2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 5-HT2A antagonist 2

5HT2A antagonist 2 is an orally active, selective antagonist for 5HT2A with IC50 of 14 nM. 5-HT2A antagonist 2 exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1.

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5-HT2A antagonist 2

5-HT2A antagonist 2 Chemical Structure

CAS No. : 2641482-08-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

5-HT2A antagonist 2 Related Antibodies

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Description

5HT2A antagonist 2 is an orally active, selective antagonist for 5HT2A with IC50 of 14 nM. 5-HT2A antagonist 2 exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1[1].

IC50 & Target

5-HT2A Receptor

 

5-HT2A Receptor

14 nM (IC50)

In Vivo

5-HT2A antagonist 2 (5-10 mg/kg, p.o., daily for 12 weeks) protects against the HFD-induced MASLD in C57BL6J mice[1].
5-HT2A antagonist 2 (5-10 mg/kg, p.o., daily for 12 weeks) inhibits liver fibrosis and inflammation in CDAHFD fed C57BL6/J mice[1].
5-HT2A antagonist 2 exhibits pharmacokinetic profils in rat and in dog[1]:

Pharmacokinetic Analysis of 5-HT2A antagonist 2 in rat and dog[1]

species route Dose (mg/kg) T1/2 (h) AUC (μg·h/mL) CL (L/h/kg) V (L/kg) F (%)
rat iv 5 4.4 1.55 2.82 8.86 -
dog iv 5 8.6 16.79 0.42 4.36 -
dog po 5 1.02 19.11 - - 73

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

Animal Model: HFD-fed C57BL6/J mice[1]
Dosage: 5-10 mg/kg
Administration: p.o., daily for 12 weeks
Result: Reduced fat mass and weight of liver and inguinal white adipose tissue (iWAT), improved glucose tolerance.
Reduced steatosis, lobular inflammation, and hepatocyte ballooning in liver tissue.
Animal Model: choline-deficient, L-amino acid-defined high-fat diet (CDAHFD) fed C57BL6/J mice[1]
Dosage: 5-10 mg/kg
Administration: p.o., daily for 12 weeks
Result: Decreased mRNA expressions of ol1a1 and α-SMA, decreased collagen accumulation and expressions of α-SMA, TNF-α, and IL-1β .
Molecular Weight

517.06

Formula

C30H33ClN4O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=C(CCN2CC/C(CC2)=C3C(C=CC(Cl)=C4)=C4CCC5=CC=CN=C5\3)C(N(CCCC6O)C6=N1)=O
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 : 25 mg/mL (48.35 mM; Need ultrasonic; 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 1.9340 mL 9.6701 mL 19.3401 mL
5 mM 0.3868 mL 1.9340 mL 3.8680 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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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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V2

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

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g

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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 1.9340 mL 9.6701 mL 19.3401 mL 48.3503 mL
5 mM 0.3868 mL 1.9340 mL 3.8680 mL 9.6701 mL
10 mM 0.1934 mL 0.9670 mL 1.9340 mL 4.8350 mL
15 mM 0.1289 mL 0.6447 mL 1.2893 mL 3.2234 mL
20 mM 0.0967 mL 0.4835 mL 0.9670 mL 2.4175 mL
25 mM 0.0774 mL 0.3868 mL 0.7736 mL 1.9340 mL
30 mM 0.0645 mL 0.3223 mL 0.6447 mL 1.6117 mL
40 mM 0.0484 mL 0.2418 mL 0.4835 mL 1.2088 mL
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5-HT2A antagonist 2 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.

Keywords:

5-HT2A antagonist 22641482-08-65-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorMetabolic Dysfunction-Associated Steatotic Liver DiseaseMASLDMetabolic Dysfunction-Associated SteatohepatitisMASHInhibitorinhibitorinhibit

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