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2mg |
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10mg |
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25mg |
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Purity: ≥98%
Semaglutide TFA (NNC0113-0217; NNC-0113-0217), the trifluoroacetic acid salt form of semaglutide (brand name: Ozempic), is a human glucagon-like peptide-1 (GLP-1) analogue acting as a GLP-1 receptor agonist with longer duration of antidiabetic action. It was being developed clinically to treat type 2 diabetes. The FDA approved semaglutide in December 2017 with the goal of helping adults with type 2 diabetes mellitus achieve better glycemic control. Chemically, semaglutide and glucagon-like peptide-1 (GLP-1) are comparable in humans. The two amino acid substitutions at positions 8 and 34, where arginine and 2-aminoisobutyric acid, respectively, are present, are the only variations. Furthermore, lysine at position 26 is acylated with stearic diacid, indicating that it is in its derivative form. The pharmaceutical product semaglutide was created by Novo Nordisk, a Danish company, and is sold under the brand name Ozempic. It decreases blood sugar by stimulating the synthesis of insulin because it is an agonist of the glucagon-like peptide-1 receptor. It was identified as a longer-acting substitute for liraglutide in 2012 by a group of Novo Nordisk researchers. 2015 saw the beginning of clinical trials, and 2016 saw the completion of phase 3.
Targets |
GLP-1 receptor
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ln Vitro |
Semaglutide is derivatized at lysine 26 and differs from human GLP-1 in two amino acid substitutions (Aib8, Arg34). Semaglutide has an affinity for GLP-1R of 0.38±0.06 nM[1]. A GLP-1 analogue that is 94% sequence similar to human GLP-1 is semaglutide [3].
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ln Vivo |
Semaglutide has an MRT of 63.6 hours after s.c. dosing to mini-pigs and a plasma half-life of 46 hours in mini-pigs after intravenous administration[1]. Motor impairments caused by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) are ameliorated by semaglutide. Semaglutide also protects dopaminergic neurons in the substantia nigra and striatum by rescuing the decrease in tyrosine hydroxylase (TH) levels, reducing lipid peroxidation, alleviating inflammation, inhibiting the apoptosis pathway, and increasing the expression of autophagy-related proteins. Furthermore, semaglutide, a long-acting GLP-1 analogue, outperforms liraglutide in the majority of parameters[2]. Semaglutide reduces body weight and blood glucose by promoting the release of insulin[3].
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Enzyme Assay |
HEK293‐SNAP‐GLP‐1R cells were labelled in suspension with SNAP‐Lumi4‐Tb (40 nM, Cisbio, Codelet, France) for 1 hour at room temperature in complete medium. After washing and resuspension in hanks' balanced salt solution containing 0.1% bovine serum albumin and metabolic inhibitors (20 mmol/L 2‐deoxygucose and 10 mmol/L NaN3) to prevent GLP‐1R internalization, binding experiments were performed by time‐resolved förster resonance energy transfer (FRET) using exendin (9‐39) with fluorescein isothiocyanate (FITC) installed at position K12 as previously described.[4]
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Cell Assay |
Semaglutide activates the GLP-1 receptor in pancreatic beta cells leading to glucose-dependent insulin release. It also decreases glucagon secretion, slows gastric emptying, and promotes satiety.
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Animal Protocol |
Mice: Male C57BL/6 mice 10 weeks old (20-25 g) are used throughout the study. Six groups of mice are randomly assigned (n = 12 per group). The treatments were as follows: (i) saline alone was given to the control group; (ii) NN-2211 group received saline and NN-2211 (25 nmol/kg ip. once daily for 7 days); (iii) Semaglutide group received saline and Semaglutide (25 nmol/kg ip. once daily for 7 days); (iv) MPTP group received MPTP alone (once daily 20 mg/kg ip. for 7 days); (v) MPTP (once daily 20 mg/kg ip. for 7 days) was immediately followed by NN-2211 treated group (25 nmol/kg ip. once daily for 7 days). (vi) MPTP (20 mg/kg i.p. once daily for 7 days), which was immediately followed by the group treated with semaglutide (25 nmol/kg i.p. once daily for 7 days). Measure behavioral changes, neuronal damage, inflammatory markers, and other biomarkers at the conclusion of drug treatments. [2]
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References |
[3]. Semaglutide: First Global Approval. Drugs. 2018 Feb;78(2):275-284. |
Molecular Formula |
C189H292F3N45O61
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Molecular Weight |
4227.66
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Related CAS # |
910463-68-2 (Semaglutide free base); 1997361-85-9 (Semaglutide acetate)
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Sequence |
H-His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly-OH
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SequenceShortening |
HXEGTFTSDV SSYLEGQAAK EFIAWLVRGR G
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Appearance |
White to off-white solid powder
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Synonyms |
NNC 0113-0217 TFA; NNC 0113-0217; NNC-0113-0217; NNC-0113 0217
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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 |
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) |
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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 | 0.2365 mL | 1.1827 mL | 2.3654 mL | |
5 mM | 0.0473 mL | 0.2365 mL | 0.4731 mL | |
10 mM | 0.0237 mL | 0.1183 mL | 0.2365 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.
The composite primary outcome occurred in 108 of 1648 patients (6.6%) in the semaglutide group and 146 of 1649 (8.9%) in the placebo group (hazard ratio, 0.74; 95% confidence interval [CI], 0.58 to 0.95; P<0.001 for noninferiority; P=0.02 for superiority). N Engl J Med . 2016 Nov 10;375(19):1834-1844. td> |
At week 104, among patients receiving semaglutide, the mean glycated hemoglobin level decreased from 8.7% at baseline to 7.6% in the group receiving 0.5 mg and to 7.3% in the group receiving 1.0 mg, for changes of −1.1% and −1.4%, respectively; in the placebo group, the mean level decreased to 8.3% in the two dose groups, for a reduction of 0.4% in each group. N Engl J Med . 2016 Nov 10;375(19):1834-1844. td> |
Gastrointestinal disorders were more frequent in the semaglutide group than in the placebo group (Table 3, and Table S11 in the Supplementary Appendix). N Engl J Med . 2016 Nov 10;375(19):1834-1844. td> |