1. GPCR/G Protein
  2. CRFR
  3. R121919

R121919 (Synonyms: NBI30775)

Cat. No.: HY-14127 Purity: 99.84%
Handling Instructions

R121919 (NBI30775) is a potent small-molecule CRF1 receptor antagonist with a Ki of 2 to 5 nM for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types.

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

R121919 Chemical Structure

R121919 Chemical Structure

CAS No. : 195055-03-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 221 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 264 In-stock
Estimated Time of Arrival: December 31
10 mg USD 420 In-stock
Estimated Time of Arrival: December 31
25 mg USD 840 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

R121919 (NBI30775) is a potent small-molecule CRF1 receptor antagonist with a Ki of 2 to 5 nM for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types[1].

IC50 & Target

Ki: 2 to 5 nM (CRF1)[1]

In Vitro

R121919 is a potent small-molecule CRF1 receptor antagonistwith high affinity for the CRF1 receptor (Ki=2–5 nM) and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types[1].

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

In Vivo

R121919 dose dependently decreases adrenocorticopin hormone and corticosterone responses to restraint stress in rats. Peak plasma adrenocorticopin hormone and corticosterone concentrations at a dose of 10 mg/kg R121919 are 9 and 25%, respectively[1]. R121919 reduces levels of anxiety in mice with a steep dose-response curve. Molecules such as GR, MR, BAG-1 and AP-1 have been identified as some of the drug's intracellular targets[2].

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

Molecular Weight

380.53

Formula

C₂₂H₃₂N₆

CAS No.

195055-03-9

SMILES

CCCN(C1=CC(C)=NC2=C(C3=CN=C(N(C)C)C=C3C)C(C)=NN21)CCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

Ethanol : 100 mg/mL (262.79 mM; Need ultrasonic)

DMSO : 6.2 mg/mL (16.29 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6279 mL 13.1396 mL 26.2791 mL
5 mM 0.5256 mL 2.6279 mL 5.2558 mL
10 mM 0.2628 mL 1.3140 mL 2.6279 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.57 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% EtOH    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1][2]

Rats: For the restraint stress,R121919 is dissolved in an aqueous 70% (v/v) polyethylene glycol 400 solution, and serially diluted in this vehicle to the appropriate concentrations. The drug is injected i.v. in a volume of 1 mL/kg to Male Sprague-Dawley rats. For the defensive withdrawal experiments, R121919 solutions are made fresh the night before each experiment. R121919 is dissolved in a vehicle consisting of 5% (v/v) polyethoxylated castor oil[1].

Mice: R121919 is dissolved in an aqueous. The drug is administered orally (1 mL/100 g bodyweight) via a feeding tube to six to ten mice per group; the doses applied are 0.5, 1.0 and 5.0 mg/kg for the DBA/2NCRL mice and 1.0, 5.0, and 30 mg/kg for the DBA/2Ola strain; an additional (vehicle) group of mice receives water, while a further group of mice (untreated controls) are spared the aforementioned manipulations[2].

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

References
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Keywords:

R121919NBI30775R 121919R-121919NBI 30775NBI-30775CRFRCorticotropin-releasing Factor ReceptorInhibitorinhibitorinhibit

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R121919
Cat. No.:
HY-14127
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