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Cat. No.: HY-182645

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CRF1 receptor antagonist-2

CRF1 receptor antagonist-2 is an orally active, blood-brain barrier permeable CRF1 receptor antagonist, with an IC₅₀ of 4 nM in CHO-K1 cell membranes and an IC₅₀ of 7 nM in rat brain cell membranes. CRF1 receptor antagonist-2 exerts anxiolytic effects in swim stress-loaded rats. CRF1 receptor antagonist-2 can be used in studies related to stress-induced anxiety.

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

CAS No.: 441060-02-2
Formula: C₂₂H₂₇ClN₄O
Molecular Weight:398.93

Storage:

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

CRF1 receptor antagonist-2 Chemical Structure

CAS No.: 441060-02-2

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

CRFR1

All CRFR Isoforms :

CRFR1
CRFR2

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	EC₅₀	40 nM Compound: 7b	Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay	[PMID: 21865047]

In Vitro

CRF1 receptor antagonist-2 (Compound 7b) (1-10000 nM; 2 h) potently inhibits the binding of human CRF1 receptor, with an IC₅₀ of 4 nM in CHO-K1 cell membranes^[1].
CRF1 receptor antagonist-2 (1-10000 nM; 2 h) potently inhibits the binding of rat CRF1 receptors, with an IC₅₀ of 7 nM in rat brain cell membranes^[1].
CRF1 receptor antagonist-2 (1-10000 nM; 15 min) potently inhibits CRF-stimulated cAMP production in CHO-K1 cells expressing the human CRF1 receptor, with an EC₅₀ value of 40 nM^[1].
CRF1 receptor antagonist-2 (1-10000 nM; 15 min) potently inhibits CRF1 receptor-stimulated cAMP production in cells expressing rat CRF1 receptors, with an EC₅₀ of 40 nM^[1].

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

Parmacokinetics

Species	Dose	Route	AUC_0-∞	T_1/2	CL_total	V_ss	T_max	C_max	Bioavailability
Rat^[1]	0.3 mg/kg	i.v.	278 ng·h/mL	4.7 h	18 mL/min/kg	1780 mL/kg	/	/	/
Rat^[1]	3 mg/kg	p.o.	608 ng·h/mL	7.8 h	/	/	1.0 h	87.1 ng/mL	22 %

In Vivo

CRF1 receptor antagonist-2 (3-10 mg/kg; p.o.; single dose) significantly increases time spent in open arms in swim stress-loaded rats, demonstrating anxiolytic efficacy^[1].

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

Animal Model:

Sprague-Dawley (male, 230-280 g, forced swim stress-induced anxiety model)^[1]
Dosage:

1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:

p.o.; single dose
Result:

Failed to produce a statistically significant effect on time spent in open arms at 1 mg/kg compared to vehicle.
Increased mean time spent in open arms to ~31 seconds at 3 mg/kg compared to vehicle .
Increased mean time spent in open arms to ~30 seconds at 10 mg/kg compared to vehicle.

Chemical Information

CAS No. 441060-02-2
Molecular Weight 398.93
Formula C₂₂H₂₇ClN₄O
SMILES

ClC1=C(C2=C3N=C4C(CCC4)=C(N3N=C2C)NC(CC)CC)C=CC(OC)=C1
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]. Saito T, et al. 6,7-Dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidines and their derivatives as novel corticotropin-releasing factor 1 receptor antagonists. Bioorg Med Chem. 2011 Sep 15;19(18):5432-45. [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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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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CRF1 receptor antagonist-2

All CRFR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

CRF1 receptor antagonist-2 Related Classifications

HY-182645 Related Classifications