Survodutide TFA
Based on 1 Customer Validation
Survodutide (BI 456906) TFA is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide TFA, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide TFA has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake.
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- Pureté: 99.39%
- Formule: C192H289N47O61·xC2HF3OC2
- Masse moléculaire:4231.62 (free base)
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Stockage:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL6/J mice pre-fed with a 60% HFD (22 weeks)[1]
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Dosage:3, 10, 20, 30 nmol/kg
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Administration:SC; daily; 30 days
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Result:Dose-dependently reduced bodyweight from baseline by up to 32% at Day 28 at a dose of 30 nmol/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Appearance Solid
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Masse moléculaire 4231.62 (free base)
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Formule C192H289N47O61·xC2HF3OC2
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Color White to off-white
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Synonyms
BI 456906 TFA
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Sequence
His-{1-Aminocyclobutanecarboxylic acid}-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Lys-Tyr-Leu-Asp-Glu-Arg-Ala-Ala-Lys-Asp-Phe-Ile-{Lys(Gly-Gly-Ser-Gly-Ser-Gly-γGlu-C18 diacid)}-Trp-Leu-Glu-Ser-Ala-NH2
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Sequence Shortening
H-{1-Aminocyclobutanecarboxylic acid}-QGTFTSDYSKYLDERAAKDFI-{Lys(GGSGSG-γGlu-C18 diacid)}-WLESA-NH2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
DMSO : ≥ 100 mg/mL
H2O : ≥ 100 mg/mL
* "≥" means soluble, but saturation unknown.
Pureté et documentation
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Fiche technique (295 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Survodutide TFA Related Classifications
HY-P4146A Related Classifications
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