2. GPCR/G Protein
  3. CRFR
  4. Verucerfont

Verucerfont  (Synonyms: GSK561679)

Cat. No.: HY-14875 Purity: 99.51%
COA Handling Instructions

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Verucerfont is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000 nM for CRF1, CRF2, and CRF-BP, respectively.

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

Verucerfont Chemical Structure

Verucerfont Chemical Structure

CAS No. : 885220-61-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 187 In-stock
Solution
10 mM * 1 mL in DMSO USD 187 In-stock
Solid
5 mg USD 170 In-stock
10 mg USD 280 In-stock
50 mg USD 770 In-stock
100 mg USD 1080 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Verucerfont Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

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Description

Verucerfont is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000 nM for CRF1, CRF2, and CRF-BP, respectively.

IC50 & Target

IC50: 6.1 nM (CRF1), >1000 nM (CRF2), >1000 nM (CRF-BP)[1]
In Vivo

Post hoc analysis shows that the prototypic non-peptide CRF1 receptor antagonist NBI30775 (R121919) and Verucerfont are both significantly different from vehicle, CP-316 311, and pexacerfont (P<0.001 for all comparisons collapse across time-points); the latter three treatments in turn do not differ from each other. A differential effect of treatments over time is also shown by a significant treatment×time interaction (F[20,140]=6.4, P<0.001). Accordingly, detailed Post hoc analysis shows that both NBI30775 and Verucerfont inhibit ACTH release throughout the following 6 h of measurement (P<0.001 vs vehicle at each time-point, and vs the respective pretreatment baseline)[1].

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

406.48

Formula

C22H26N6O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC[C@H](NC1=CC(C)=NC2=C(C3=CC=C(OC)C=C3C)C(C)=NN12)C4=NC(C)=NO4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (205.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4601 mL 12.3007 mL 24.6015 mL
5 mM 0.4920 mL 2.4601 mL 4.9203 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.51%

COA (256 KB) HNMR (266 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1]

Male Sprague-Dawley rats are received at 175 to 200 g and housed in a 12 to 12 light cycle for 1 week before adrenalectomy. Rats are adrenalectomized at Neurocrine Biosciences, and NaCl is replenished. Adrenalectomy is verified by plasma corticosterone measurements. Seven days after adrenalectomy, rats are implanted with femoral vein catheters. After ~4 days, rats are prepared for blood sampling by attaching their catheters to PE50 tubing and a syringe, and acclimated to individual opaque sampling cages for 1 h. These cages allow sampling to occur without disturbance to the rat. Blood samples (0.3 mL) are taken after acclimation and blood volumes are replaced with 5 U/mL heparinized saline. Blood samples are stored on ice with EDTA. After a baseline blood sample, rats receive oral doses of either vehicle at 5 mL/kg or the respective drug (including Verucerfont) in the same volume of vehicle. In each case, the dose is 10 mg/kg, based on prior pharmacokinetic studies showing that this dose results in adequate and comparable exposure. Blood samples are taken 1, 2, 3, 4, and 6 h later. Plasma is separated by centrifugation at 4°C and stored at -80 °C for subsequent measurement of ACTH by radioimmunoassay[1].

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4601 mL 12.3007 mL 24.6015 mL 61.5036 mL
5 mM 0.4920 mL 2.4601 mL 4.9203 mL 12.3007 mL
10 mM 0.2460 mL 1.2301 mL 2.4601 mL 6.1504 mL
15 mM 0.1640 mL 0.8200 mL 1.6401 mL 4.1002 mL
20 mM 0.1230 mL 0.6150 mL 1.2301 mL 3.0752 mL
25 mM 0.0984 mL 0.4920 mL 0.9841 mL 2.4601 mL
30 mM 0.0820 mL 0.4100 mL 0.8200 mL 2.0501 mL
40 mM 0.0615 mL 0.3075 mL 0.6150 mL 1.5376 mL
50 mM 0.0492 mL 0.2460 mL 0.4920 mL 1.2301 mL
60 mM 0.0410 mL 0.2050 mL 0.4100 mL 1.0251 mL
80 mM 0.0308 mL 0.1538 mL 0.3075 mL 0.7688 mL
100 mM 0.0246 mL 0.1230 mL 0.2460 mL 0.6150 mL
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Verucerfont Related Classifications

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:

Verucerfont885220-61-1GSK561679GSK 561679GSK-561679CRFRCorticotropin-releasing Factor ReceptorCRHRInhibitorinhibitorinhibit

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