Cat. No.: HY-P1731CP

Tirzepatide (crude)

Tirzepatide (LY3298176) (crude) is the crude form of Tirzepatide (HY-P1731).Tirzepatide (LY3298176) is a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. Tirzepatide exerts anti-apoptotic and pro-differentiation effects via the pAkt/CREB/BDNF cascade and miRNA in neurons; in the heart, it promotes BCAA catabolism and inhibits the mTOR pathway by mediating the dephosphorylation of BCKDHA; meanwhile, it effectively reduces insulin and leptin levels and suppresses inflammatory responses at the systemic level. Tirzepatide can be used for research on myocardial infarction, colon cancer, diabetes, diabetic cognitive impairment, neurodegeneration, diabetes-related neuropathy, and obesity.

For research use only. We do not sell to patients.

CAS No.: 2023788-19-2
Formula: C₂₂₅H₃₄₈N₄₈O₆₈
Molecular Weight:4813.45

Storage:

Sealed storage, away from moisture.

Powder -80°C, 2 years , -20°C, 1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Custom Peptide Synthesis

Tirzepatide (crude) Chemical Structure

CAS No.: 2023788-19-2

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

GLP-1

mTOR

All mTOR Isoforms :

In Vitro

Tirzepatide (LY3298176) (0.2 μM; 7 days) sodium has no effect on the proliferation of human neuroblastoma SHSY5Y cells exposed to normoglycemic or hyperglycemic conditions, and upregulates the expression of nerve growth markers, differentiation markers, and glucose transporters^[2].
Tirzepatide (0.2 μM; 7 days) sodium reverses high glucose-induced apoptosis and significantly reduces the BAX/Bcl-2 protein ratio in SH-SY5Y cells^[2].
Tirzepatide (35-100 nM; 96 h) sodium exerts no direct effect on the proliferation of MC38 mouse colon cancer cells in vitro^[3].
Tirzepatide sodium binds to BCKDHA, a key enzyme in branched-chain amino acid (BCAA) catabolism^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:

human neuroblastoma SHSY5Y cells (exposed to normal glucose (25 mM) or high glucose (150 mM))
Concentration:

0.2 μM
Incubation Time:

7 days
Result:

Did not alter Ki-67 median fluorescence compared to untreated high glucose cells.
Had no significant effect on Ki-67 median fluorescence in normal glucose-exposed cells.

Western Blot Analysis^[2]

Cell Line:

human neuroblastoma SHSY5Y cells (exposed to normal glucose (25 mM) or high glucose (150 mM))
Concentration:

0.2 μM
Incubation Time:

7 days
Result:

Increased p-Akt protein levels (and p-Akt/AKT ratio), MAP2 protein levels, GAP43 protein level, and AGBL4 protein levels in normal glucose-exposed cells.
Prevented the high glucose-induced downregulation of p-Akt, MAP2, and GAP43 protein levels.

Real Time qPCR^[2]

Cell Line:

human neuroblastoma SHSY5Y cells (exposed to normal glucose (25 mM) or high glucose (150 mM))
Concentration:

0.2 μM
Incubation Time:

7 days
Result:

Decreased miR-34a expression and increased miR-212 and miR-29c expression in normal glucose-exposed cells.
Reversed the high glucose-induced increase in miR-34a expression and reversed the high glucose-induced decrease in miR-212 and miR-29c expression in high glucose-exposed cells.
prevented the high glucose-induced downregulation of MAP2 and GAP43 mRNA expression in high glucose-exposed cells.
Did not affect AGBL4 mRNA or protein levels in high glucose-exposed cells.

Cell Proliferation Assay^[3]

Cell Line:

MC38 murine colorectal cancer cells
Concentration:

35, 70, 100 nM
Incubation Time:

96 h
Result:

Did not significantly alter proliferation rate of MC38 cells after 96 hours of incubation, as measured by cell number counts.

In Vivo

Tirzepatide (LY3298176) (1.35 mg/kg; i.p.; once weekly; for 15 weeks) sodium improves spatial learning and memory impairment, inhibits hippocampal Aβ aggregation, and alleviates neuroinflammation in diabetic rat models induced by a high-fat diet (HF diet) combined with STZ (HY-13753)^[1].
Tirzepatide sodium (1.35 mg/kg; i.p.; once weekly; for 15 weeks) induces mild metabolic and molecular changes in healthy rats without impairing spatial learning or memory abilities^[1].
Tirzepatide sodium (10 nM/kg; s.c.; once daily; for 28 days) significantly reduces body weight, food intake, serum insulin and leptin levels, and indirectly inhibits tumor growth in a diet-induced obese (DIO) MC38 colon cancer mouse model^[3].
Tirzepatide sodium (10 nM/kg; s.c.; once daily; for 14 days) significantly reduces body weight, food intake, serum insulin and leptin levels in diet-induced obese mouse models^[3].
Tirzepatide sodium (10 nM/kg/day; i.p.; once daily; for 14 consecutive days) exerts protective effects in a mouse model of myocardial infarction (MI) induced by coronary artery ligation, including reducing mortality, decreasing myocardial infarction size, promoting branched-chain amino acid (BCAA) catabolism, and facilitating early fibrotic repair^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Sprague Dawley (male, 7-8 weeks old, 180-200 g, high-fat diet + streptozotocin injection)^[1]
Dosage:

1.35 mg/kg
Administration:

i.p.; once weekly; 8 weeks
Result:

Significantly reduced fasting blood glucose and insulin levels.
Shortened escape latency and increased time spent in the target quadrant in the Morris water maze.
Decreased Aβ40 production and neuronal loss in the hippocampus.
Inhibited the mRNA expression of TNF-α, IL-6, IL-1β, and the phosphorylation of NF-κB.

Animal Model:

Sprague Dawley (male, 7-8 weeks old, 180-200 g, normal diet-fed)^[1]
Dosage:

1.35 mg/kg
Administration:

i.p.; once weekly; 8 weeks
Result:

Induced a slight reduction in fasting blood glucose levels.
Slightly increased body weight.
Did not alter swimming speed in Morris water maze testing.
Caused minor reductions in hippocampal APP and BACE1 levels.
Had no significant effect on hippocampal Aβ40 levels or neuron density.
Slightly increased hippocampal PSD95 and SYT1 expression.
Increased density of stubby, mushroom-like, long, and filopodia-like dendritic spines.
Slightly reduced hippocampal mRNA levels of TNF-α, IL-6, and IL-1β.
Decreased phosphorylated NF-κB-positive cell percentage and phosphorylated IKKα levels.
Increased hippocampal p-IRS-1-S307, p-PI3K, p-AKT, p-GSK3β, and GSK3β levels.

Animal Model:

C57BL/6 (male; diet-induced obesity via high-fat diet feeding)^[3]
Dosage:

10 nM/kg
Administration:

s.c.; once daily; 14 days
Result:

Reduced body weight relative to vehicle controls.
Reduced circulating glucose, insulin, leptin, and c-peptide levels in both fed and fasted states.
Eliminated the positive correlation between body weight and serum insulin levels seen in vehicle-treated controls.

Animal Model:

C57BL/6 (male; diet-induced obesity via high-fat diet feeding; subcutaneous allograft of MC38 colon cancer cells)^[3]
Dosage:

10 nM/kg
Administration:

s.c.; once daily; 28 days
Result:

Caused a significant decrease in food intake and body weight.
Lowered glucose, insulin, leptin, and c-peptide levels in both fed and fasted states.
Significantly reduced MC38 tumor volume compared to the control group.

Animal Model:

C57BL/6J wild-type (12-week-old male/female; myocardial infarction model via permanent left descending coronary artery ligation or concurrent low-BCAA diet intervention)^[4]
Dosage:

10 nM/kg/day
Administration:

i.p.; once daily; 14 days (starting day 1 post-MI)
Result:

Significantly improved long-term survival and reduced the incidence of cardiac rupture.
Decreased myocardial infarct size and improved left ventricular systolic function (increased LVEF).
Bound to BCKDHA and reduced its S293 phosphorylation, enhancing enzyme activity to promote cardiac BCAA catabolism and inhibit abnormal mTOR pathway activation.

Chemical Information

CAS No. 2023788-19-2
Appearance Solid
Molecular Weight 4813.45
Formula C₂₂₅H₃₄₈N₄₈O₆₈
Sequence

Tyr-{Aib}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{Aib}-Leu-Asp-Lys-Ile-Ala-Gln-{C20 diacid-gamma-Glu-(AEEA)2-Lys}-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2
Sequence Shortening

Y-{Aib}-EGTFTSDYSI-{Aib}-LDKIAQ-{C20 diacid-gamma-Glu-(AEEA)2-Lys}-AFVQWLIAGGPSSGAPPPS-NH2
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Guo X, et al. Tirzepatide ameliorates spatial learning and memory impairment through modulation of aberrant insulin resistance and inflammation response in diabetic rats. Frontiers in pharmacology. 2023;14:1146960. [Content Brief]

[2]. Fontanella RA, et al. Tirzepatide prevents neurodegeneration through multiple molecular pathways. Journal of translational medicine. 2024 Jan 29;22(1):114. [Content Brief]

[3]. Huang, L., et al. Tirzepatide inhibits tumor growth in mice with diet-induced obesity. bioRxiv, 2023-06.

[4]. Chen M, et al. Glucose-dependent insulinotropic polypeptide/glucagon-like peptide 1 receptor agonist tirzepatide promotes branched chain amino acid catabolism to prevent myocardial infarction in non-diabetic mice. Cardiovascular research. 2025 Apr 29;121(3):454-467. [Content Brief]

[5]. Hoffmann K, et al. The efficacy and safety of dual GIP/GLP1 receptor agonists (tirzepatide) in diabetes and obesity: a systematic review and network meta-analysis. Expert opinion on drug safety. 2026 Jun;25(6):1031-1046.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Tirzepatide (crude)

All mTOR Isoforms