2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. EGIS-7625

EGIS-7625 is an orally active and selective competitive antagonist of 5-HT2B receptor, with a human Ki value of 1 nM. EGIS-7625 shows low affinity for 5-HT2A and 5-HT2C receptors. The pKi values of EGIS-7625 for human 5-HT2B, 5-HT2A and 5-HT2C are 9.0, 6.2 and 7.7, respectively. EGIS-7625 alleviates mCPP-induced hypoactivity.

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EGIS-7625

EGIS-7625 Chemical Structure

CAS No. : 755040-97-2

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Other Forms of EGIS-7625:

EGIS-7625 Related Antibodies

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Description

EGIS-7625 is an orally active and selective competitive antagonist of 5-HT2B receptor, with a human Ki value of 1 nM. EGIS-7625 shows low affinity for 5-HT2A and 5-HT2C receptors. The pKi values of EGIS-7625 for human 5-HT2B, 5-HT2A and 5-HT2C are 9.0, 6.2 and 7.7, respectively. EGIS-7625 alleviates mCPP-induced hypoactivity[1].

IC50 & Target[1]

5-HT2A Receptor

 

5-HT2B Receptor

 

5-HT2C Receptor

 

5-HT2B Receptor

9.0 (pKi)

5-HT2A Receptor

6.2 (pKi)

5-HT2C Receptor

7.7 (pKi)

In Vitro

EGIS-7625 (1-10 nM) acts as a potent competitive antagonist of 5-HT2B receptor-mediated contraction in rat fundus strips, with a pA2 value of 9.4[1].
EGIS-7625 (1-30 μM; 30 minutes) acts as a weak competitive antagonist of 5-HT2A receptor-mediated contraction in rabbit pulmonary artery strips, with a pA2 value of 6.7[1].

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

EGIS-7625 Related Antibodies
In Vivo

EGIS-7625 (30 mg/kg; subcutaneous injection; single dose) does not antagonize mCPP-induced 5-HT2C receptor-mediated feeding suppression in rats[1].
EGIS-7625 (3-30 mg/kg; p.o.; single administration) antagonizes mCPP-induced 5-HT2C receptor-mediated hypoactivity in rats at the highest dose of 30.0 mg/kg, while no significant effects are observed at lower doses[1].

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

Animal Model: Wistar (male, 180-240 g) rats[1]
Dosage: 3, 10, 30 mg/kg
Administration: p.o.; single dose
Result: Significantly diminished mCPP-induced hypomotility at 30 mg/kg p.o.
Did not produce a significant effect at 3.0 mg/kg and 10.0 mg/kg p.o.
Molecular Weight

399.31

Formula

C18H24Cl2N4O2
CAS No.
SMILES

NC1=CC(N2CCN(CC3=CC=CC=C3)CC2)=C([N+]([O-])=O)C=C1C.Cl.Cl
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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EGIS-7625 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:

EGIS-7625755040-97-2EGIS7625EGIS 76255-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorcompetitivehypomotilityhypophagiaInhibitorinhibitorinhibit

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