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Cat. No.: HY-14128

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NBI-34041

(Synonyms: SB-723620)

NBI-34041 (SB-723620) is a selective and orally active nonpeptide CRF1 receptor antagonist with an IC₅₀ of 58.9 nM and a K_i of 4.0 nM for human CRF1 receptor. NBI-34041 has no inhibitory effect on the CRF2 receptor. NBI-34041 can be used for depression and anxiety disorders research.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No.: 268545-87-5
Formule: C₂₂H₂₆Cl₂N₄
Masse moléculaire:417.37

Stockage:

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

Data Sheet (273 KB)

NBI-34041 Chemical Structure

CAS No.: 268545-87-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

CRFR1

58.9 nM (IC₅₀)

CRFR1

4 nM (Ki)

CRFR2

>10000 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform CRFR :

CRFR1
CRFR2

In Vitro

NBI-34041 could inhibit the production of cAMP in a concentration-dependent manner with an IC₅₀ of approximately 60 nM. At concentrations of NBI-34041 up to 10 000 nM, NBI-34041 is unable to fully inhibit sauvagine stimulated cAMP from cells expressing the human CRF2 receptor^[1].

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

In Vivo

NBI-34041 (3-30 mg/kg; oral gavage; a single dose) significantly attenuates the elevation in plasma ACTH induced by CRF. NBI-34041 also demonstrates efficacy in attenuating shock-induced ACTH release in a dose-dependent manner^[1].

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

Animal Model:

Male Wistar or Sprague-Dawley rats (300-350 g)^[1]
Dosage:

3 mg/kg, 10 mg/kg, or 30 mg/kg
Administration:

Oral gavage; a single dose
Result:

Did not impair diurnal adrenocorticotropic hormone (ACTH) and cortisol secretion or CRF evoked ACTH and cortisol responses but attenuated the neuroendocrine response to psychosocial stress.

Chemical Information

CAS No. 268545-87-5
Masse moléculaire 417.37
Formule C₂₂H₂₆Cl₂N₄
SMILES

CC1=NC2=C3C(N(C(CCC)CCC)CCN3N=C2C4=CC=C(Cl)C=C4Cl)=C1
Synonyms

SB-723620
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Marcus Ising, et al. High-affinity CRF1 receptor antagonist NBI-34041: preclinical and clinical data suggest safety and efficacy in attenuating elevated stress response. Neuropsychopharmacology. 2007 Sep;32(9):1941-9. [Content Brief]

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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.

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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NBI-34041

Voir tous les produits spécifiques à Isoform CRFR

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

NBI-34041 Related Classifications

HY-14128 Related Classifications