Tamanho : 50mg
Telefone : +1 850 650 7790
Synonyms: LY-3298176
| Description | Tirzepatide (LY3298176) is a long-acting glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor dual agonist. In HEK293 cells, it can effectively stimulate cAMP accumulation, with an EC50 of 0.0224 nM for the GIP receptor (GIPR) and an EC50 of 0.934 nM for the GLP-1 receptor (GLP-1R). |
| Targets & IC50 | ERG current (human):> 300 µM |
| In vitro | METHODS: SHSY5Y cells were treated with Tirzepatide (0-0.4 μM) for 7 days, and the expression level of target proteins was detected by Western Blot method. RESULTS: Tirzepatide upregulates the protein levels of CREB and BDNF, and simultaneously increases the protein levels of Bcl-2, pAkt, MAP2, GAP43, AGBL4, GLUT4, and SORBS1. [1] |
| In vivo | Methods: To investigate the effect of Tirzepatide on obesity, Tirzepatide (10 nmol/kg) was administered subcutaneously to obese mice induced by high-fat diet. Results: Treatment with Tirzepatide reduced body weight in mice and also improved obesity-induced serum adiponectin, leptin, GIP, and C-reactive protein levels. [2] |
| Synonyms | LY-3298176 |
| Molecular Weight | 4813.45 |
| Formula | C225H348N48O68 |
| Cas No. | 2023788-19-2 |
| Smiles | CC[C@H](C)[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](C(=O)O)NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC2=CNC3=CC=CC=C32)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N4CCC[C@H]4C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N5CCC[C@H]5C(=O)N6CCC[C@H]6C(=O)N7CCC[C@H]7C(=O)N[C@@H](CO)C(=O)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)C(C)(C)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](CC8=CC=C(C=C8)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC9=CC=CC=C9)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@H](CC1=CC=C(C=C1)O)N |
| Relative Density. | no data available |
| Sequence | Tyr-{Aib}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{Aib}-Leu-Asp-Lys-Ile-Ala-Gln-{Lys(AEEA-AEEA-γGlu-C20 diacid)}-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH₂ |
| Sequence Short | YXEGTFTSDYSIXLDKIAQEAFVQWLIAGGPSSGAPPPS |
| Storage | Keep away from moisture,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (20.78 mM), Sonication is recommended.  H2O: < 0.5 mg/mL (insoluble) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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