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Cat. No.: HY-123480A

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EGIS-7625 free base

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

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

CAS No.: 751462-86-9
Formula: C₁₈H₂₂N₄O₂
Molecular Weight:326.39

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

EGIS-7625 free base Chemical Structure

CAS No.: 751462-86-9

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Fluorescent Dye

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

Biological Activity
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- In Vitro
- In Vivo
Chemical Information
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Biological Activity

Description

All 5-HT Receptor Isoforms :

In Vitro

EGIS-7625 (1-10 nM) free base 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) free base 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.

In Vivo

EGIS-7625 (30 mg/kg; subcutaneous injection; single dose) free base does not antagonize mCPP-induced 5-HT₂C receptor-mediated feeding suppression in rats^[1].
EGIS-7625 (3-30 mg/kg; p.o.; single administration) free base 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.

Chemical Information

CAS No. 751462-86-9
Appearance Solid
Molecular Weight 326.39
Formula C₁₈H₂₂N₄O₂
SMILES

NC(C=C1N2CCN(CC2)CC3=CC=CC=C3)=C(C)C=C1[N+]([O-])=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Kovács A, et al. Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist. Cardiovasc Drugs Ther. 2003;17(5-6):427-434. [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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Biological Activity
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- In Vivo
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EGIS-7625 free base

All 5-HT Receptor Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

EGIS-7625 free base Related Classifications

HY-123480A Related Classifications