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  4. 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.

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CRF1 receptor antagonist-2

CRF1 receptor antagonist-2 Chemical Structure

CAS No. : 441060-02-2

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CRF1 receptor antagonist-2 Related Antibodies

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Description

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[1].

IC50 & Target[1]

CRFR1

 

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.

CRF1 receptor antagonist-2 Related Antibodies
Parmacokinetics
Species Dose Route AUC0-∞ T1/2 CLtotal Vss Tmax Cmax 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.
Molecular Weight

398.93

Formula

C22H27ClN4O
CAS No.
SMILES

ClC1=C(C2=C3N=C4C(CCC4)=C(N3N=C2C)NC(CC)CC)C=CC(OC)=C1
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Purity & Documentation
References
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CRF1 receptor antagonist-2 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:

CRF1 receptor antagonist-2441060-02-2CRFRCorticotropin-releasing Factor ReceptorCRHRrat CRF1 receptor-expressing cellsanxiolytic effectsswim stress-loaded ratsCRF1 receptorcAMPrat brain membranesCHO-K1 cellhuman CRF1 receptor-expressing CHO-K1 cellsstress-induced anxietyInhibitorinhibitorinhibit

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