| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vivo |
Crinecerfont (SSR-125543) (20 mg/kg; intraperitoneal injection; daily; 5 weeks) tosylate can improve the negative feedback sensitivity of the hypothalamus-pituitary-adrenal (HPA) axis in chronically stressed mice, but exacerbates their basal diurnal corticosterone secretion and does not change the diurnal activity or negative feedback sensitivity of the HPA axis in non-stressed control mice [1].
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|---|---|
| Animal Protocol |
Animal/Disease Models:BALB/cByJ mice (male, 3-4 months old) [1]
Doses: 20 mg/kg Route of Administration: Intraperitoneal injection; daily; 5 weeks Experimental Results: No effect on the diurnal rhythm activity of fecal corticosterone metabolites; no effect on plasma corticosterone levels; no effect on HPA axis negative feedback sensitivity. Animal/Disease Models:BALB/cByJ mice (male, 3-4 months old, chronically stressed for 7 weeks by unpredictable chronic mild stress)[1] Doses: 20 mg/kg Route of Administration: Intraperitoneal injection; once daily for 5 weeks Experimental Results: Fecal corticosterone metabolite concentrations were elevated at six of the nine circadian rhythm time points; baseline plasma corticosterone levels were elevated; corticosterone inhibition was restored in the dexamethasone inhibition test, thereby improving HPA axis negative feedback sensitivity. |
| References |
|
| Molecular Formula |
C34H36CLFN2O4S2
|
|---|---|
| Molecular Weight |
655.24
|
| CAS # |
2649012-17-7
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
C#CCN(C1=NC(C2=C(C=C(C(C)=C2)OC)Cl)=C(S1)C)[C@H](C3=CC(F)=C(C=C3)C)CC4CC4.O=S(C5=CC=C(C)C=C5)(O)=O
|
| Synonyms |
SSR-125543 tosylate
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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)
|
| 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 | 1.5262 mL | 7.6308 mL | 15.2616 mL | |
| 5 mM | 0.3052 mL | 1.5262 mL | 3.0523 mL | |
| 10 mM | 0.1526 mL | 0.7631 mL | 1.5262 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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