2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. TGF-8027

TGF-8027 is a selective 5-HT2A agonist that can cross the blood-brain barrier. TGF-8027 exhibits EC50s of 3.3 nM, 160 nM and 7600 nM against human 5-HT2A, 5-HT2C and 5-HT2B and exhibits EC50s against mouse 5-HT2A and mouse 5-HT2C of 14 and 210 nM. TGF-8027 can induce a head-shaking response in mice. TGF-8027 can be used to study diseases that target the 5-HT2A receptor (such as depression).

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TGF-8027

TGF-8027 Chemical Structure

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TGF-8027 Related Antibodies

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Description

TGF-8027 is a selective 5-HT2A agonist that can cross the blood-brain barrier. TGF-8027 exhibits EC50s of 3.3 nM, 160 nM and 7600 nM against human 5-HT2A, 5-HT2C and 5-HT2B and exhibits EC50s against mouse 5-HT2A and mouse 5-HT2C of 14 and 210 nM. TGF-8027 can induce a head-shaking response in mice. TGF-8027 can be used to study diseases that target the 5-HT2A receptor (such as depression)[1].

IC50 & Target[1]

5-HT2A Receptor

3.3 nM (EC50)

5-HT2C Receptor

160 nM (EC50)

5-HT2B Receptor

7600 nM (EC50)

In Vivo

TGF-8027 (0.4-40 mg/kg, s.c., single dose) induces a head-shaking response in mice in a dose-dependent manner with an EC50 of 1.86 mg/kg[1].

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

Animal Model: Head-twitch response (HTR) model established in C57BL/6J mice[1]
Dosage: 0.4, 1.33, 4, 13.33 and 40 mg/kg
Administration: Subcutaneous injection (s.c.), single dose
Result: Induced a head-shaking response in mice in a dose-dependent manner.
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
References
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TGF-8027 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TGF-8027TGF8027TGF 80275-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2A receptorstructure-based drug designselective agonisthead-twitch response (HTR)Inhibitorinhibitorinhibit

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