Survodutide TFA |
Catalog No.GC72223
One-Click Copy Product Info
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Survodutide TFA 는 CHO-K1 세포에서 EC50s가 각각 0.52 nM과 0.33 nM인 강력한 선택적 인슐린 수용체/GLP-1R 이중 흥분제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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The EC50 is 0.36 nM for Survodutide (BI 456906) TFA in the endogenous mouse GLP-1R in the insulinoma cell line MIN6, and the EC50 is 60 pM for GLP-1. In 0.5% human and mouse plasma, Survodutide TFA shows a similar potency to that of endogenous GLP-1. For the GCGR, in 0.5% human and mouse plasma, Survodutide TFA is 6-fold less potent (0.29 and 0.17 nM, respectively) in relation to endogenous glucagon (47 and 30 pM, respectively)[1].
Proteolytic stability of Survodutide TFA is helped by C-terminal amidation and the introduction of a non-coded amino acid 1-aminocyclobutane-1-carboxylic acid (Ac4c) in position 2, well established as the site of proteolytic activity for dipeptidyl peptidase-4. The desired extended terminal half-life of Survodutide TFA is achieved by the introduction of a glycine–serine linker in position 24, carrying a C18 di-acid[1].
Survodutide (BI 456906; 3, 10, 20, 30 nmol/kg; SC; daily; 30 days) TFA achieves a greater bodyweight-lowering efficacy in diet-induced obese mice compared with maximally effective doses of Semaglutide . Survodutide TFA dose-dependently reduces plasma glucagon[1].
Survodutide (1, 3, 10, 30, 100 nmol/kg; SC; single dose) TFA dose-dependently reducesacute food intake in WT but not in GLP-1R KO mice (Three-week-old, male, lean NMRI outbred mice)[1].
Survodutide (1, 3, 10, 30, 100 nmol/kg; SC; single dose) TFA engages the glucagon receptor in vivo upon single dosing, increases liver nicotinamide N-methyltransferase mRNA, and reduces plasma serine and glutamine[1].
Survodutide (SC injection) TFA causes mean residence times of 44 and 140 h and Tmax values of 7 and 51 h obtained in mice and dogs, respectively[1].
Pharmacokinetic Parameters of Survodutide (BI 456906) in mice and dogs[1].
| Mice (20 nmol/kg; SC) | Dogs (10 nmol/kg; SC) | |
| Tmax (h) | 7 | 50.7 |
| Cmax (nM) | 84.9 | 62.0 |
| AUC0-∞ (nM∗h) | 4640 | 9540 |
References:
[1]. Tina Zimmermann, et al. BI 456906: Discovery and preclinical pharmacology of a novel GCGR/GLP-1R dual agonist with robust anti-obesity efficacy. Mol Metab. 2022 Dec:66:101633.
| Cas No. | SDF | ||
| Formula | C192H289N47O61.xC2HF3OC2 | M.Wt | 4231.62 (free base) |
| Solubility | H2O : ≥ 100 mg/mL | Storage | Sealed storage, away from moisture and light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 236.3 μL | 1.1816 mL | 2.3632 mL |
| 5 mM | 47.3 μL | 236.3 μL | 472.6 μL |
| 10 mM | 23.6 μL | 118.2 μL | 236.3 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)