5-HT2A antagonist 2
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 98.90%
- CAS No.: 2641482-08-6
- Formula: C30H33ClN4O2
- Molecular Weight:517.06
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All 5-HT Receptor Isoforms
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Biological Activity
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5-HT2A Receptor |
5-HT2A Receptor 14 nM (IC50) |
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.
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Animal Model:HFD-fed C57BL6/J mice[1]
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Dosage:5-10 mg/kg
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Administration:p.o., daily for 12 weeks
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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.
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Animal Model:choline-deficient, L-amino acid-defined high-fat diet (CDAHFD) fed C57BL6/J mice[1]
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Dosage:5-10 mg/kg
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Administration:p.o., daily for 12 weeks
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Result:Decreased mRNA expressions of ol1a1 and α-SMA, decreased collagen accumulation and expressions of α-SMA, TNF-α, and IL-1β .
Chemical Information
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CAS No. 2641482-08-6
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Appearance Solid
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Molecular Weight 517.06
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Formula C30H33ClN4O2
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Color Off-white to light yellow
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SMILES
CC1=C(CCN2CC/C(CC2)=C3C(C=CC(Cl)=C4)=C4CCC5=CC=CN=C5\3)C(N(CCCC6O)C6=N1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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 |
5-HT2A antagonist 2 Related Classifications
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