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
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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].

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].

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.
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
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HY-14127
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