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.
| Molecular Weight | 380.53 |
| Formula | C22H32N6 |
| CAS Number | 195055-03-9 |
| Form | Solid |
| Solubility (25°C) | Ethanol 100 mg/mL (ultrasonic) DMSO 6.2 mg/mL (ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related CRFR Products |
|---|
| K41498 TFA
K41498 TFA is an antisauvagine-30 (aSvg-30) analog and a strongly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM, and 425 nM for human CRF2α, CRF2β, and CRF1 receptors, respectively.K41498 TFA inhibits sauvagine-stimulated cAMP accumulation in hCRF2α/hCRF2β expressing cells. K41498 TFA can be used in hypotension studies. |
| Astressin 2B TFA
Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist with IC50 values of 1.3 and > 500 nM for CRF2 and CRF1, respectively. |
| Urocortin, rat
Urocortin, rat (Urocortin (Rattus norvegicus)) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF2α and mouse CRF2β, respectively. |
| Urocortin, human
Urocortin, human, a 40-aa neuropeptide, acts as a selective agonist of endogenous CRF2 receptor, with Kis of 0.4, 0.3, and 0.5 nM for hCRF1, rCRF2α and mCRF2β, respectively. |
| CRF(6-33)(human)
CRF(6-33)(human) is a CRF binding protein (CRF-BP) ligand inhibitor. |
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