Nemifitide diTFA
Based on 1 Customer Validation
Nemifitide diTFA (INN 00835 diTFA) is a 5-HT2A receptor ligand that crosses the blood-brain barrier. Nemifitide diTFA is used in research related to major depressive disorder.
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- Pureté: 98.24%
- CAS No.: 204992-09-6
- Formule: C37H45F7N10O10
- Masse moléculaire:922.80
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Stockage:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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5-HT2A Receptor |
In Vitro
Nemifitide diTFA (INN 00835 diTFA) and its active metabolite (M1) bind to 5-HT2A, 5-HT2C, melanocortin MC4, MC5, and bombesin receptors at micromolar concentrations in cell-free biochemical assays[1].
Nemifitide diTFA binds to 5-HT2A, 5-HT2C, NPY1, MC4, MC5, and bombesin receptors in cell-free biochemical assays[2].
Nemifitide diTFA undergoes extensive metabolism in rat and human intestinal and liver enzyme preparations in vitro[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Nemifitide (0.3 mg/kg; i.p.; daily; 5 days) diTFA produces a rapid-onset antidepressant-like effect in male FSL rats, significantly increasing forced swim test swimming time after just 5 days of daily intraperitoneal administration of 0.3 mg/kg[2].
Nemifitide (0.3 mg/kg; i.p.; daily; 14 days) diTFA produces prolonged antidepressant-like effects in male FSL rats, with significantly increased forced swim test swimming time persisting for at least 5 days after cessation of 14 days of daily intraperitoneal administration of 0.3 mg/kg[2].
Nemifitide (0.3 mg/kg; i.p.; daily; 14 days) diTFA does not produce antidepressant-like effects in male FRL control rats, as 14 days of daily intraperitoneal administration of 0.3 mg/kg does not significantly increase forced swim test swimming time[2].
Nemifitide (0.3 mg/kg; i.p.; daily; 14 days) diTFA produces antidepressant-like effects in male HDS and LDS rats, significantly increasing forced swim test swimming time after 14 days of daily intraperitoneal administration of 0.3 mg/kg[2].
Nemifitide (0.3 mg/kg; i.p.; daily; 14 days) diTFA produces antidepressant-like effects in female FSL rats, significantly increasing forced swim test swimming time after 14 days of daily intraperitoneal administration of 0.3 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Flinders Sensitive Line (FSL) (male, ~70 days old, 280-320 g, genetic depression model)[2]
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Dosage:0.0125 mg/kg; 0.025 mg/kg; 0.05 mg/kg; 0.1 mg/kg; 0.2 mg/kg; 0.3 mg/kg; 0.4 mg/kg; 0.6 mg/kg; 0.8 mg/kg; 1.2 mg/kg; 2.4 mg/kg; 3.0 mg/kg; 4.0 mg/kg; 5.0 mg/kg; 15.0 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Significantly increased swimming time in the forced swim test at doses 0.025 mg/kg, 0.05 mg/kg, 0.1 mg/kg, 0.2 mg/kg, 0.3 mg/kg, 3.0 mg/kg, 4.0 mg/kg, 5.0 mg/kg, and 15.0 mg/kg.
Did not significantly increase swimming time at doses 0.4 mg/kg, 0.6 mg/kg, 0.8 mg/kg, and 1.2 mg/kg.
Produced intermediate effects at 0.0125 mg/kg and 2.4 mg/kg, with swimming time significantly higher than vehicle-treated FSL rats but significantly lower than untreated FRL control rats.
Identified 0.3 mg/kg as the most effective dose.
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Animal Model:Flinders Sensitive Line (FSL) (male, ~70 days old, 280-320 g, genetic depression model)[2]
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Dosage:0.3 mg/kg
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Administration:i.p.; daily; 5 days
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Result:Significantly increased swimming time in the forced swim test compared to vehicle-treated FSL rats.
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Animal Model:Flinders Sensitive Line (FSL) (male, ~70 days old, 280-320 g, genetic depression model)[2]
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Dosage:0.3 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Significantly increased swimming time 22-24 hours after the final dose.
Maintained the effect 5 days after treatment cessation, with treated rats swimming significantly more than vehicle-treated rats at the 5-day follow-up.
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Animal Model:Flinders Resistant Line (FRL) (male, ~70 days old, genetic control strain for depression model)[2]
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Dosage:0.3 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Did not significantly increase swimming time in FRL rats; treated rats swam an average of 199.8 seconds, which did not differ from untreated FRL controls.
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Animal Model:High DPAT Sensitive (HDS) (male, selectively bred depression model); Low DPAT Sensitive (LDS) (male, selectively bred depression model)[2]
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Dosage:0.3 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Significantly increased swimming time in both HDS and LDS rats compared to vehicle-treated controls of the same strain.
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Animal Model:Flinders Sensitive Line (FSL) (female, genetic depression model)[2]
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Dosage:0.3 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Significantly increased swimming time in female FSL rats; treated rats swam an average of 428 seconds, compared to 288.9 seconds in vehicle-treated female FSL rats.
Chemical Information
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CAS No. 204992-09-6
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Appearance Solid
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Masse moléculaire 922.80
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Formule C37H45F7N10O10
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Color White to off-white
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Synonyms
INN 00835 diTFA
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Sequence
{Fluoro-Phe}-{Hyp}-Arg-Gly-Trp-NH2
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Sequence Shortening
{Fluoro-Phe}-{Hyp}-RGW-NH2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
In Vitro:
H2O : 250 mg/mL (270.91 mM; Need ultrasonic)
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (292 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Montgomery SA, et al. Efficacy and safety of 30 mg/d and 45 mg/d nemifitide compared to placebo in major depressive disorder. The international journal of neuropsychopharmacology. 2006 Oct;9(5):517-28. [Content Brief]
[2]. Overstreet DH, et al. Antidepressant-like effects of a novel pentapeptide, nemifitide, in an animal model of depression. Psychopharmacology. 2004 Sep;175(3):303-9. [Content Brief]
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 (sealed storage, away from moisture and light). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.0837 mL | 5.4183 mL | 10.8366 mL | 27.0915 mL |
| 5 mM | 0.2167 mL | 1.0837 mL | 2.1673 mL | 5.4183 mL | |
| 10 mM | 0.1084 mL | 0.5418 mL | 1.0837 mL | 2.7091 mL | |
| 15 mM | 0.0722 mL | 0.3612 mL | 0.7224 mL | 1.8061 mL | |
| 20 mM | 0.0542 mL | 0.2709 mL | 0.5418 mL | 1.3546 mL | |
| 25 mM | 0.0433 mL | 0.2167 mL | 0.4335 mL | 1.0837 mL | |
| 30 mM | 0.0361 mL | 0.1806 mL | 0.3612 mL | 0.9030 mL | |
| 40 mM | 0.0271 mL | 0.1355 mL | 0.2709 mL | 0.6773 mL | |
| 50 mM | 0.0217 mL | 0.1084 mL | 0.2167 mL | 0.5418 mL | |
| 60 mM | 0.0181 mL | 0.0903 mL | 0.1806 mL | 0.4515 mL | |
| 80 mM | 0.0135 mL | 0.0677 mL | 0.1355 mL | 0.3386 mL | |
| 100 mM | 0.0108 mL | 0.0542 mL | 0.1084 mL | 0.2709 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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