1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. 5-HT4 antagonist 1

5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6.

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

5-HT4 antagonist 1 Chemical Structure

5-HT4 antagonist 1 Chemical Structure

CAS No. : 261766-73-8

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Based on 1 publication(s) in Google Scholar

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Description

5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6.

IC50 & Target

5-HT4 Receptor

9.6 (pKi)

In Vitro

5-HT4 antagonist 1 (compound 6b) is a 5-HT4 receptor antagonist with a pKi of 9.6.

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

In Vivo

5-HT4 antagonist 1 (compound 6b) demonstrates good exposure and prolongs t1/2 in other species, including the mouse (t1/2 7 h), rat (t1/2 12 h) and mini-pig (t1/2 21 h). In Phase I clinical trial, it is found that 5-HT4 antagonist 1 has good oral bioavailability with a steady state plasma t1/2 of >100 h[1].

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

Molecular Weight

480.62

Formula

C23H36N4O5S

CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

O=C(C1=C2OCCOC2=CC=C1)NCC3CCN(CCCS(=O)(N4CCN(C)CC4)=O)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (41.61 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0806 mL 10.4032 mL 20.8065 mL
5 mM 0.4161 mL 2.0806 mL 4.1613 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0806 mL 10.4032 mL 20.8065 mL 52.0161 mL
5 mM 0.4161 mL 2.0806 mL 4.1613 mL 10.4032 mL
10 mM 0.2081 mL 1.0403 mL 2.0806 mL 5.2016 mL
15 mM 0.1387 mL 0.6935 mL 1.3871 mL 3.4677 mL
20 mM 0.1040 mL 0.5202 mL 1.0403 mL 2.6008 mL
25 mM 0.0832 mL 0.4161 mL 0.8323 mL 2.0806 mL
30 mM 0.0694 mL 0.3468 mL 0.6935 mL 1.7339 mL
40 mM 0.0520 mL 0.2601 mL 0.5202 mL 1.3004 mL
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5-HT4 antagonist 1 Related Classifications

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.

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5-HT4 antagonist 1
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HY-100170
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