Tirzepatide
$56.00 – $287.00Price range: $56.00 through $287.00
With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
Questions
Tirzepatide Common Questions
What’s pIC50?
pIC50 is the negative log of the IC50 value when converted to molar.That is, pIC50=-log(IC50).
What’s Kd?
Dissociation consent (Kd) reflects the affinity of a compound for its target. In some cases, it can be equivalent to Ki.
Product Introduction
Bioactivity
Description
Tirzepatide (LY-3298176) is a dual agonist of glucose-dependent polypeptide (GIP) (EC50=0.042 nM) and glucagon-like peptide-1 (GLP-1) (EC50=0.086 nM) receptors, and it has neuroprotective activity. It can improve blood pressure and lower low-density lipoprotein (LDL) cholesterol and triglycerides, and can be used to study diabetes and obesity.
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 vitro
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
Chemical Properties
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-{C20 diacid-gamma-Glu-(Ala-Glu-Glu-Ala)2-Lys}-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2
Sequence Short
Y-{Aib}-EGTFTSDYSI-{Aib}-LDKIAQ-{C20 diacid-gamma-Glu-(AEEA)2-Lys}-AFVQWLIAGGPSSGAPPPS
Storage & Solubility Information
Storage
Formula
Solution Preparation Table
DMSO
|
1mg |
5mg |
10mg |
50mg |
|
|---|---|---|---|---|
|
1 mM |
0.2078 mL |
1.0388 mL |
2.0775 mL |
10.3876 mL |
|
5 mM |
0.0416 mL |
0.2078 mL |
0.4155 mL |
2.0775 mL |
|
10 mM |
0.0208 mL |
0.1039 mL |
0.2078 mL |
1.0388 mL |
|
20 mM |
0.0104 mL |
0.0519 mL |
0.1039 mL |
0.5194 mL |
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.
References
- 1. Fontanella RA, et al. Tirzepatide prevents neurodegeneration through multiple molecular pathways. J Transl Med. 2024 Jan 29;22(1):114.
- 2. Weimin K, et al. Tirzepatide as an innovative treatment strategy in a pre-clinical model of obesity-driven endometrial cancer. Gynecologic Oncology. 2024;191:116-123.
- 3. Guo X, et al. Tirzepatide ameliorates spatial learning and memory impairment through modulation of aberrant insulin resistance and inflammation response in diabetic rats. Front Pharmacol. 2023 Aug 28;14:1146960.
