2. GPCR/G Protein
  3. CRFR
  4. NBI 30545

NBI 30545 is a blood-brain barrier permeable CRF1R antagonist with a Ki value of 3.4 nM for the human receptor. NBI 30545 inhibits CRF-stimulated intracellular cAMP accumulation and ACTH release. NBI 30545 can be used in the research of depression, anxiety disorders and stress-related diseases.

For research use only. We do not sell to patients.

NBI 30545

NBI 30545 Chemical Structure

CAS No. : 195054-99-0

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NBI 30545 Related Antibodies

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Description

NBI 30545 is a blood-brain barrier permeable CRF1R antagonist with a Ki value of 3.4 nM for the human receptor. NBI 30545 inhibits CRF-stimulated intracellular cAMP accumulation and ACTH release. NBI 30545 can be used in the research of depression, anxiety disorders and stress-related diseases[1].

In Vitro

NBI 30545 inhibits CRF-stimulated cAMP accumulation in cells expressing the human CRF1 receptor with an IC50 of 76 nM[1].
NBI 30545 inhibits CRF-stimulated ACTH release in cultured rat anterior pituitary cells with an IC50 of 37 nM[1].

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

NBI 30545 Related Antibodies
Parmacokinetics
Species Dose Route Vd CL T1/2 AUC Brain-Kp (AUClast) Bioavailability
Rat[1] 10 mg/kg i.v. 4.7 L/kg 43 mL/min/kg 1.1 h / / /
Rat[1] 10 mg/kg p.o. / / / 1182 ng·h/mL 1472 ng/g·h 30.5 %
In Vivo

NBI 30545 (Compound 18n) (10 mg/kg; i.v., p.o.; single dose) achieves good oral plasma and brain exposure in rats with a 30.5% bioavailability and 1.2 brain/plasma ratio, along with extensive tissue distribution and a short half-life after intravenous administration[1].

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

Animal Model: Sprague-Dawley[1]
Dosage: 10 mg/kg (i.v.); 10 mg/kg (p.o.)
Administration: i.v.; single dose; p.o.; single dose
Result: Achieved a volume of distribution of 4.7 L/kg, clearance of 43 mL/min/kg, and a half-life of 1.1 h after intravenous administration.
Reached a plasma AUC of 1182 ng/mL·h, brain AUC of 1472 ng/g·h, oral bioavailability of 30.5%, and a brain/plasma ratio of 1.2 after oral administration.
Molecular Weight

398.51

Formula

C22H30N4O3
CAS No.
SMILES

N1=C(C=C(N2N=C(C(=C12)C=3C=CC(OC)=CC3OC)C)N(CCOC)CCC)C
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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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NBI 30545 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:

NBI 30545195054-99-0NBI30545NBI-30545CRFRCorticotropin-releasing Factor ReceptorCRHRstress related disordersACTH releasecorticotropin-releasing factor-1 (CRF1) receptordepressionanxietycloned human CRF1 receptorintracellular cAMP accumulationrat anterior pituitary cellsInhibitorinhibitorinhibit

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