| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
R 121919 hydrochloride targets the CRF1 receptor as a high-affinity antagonist with a Ki of 3.5 nM. By blocking CRF1 receptors, it reduces stress-induced elevations of plasma ACTH. It modulates the hypothalamic-pituitary-adrenal (HPA) axis and stress responses.
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|---|---|
| ln Vitro |
In vitro, R 121919 hydrochloride is a high-affinity CRF1 receptor antagonist with a Ki of 3.5 nM. It shows activity in receptor binding and functional assays. The compound is selective for CRF1.
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| ln Vivo |
In vivo, R 121919 hydrochloride is orally bioavailable. It has antidepressant and anxiolytic effects. It reduces stress-induced elevations of plasma ACTH. It is used in research on stress, anxiety, and depression.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for R 121919 hydrochloride are performed using CRF1 receptor binding studies. The compound is incubated with CRF1 receptor preparations and radiolabeled CRF ligands at concentrations ranging from 0.001-100 µM. Binding affinity is measured and Ki values (3.5 nM) are calculated from displacement curves.
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| Cell Assay |
In vitro cellular assays are performed using cells expressing CRF1 receptors. Cells are treated with R 121919 hydrochloride at concentrations ranging from 0.001-10 µM for 24-48 hours. Receptor antagonism is assessed by measuring inhibition of CRF-induced cAMP production. Cell viability is assessed using MTT assays.
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| Animal Protocol |
In vivo animal experiments are conducted using rodent models of stress, anxiety, and depression. R 121919 hydrochloride is administered orally at doses ranging from 0.1-30 mg/kg. Stress-induced ACTH elevation is measured. Behavioral assays such as elevated plus maze and forced swim test are performed. Pharmacokinetic parameters are determined from plasma samples.
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| References |
|
| Molecular Formula |
C22H32N6.HCL
|
|---|---|
| Molecular Weight |
416.99062
|
| Exact Mass |
416.246
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| CAS # |
195055-66-4
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| PubChem CID |
22029352
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
5.21
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
29
|
| Complexity |
480
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCCN(CCC)C1=CC(=NC2=C(C(=NN12)C)C3=CN=C(C=C3C)N(C)C)C.Cl
|
| InChi Key |
LGDDPMVPDGTXMV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H32N6.ClH/c1-8-10-27(11-9-2)20-13-16(4)24-22-21(17(5)25-28(20)22)18-14-23-19(26(6)7)12-15(18)3;/h12-14H,8-11H2,1-7H3;1H
|
| Chemical Name |
3-[6-(dimethylamino)-4-methylpyridin-3-yl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3981 mL | 11.9907 mL | 23.9814 mL | |
| 5 mM | 0.4796 mL | 2.3981 mL | 4.7963 mL | |
| 10 mM | 0.2398 mL | 1.1991 mL | 2.3981 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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