Crinecerfont
Based on 1 Customer Validation
Crinecerfont (SSR-125543) is an orally effective corticotropin-releasing factor receptor type-1 (CRF1 receptor) antagonist. Crinecerfont blocks CRF1 receptor signaling to reduce adrenocorticotropic hormone secretion. Crinecerfont improves hypothalamic-pituitary-adrenal axis negative feedback sensitivity in chronically stressed mice. Crinecerfont can be used for the research of chronic stress conditions and classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency. Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- Pureza: 98.08%
- No. CAS: 752253-39-7
- Fòrmula: C27H28ClFN2OS
- Peso molecular:483.04
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Membrane Transporter/Ion Channel Compound Library
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High-Throughput Bioactive Compound Library
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Alkyne Compound Library
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Classic FDA-Approved Drug Library
HY-L261
Actividad biológica
IC50: CRF1 receptor
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/cByJ mice (male, 3-4 months old, chronic stress induced via unpredictable chronic mild stress for 7 weeks)[1]
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Dosage:20 mg/kg
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Administration:i.p.; daily; 5 weeks
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Result:Exacerbated fecal corticosterone metabolite concentrations at six out of nine circadian time points; increased basal plasma corticosterone levels; restored corticosterone suppression in the dexamethasone suppression test to improve HPA axis negative feedback sensitivity.
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Animal Model:BALB/cByJ mice (male, 3-4 months old)[1]
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Dosage:20 mg/kg
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Administration:i.p.; daily; 5 weeks
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Result:Showed no effects on fecal corticosterone metabolite circadian activity; showed no effects on plasma corticosterone levels; showed no effects on HPA axis negative feedback sensitivity.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 752253-39-7
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Appearance Solid
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Peso molecular 483.04
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Fòrmula C27H28ClFN2OS
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Color Light yellow to yellow
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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
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Synonyms
SSR-125543
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (207.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ibarguen-Vargas Y, et al. CRF-R1 Antagonist Treatment Exacerbates Circadian Corticosterone Secretion under Chronic Stress, but Preserves HPA Feedback Sensitivity. Pharmaceutics. 2021;13(12):2114. Published 2021 Dec 8. [Content Brief]
[2]. Newfield RS, et al. Crinecerfont, a CRF1 Receptor Antagonist, Lowers Adrenal Androgens in Adolescents With Congenital Adrenal Hyperplasia. J Clin Endocrinol Metab. 2023;108(11):2871-2878. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0702 mL | 10.3511 mL | 20.7022 mL | 51.7555 mL |
| 5 mM | 0.4140 mL | 2.0702 mL | 4.1404 mL | 10.3511 mL | |
| 10 mM | 0.2070 mL | 1.0351 mL | 2.0702 mL | 5.1756 mL | |
| 15 mM | 0.1380 mL | 0.6901 mL | 1.3801 mL | 3.4504 mL | |
| 20 mM | 0.1035 mL | 0.5176 mL | 1.0351 mL | 2.5878 mL | |
| 25 mM | 0.0828 mL | 0.4140 mL | 0.8281 mL | 2.0702 mL | |
| 30 mM | 0.0690 mL | 0.3450 mL | 0.6901 mL | 1.7252 mL | |
| 40 mM | 0.0518 mL | 0.2588 mL | 0.5176 mL | 1.2939 mL | |
| 50 mM | 0.0414 mL | 0.2070 mL | 0.4140 mL | 1.0351 mL | |
| 60 mM | 0.0345 mL | 0.1725 mL | 0.3450 mL | 0.8626 mL | |
| 80 mM | 0.0259 mL | 0.1294 mL | 0.2588 mL | 0.6469 mL | |
| 100 mM | 0.0207 mL | 0.1035 mL | 0.2070 mL | 0.5176 mL |
Crinecerfont Related Classifications
Referencia número: HY-106203
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- Crinecerfont
- 752253-39-7
- SSR-125543
- SSR125543
- SSR 125543
- CFTR
- chronic stress conditions
- classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency
- adrenal androgens
- hypothalamic-pituitary-adrenal axis
- depression
- adrenocorticotropic hormone
- corticosterone
- corticotropin-releasing factor receptor type-1
- chronically stressed mice
- anxiety
- Inhibitor
- inhibitor
- inhibit