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 Chemical Structure

5-HT2A antagonist 2 Chemical Structure

CAS No. : 2641482-08-6

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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

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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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5-HT2A antagonist 2 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:

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

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