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Cat. No.: HY-119247

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NBI 30545

NBI 30545 is a blood-brain barrier permeable CRF1R antagonist with a K_i 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.

CAS No.: 195054-99-0
Formula: C₂₂H₃₀N₄O₃
Molecular Weight:398.51

Storage:

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

NBI 30545 Chemical Structure

CAS No.: 195054-99-0

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Use of MCE Products

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

Biological Activity
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All CRFR Isoforms :

CRFR1
CRFR2

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	76 nM Compound: 8	Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor	[PMID: 15341493]
Pituitary gland cell	IC₅₀	37 nM Compound: 18n	Inhibition of CRF-stimulated ACTH release in cultured rat anterior pituitary cells Inhibition of CRF-stimulated ACTH release in cultured rat anterior pituitary cells	[PMID: 15203140]
Pituitary gland cell	IC₅₀	76 nM Compound: 18n	Inhibition of CRF-stimulated cAMP production in cultured rat anterior pituitary cells Inhibition of CRF-stimulated cAMP production in cultured rat anterior pituitary cells	[PMID: 15203140]

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. .

Parmacokinetics

Species	Dose	Route	V_d	CL	T_1/2	AUC	Brain-Kp (AUC_last)	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.

Chemical Information

CAS No. 195054-99-0
Molecular Weight 398.51
Formula C₂₂H₃₀N₄O₃
SMILES

N1=C(C=C(N2N=C(C(=C12)C=3C=CC(OC)=CC3OC)C)N(CCOC)CCC)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Chen C, et al. Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility. Bioorg Med Chem Lett. 2004;14(14):3669-3673. [Content Brief]

Calculators

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Dilution Calculator

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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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