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Cat. No.: HY-178760

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TGF-8027

TGF-8027 is a selective 5-HT_2A receptor agonist with a K_i of 7.4 nM and an EC₅₀ of 3.3 nM at the human receptor. TGF-8027 activates the 5-HT_2A receptor-mediated Gq protein signaling pathway. TGF-8027 induces dose-dependent head-twitch responses in mice.

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

CAS No.: 3136748-24-5
Formula: C₁₉H₂₂N₂O₃
Molecular Weight:326.39

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (282 KB)

TGF-8027 Chemical Structure

CAS No.: 3136748-24-5

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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
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Biological Activity

Description

IC₅₀ & Target

^[1]

5-HT_2A Receptor

7.4 nM (Ki)

5-HT_2A Receptor

3.3 nM (EC₅₀)

All 5-HT Receptor Isoforms :

In Vitro

TGF-8027 (compound 1) (60 minutes at 37°C) is a 5-HT_2A agonist in HEK293T cells with an EC₅₀ of 3.3 nM and 48.5-fold selectivity over 5-HT_2C in the Gq dissociation BRET assay^[1].
TGF-8027 (60 minutes at 37°C) shows 368-fold selectivity for 5-HT_2A over 5-HT_2C VGV in the Gq dissociation BRET assay in HEK293T cells^[1].
TGF-8027 (60 minutes at 37°C) has an EC₅₀ of 14 nM for mouse 5-HT_2A in HEK293T cells and shows reduced selectivity for mouse 5-HT_2C^[1].
TGF-8027 exhibits 85-fold selectivity for 5-HT_2A over 5-HT_2C in calcium flux assays in Flp-In 293 T-Rex cells^[1].
TGF-8027 (60 minutes at 37°C) recruits β-arrestin2 at 5-HT_2A in HEK293T cells with an EC₅₀ of 4.5 nM and an E_max of 108%^[1].
TGF-8027 binds to human 5-HT_2A with an affinity of 7.4 nM and exhibits 149-fold selectivity for 5-HT_2A over 5-HT_2C in a cell-free radioligand binding assay^[1].

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

In Vivo

TGF-8027 (Compound 1) (5 mL/kg; subcutaneous injection; single injection per test; 30-minute recording period) dose-dependently induces 5-HT_2A-mediated head-twitch behavior in mice, with an ED₅₀ of 1.86 mg/kg^[1].

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

Animal Model:

C57BL/6J (male, 6-8 weeks old)^[1]
Dosage:

5 mL/kg
Administration:

s.c.; single injection per test session; 30-minute recording period
Result:

The ED₅₀ was 1.86 mg/kg (95% CI 1.18-2.92).

Chemical Information

CAS No. 3136748-24-5
Molecular Weight 326.39
Formula C₁₉H₂₂N₂O₃
SMILES

COC1=C(CCNC(C)C2=CC=CC=C2O)C=C(OC)C(C#N)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Fenske TG, et al. Discovery of Highly Selective 5-HT Agonists Using Structure-Guided Design. Journal of medicinal chemistry. 2025 Oct 09;68(19):20619-20635. [Content Brief]

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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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100 mg

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