1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. 5-HT3 antagonist 5

5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice.

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5-HT3 antagonist 5 Chemical Structure

5-HT3 antagonist 5 Chemical Structure

CAS No. : 901599-43-7

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 143 In-stock
Solution
10 mM * 1 mL in DMSO USD 143 In-stock
Solid
5 mg USD 130 In-stock
10 mg USD 200 In-stock
25 mg USD 400 In-stock
50 mg USD 650 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice[1].

IC50 & Target

5-HT3 Receptor

 

In Vitro

5-HT3 antagonist 5 (compound 4c) exhibits 5-HT3 receptor antagonisms in longitudinal muscle myenteric plexus preparation from guinea pig ileum against 5-HT3 agonist, 2-methyl-5-HT, with pA2 value of 5[1].

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

In Vivo

5-HT3 antagonist 5 (compound 4c) (1 mg/kg; i.p.; single dose) decreases the duration of immobility and shows anti-depressant effect in FST mice[1].

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

Animal Model: Swiss albino mice (23 ± 2 g)[1]
Dosage: 1 mg/kg
Administration: Intraperitoneal injection; single dose; locomotor scores tested 10 min after administration
Result: Reduced the duration of immobility as compared to the vehicle-treated (control) group.
Showed no effect on the locomotion of mice as observed in spontaneous locomotor activity.
Molecular Weight

279.29

Formula

C16H13N3O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=NC2=CC=CC=C2N=C1)NC3=CC=C(C=C3)OC

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 : 20.83 mg/mL (74.58 mM; ultrasonic and warming 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 3.5805 mL 17.9025 mL 35.8051 mL
5 mM 0.7161 mL 3.5805 mL 7.1610 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.

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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 3.5805 mL 17.9025 mL 35.8051 mL 89.5127 mL
5 mM 0.7161 mL 3.5805 mL 7.1610 mL 17.9025 mL
10 mM 0.3581 mL 1.7903 mL 3.5805 mL 8.9513 mL
15 mM 0.2387 mL 1.1935 mL 2.3870 mL 5.9675 mL
20 mM 0.1790 mL 0.8951 mL 1.7903 mL 4.4756 mL
25 mM 0.1432 mL 0.7161 mL 1.4322 mL 3.5805 mL
30 mM 0.1194 mL 0.5968 mL 1.1935 mL 2.9838 mL
40 mM 0.0895 mL 0.4476 mL 0.8951 mL 2.2378 mL
50 mM 0.0716 mL 0.3581 mL 0.7161 mL 1.7903 mL
60 mM 0.0597 mL 0.2984 mL 0.5968 mL 1.4919 mL
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  • 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-HT3 antagonist 5
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