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Tirzepatide Acetate(2023788-19-2 free base)

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Catalog No. TP1111L

Tirzepatide (LY3298176) Acetate (2023788-19-2 free base) is a new molecule that can control blood glucose levels by combining dual agonism of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors.[3]

Tirzepatide Acetate(2023788-19-2 free base)

Tirzepatide Acetate(2023788-19-2 free base)

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Purity: 98.05%
Catalog No. TP1111L
Tirzepatide (LY3298176) Acetate (2023788-19-2 free base) is a new molecule that can control blood glucose levels by combining dual agonism of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors.[3]
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$358In StockIn Stock
5 mg$798In StockIn Stock
10 mg$1,180In StockIn Stock
25 mg$1,680In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.05%
Color:White
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Product Introduction

Bioactivity
Description
Tirzepatide (LY3298176) Acetate (2023788-19-2 free base) is a new molecule that can control blood glucose levels by combining dual agonism of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors.[3]
Targets&IC50
GLP1 receptor:0.934 nM (EC50), GIPR:0.0224 nM (EC50)
In vitro
METHODS: Tirzepatide (LY3298176) (1, 3, 10, 30 nM) was used to treat GIPR or GLP-1R receptors, and Tirzepatide (30 μM, 30 nM) was used to treat cells expressing recombinant GIPR or GLP-1R to investigate whether it is effective on both GIPR and GLP-1R.
RESULTS In receptor binding studies, LY3298176 had high affinity to either receptor (GIPR Ki = 0.135, SEM = 0.020 nM; GLP-1R Ki = 4.23, SEM = 0.23 nM); for GIPR, the affinity was comparable to that of native GIP, while for GLP-1R, the affinity was approximately 5-fold weaker than that of native GLP-1. In signaling studies using the same HER2 receptors, LY3298176 potently stimulated cAMP accumulation at either receptor (GIPR EC50 = 0.0224, SEM = 0.0053 nM; GLP-1R EC50 = 0.934, SEM = 0.068 nM).[1]
METHODS: Representative confocal images of Tirzepatide (LY3298176)-induced receptor internalization and EGFP fluorescence in HA-GIPR-EGFP cells treated with Tirzepatide (LY3298176) (100 nM).
RESULTS Tirzepatide (LY3298176) was weak in inducing internalization, resulting in a maximal effect of only 40% of that observed with GLP-1. Treatment with Tirzepatide (LY3298176) resulted in minimal reduction in cell surface labeling and only a slight increase in punctate localization of the receptor in the cytoplasmic/perinuclear region. [2]
In vivo
METHODS: Tirzepatide (LY3298176) (30nmol/kg,i.p) was used to evaluate in vivo glycemic control using an intraperitoneal glucose tolerance test (ipGTT) in normal and receptor-deficient mice.
RESULTS Tirzepatide (LY3298176) enhanced insulin secretion in three pancreatic islet genotypes. Tirzepatide (LY3298176) can induce glucose-dependent insulin secretion in vivo through GIPR or GLP-1R and improve glucose tolerance in mice. [1]
Chemical Properties
Molecular Weight4873.5
FormulaC227H352N48O70
SmilesC[C@H]([C@@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NC(C)(C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(NCC(N1CCC[C@H]1C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(N2CCC[C@H]2C(N3CCC[C@H]3C(N4CCC[C@H]4C(N[C@H](C(N)=O)CO)=O)=O)=O)=O)C)=O)=O)CO)=O)CO)=O)=O)=O)=O)C)=O)[C@H](CC)C)=O)CC(C)C)=O)CC5=CNC6=C5C=CC=C6)=O)CCC(N)=O)=O)C(C)C)=O)CC7=CC=CC=C7)=O)C)=O)CCCCNC(COCCOCCNC(COCCOCCNC(CC[C@H](C(O)=O)NC(CCCCCCCCCCCCCCCCCCC(O)=O)=O)=O)=O)=O)=O)CCC(N)=O)=O)C)=O)[C@H](CC)C)=O)CCCCN)=O)CC(O)=O)=O)CC(C)C)=O)C)=O)[C@H](CC)C)=O)CO)=O)CC8=CC=C(O)C=C8)=O)CC(O)=O)=O)CO)=O)[C@H](O)C)=O)CC9=CC=CC=C9)=O)NC(CNC([C@@H](NC(C(C)(NC([C@H](CC%10=CC=C(O)C=C%10)N)=O)C)=O)CCC(O)=O)=O)=O)O.CC(O)=O
Relative Density.no data available
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 245 mg/mL (50.27 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM0.2052 mL1.0260 mL2.0519 mL10.2596 mL
5 mM0.0410 mL0.2052 mL0.4104 mL2.0519 mL
10 mM0.0205 mL0.1026 mL0.2052 mL1.0260 mL
20 mM0.0103 mL0.0513 mL0.1026 mL0.5130 mL
50 mM0.0041 mL0.0205 mL0.0410 mL0.2052 mL

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