| Size | Price | Stock | Qty |
|---|---|---|---|
| 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-1)[1].
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| ln Vitro |
Retatrutide (LY3437943) TFA has EC50 values of 5.79, 0.0643, and 0.775 nM, respectively, against human GCGR, GIPR, and GLP-1R[1]. Retatrutide TFA has EC50 values of 2.32, 0.191, and 0.794 nM, respectively, against mouse GCGR, GIPR, and GLP-1R[1]. Retatrutide TFA exhibits binding affinities of 5.6, 0.057, and 7.2 nM for human GCGR, GIPR, and GLP-1R, respectively [1]. Retatrutide TFA 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 |
Retatrutide (LY3437943) TFA (subcutaneous injection; 0.47 mg/kg; single dose) enhances glucose tolerance in ipGTT by binding to GIP or GLP-1 receptors and taking part in GCGR in vivo [1]. Retatrutide TFA (subcutaneous injection; 10 mL/kg; every 3 days; for 21 days) activates the glucagon receptor, which results in a marked decrease in body weight and an increase in energy expenditure [1]. It is acceptable and safe to use retirutide TFA [1].
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| 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 |
C223H343F3N46O70
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|---|---|
| Molecular Weight |
4845.35
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| Related CAS # |
Retatrutide;2381089-83-2;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, 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) |
DMSO :≥ 100 mg/mL (~20.64 mM)
H2O :~20 mg/mL (~4.13 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (0.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.25 mg/mL (0.26 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (0.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2064 mL | 1.0319 mL | 2.0638 mL | |
| 5 mM | 0.0413 mL | 0.2064 mL | 0.4128 mL | |
| 10 mM | 0.0206 mL | 0.1032 mL | 0.2064 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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