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Art. -Nr.: HY-105077

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Nemifitide

Name: Nemifitide
Brand: MedChemExpress
SKU: HY-105077
Availability: PreOrder

(Synonyms: INN 00835)

Nemifitide (INN 00835) is a 5-HT2A receptor ligand that crosses the blood-brain barrier. Nemifitide is used in research related to major depressive disorder.

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CAS. Nr.: 173240-15-8
Formel: C₃₃H₄₃FN₁₀O₆
Molecular Weight:694.77

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Nemifitide Chemical Structure

CAS. Nr.: 173240-15-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Nemifitide (INN 00835) is a 5-HT2A receptor ligand that crosses the blood-brain barrier. Nemifitide is used in research related to major depressive disorder^[1]^[2]^[3].

IC₅₀ & Target

^[1]^[2]^[3]

5-HT_2A Receptor

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Nemifitide (INN 00835) 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 binds to 5-HT₂A, 5-HT₂C, NPY1, MC4, MC5, and bombesin receptors in cell-free biochemical assays^[2].
Nemifitide 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 (INN 00835) (0.0125-15 mg/kg; i.p.; daily; 14 days) produces antidepressant-like effects in male FSL rats via a U-shaped dose-response curve, with significant increases in forced swim test swimming time observed at doses from 0.025 mg/kg to 0.3 mg/kg and 3.0 mg/kg to 15.0 mg/kg after 14 days of daily intraperitoneal administration^[2].
Nemifitide (0.3 mg/kg; i.p.; daily; 5 days) 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) 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) 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) 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) 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.

Animal Model:

Flinders Sensitive Line (FSL) (male, ~70 days old, 280-320 g, genetic depression model)^[2]
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
Administration:

i.p.; daily; 14 days
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.

Animal Model:

Flinders Sensitive Line (FSL) (male, ~70 days old, 280-320 g, genetic depression model)^[2]
Dosage:

0.3 mg/kg
Administration:

i.p.; daily; 5 days
Result:

Significantly increased swimming time in the forced swim test compared to vehicle-treated FSL rats.

Animal Model:

Flinders Sensitive Line (FSL) (male, ~70 days old, 280-320 g, genetic depression model)^[2]
Dosage:

0.3 mg/kg
Administration:

i.p.; daily; 14 days
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.

Animal Model:

Flinders Resistant Line (FRL) (male, ~70 days old, genetic control strain for depression model)^[2]
Dosage:

0.3 mg/kg
Administration:

i.p.; daily; 14 days
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.

Animal Model:

High DPAT Sensitive (HDS) (male, selectively bred depression model); Low DPAT Sensitive (LDS) (male, selectively bred depression model)^[2]
Dosage:

0.3 mg/kg
Administration:

i.p.; daily; 14 days
Result:

Significantly increased swimming time in both HDS and LDS rats compared to vehicle-treated controls of the same strain.

Animal Model:

Flinders Sensitive Line (FSL) (female, genetic depression model)^[2]
Dosage:

0.3 mg/kg
Administration:

i.p.; daily; 14 days
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

CAS. Nr. 173240-15-8
Molecular Weight 694.77
Formel C₃₃H₄₃FN₁₀O₆
SMILES

C([C@H](CC1=CC=C(F)C=C1)N)(=O)N2[C@H](C(N[C@H](C(NCC(N[C@@H](CC=3C=4C(NC3)=CC=CC4)C(N)=O)=O)=O)CCCNC(=N)N)=O)C[C@@H](O)C2
Synonyms

INN 00835
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[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]

[3]. Feighner JP, et al. Clinical pharmacokinetic studies with INN 00835 (nemifitide), a novel pentapeptide antidepressant. Biopharmaceutics & drug disposition. 2002 Jan;23(1):33-9.

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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MOQ

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100 mg

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