse): 73 (GCGR), 2.8 (GIPR), 1.3 nM (GLP-1R)[1].
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ln Vitro |
Retatrutide (LY3437943) has EC50 values of 5.79, 0.0643, and 0.775 nM, respectively, against human GCGR, GIPR, and GLP-1R. Retatrutide exhibits activity against mouse GCGR, GIPR, and GLP-1R, as evidenced by its respective EC50 values of 2.32, 0.191, and 0.794 nM[1]. Retatrutide exhibits binding affinities of 5.6, 0.057, and 7.2 nM for human GCGR, GIPR, and GLP-1R, respectively [1]. Retatrutide exhibits binding affinities of 73, 2.8, and 1.3 nM for mouse GCGR, GIPR, and GLP-1R, respectively [1].
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ln Vivo |
Through GIP or GLP-1 receptors, rectatrutide (LY3437943) (subcutaneous injection; 0.47 mg/kg; single dosage) enhances glucose tolerance in ipGTT and takes part in GCGR in vivo[1]. By activating the glucagon receptor, retatrutide (subcutaneous injection; 10 mL/kg; every 3 days; for 21 days) significantly reduces body weight and increases energy expenditure[1]. Retatrutide is acceptable and safe[1].
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Animal Protocol |
Animal/Disease Models: Male CD-1 mice[1]
Doses: 0.47 mg/kg Route of Administration: subcutaneous (sc) administration, single Experimental Results: AUClast, ng*h/mL AUC0-∞, ng*h/mL Cmax, ng/mL Tmax, h t1 /2, h CLF, mL/h/kg 41135 41905 1680 12 21 11.22. Animal/Disease Models: Diet-induced obese (DIO) male C57/BL6 black mouse (24-25 weeks, 40-51 g)[1] Doses: 10 mL /kg Route of Administration: subcutaneous (sc) injection, cycle every 3 days, for 21 days Experimental Results: diminished body weight and improved glycemic control. |
References |
[1]. Tamer Coskun, et al. LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept. Cell Metab. 2022 Sep 6;34(9):1234-1247.e9.
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Molecular Formula |
C221H342N46O68
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Molecular Weight |
4731.33
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CAS # |
2381089-83-2
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Related CAS # |
Retatrutide TFA;Retatrutide acetate
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
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) |
DMSO: 50 mg/mL (10.57 mM)
H2O: 33.33 mg/mL (7.04 mM) |
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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 | 0.2114 mL | 1.0568 mL | 2.1136 mL | |
5 mM | 0.0423 mL | 0.2114 mL | 0.4227 mL | |
10 mM | 0.0211 mL | 0.1057 mL | 0.2114 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.