Clofutriben
Based on 1 Customer Validation
Clofutriben (ASP3662) is a selective, orally active and brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with Ki values of 5.3 nM (human), 2.6 nM (mouse), and 23 nM (rat). Clofutriben inhibits conversion of inactive glucocorticoids to active glucocorticoids, reducing intracellular glucocorticoid exposure. Clofutriben ameliorates neuropathic pain, and restores muscle pressure thresholds in rodent models, while lacking effects in inflammatory pain.
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- Purity: 98.07%
- CAS No.: 1204178-50-6
- 화학식: C19H16ClF3N4O2
- 분자량:424.80
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
11β-HSD1 (mouse) 2.6 nM (Ki) |
11β-HSD1 (human) 5.3 nM (Ki) |
11β-HSD1 (rat) 23 nM (Ki) |
In Vitro
Clofutriben (6-15 nM) potently and competitively inhibits human, mouse, and rat recombinant 11β-HSD1 with Ki values of 5.3 nM, 2.6 nM, and 23 nM respectively[2].
Clofutriben (30 μM) does not inhibit human HEK293-EBNA cell-expressed 11β-HSD2 even at concentrations up to 30 μM[2].
Clofutriben (0.03-10 μM; 30 min before Cortisone) concentration-dependently inhibits Cortisone (HY-17461)-to-Cortisol (HY-N0583) conversion in ex vivo rat prefrontal cortex and spinal cord tissue, with near-complete inhibition at 10 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Clofutriben (0.1-1 mg/kg; p.o.; single dose) at 0.3 and 1 mg/kg significantly ameliorates thermal hyperalgesia in rats, with a maximum improvement rate of 61% at 1 mg/kg[2].
Clofutriben (0.1-1 mg/kg; p.o.; single dose) at 0.3 and 1 mg/kg significantly ameliorates mechanical allodynia in STZ (HY-13753)-induced diabetic rats, with a maximum improvement rate of 52% at 1 mg/kg[2].
Clofutriben (0.1-1 mg/kg; p.o.; single dose) dose-dependently restores muscle pressure thresholds in rats, with an ED50 of 0.31 mg/kg and a maximum improvement rate of 82% at 1 mg/kg[2].
Clofutriben (0.1-1 mg/kg; p.o.; single dose) at doses up to 1 mg/kg has no effect on hot-plate test latency and only a weak effect on tail pinch test latency, indicating minimal activity against acute pain[2].
Clofutriben (0.3-3 mg/kg; p.o.; single dose) at doses up to 3 mg/kg does not impair motor coordination in healthy rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 150-315 g, spinal nerve ligation-induced)[2]
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Dosage:0.03, 0.1, 0.3 mg/kg (p.o.); 0.03-0.3 μg per animal (i.t.)
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Administration:p.o.; single dose; i.t.; single dose
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Result:Significantly raised mechanical paw withdrawal thresholds 2 h post-administration at oral doses of 0.1 and 0.3 mg/kg.
Achieved an 80% improvement rate at 0.3 mg/kg, with an ED50 of 0.087 mg/kg.
Dose-dependently reduced mechanical allodynia following intrathecal administration of 0.03, 0.1, and 0.3 μg per animal, with statistically significant effects at 0.1 and 0.3 μg 60 min post-administration.
Diminished analgesic effect of intrathecal 0.3 μg when co-administered with 10 μg Corticosterone (HY-B1618).
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1204178-50-6
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Appearance Solid
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분자량 424.80
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화학식 C19H16ClF3N4O2
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Color White to off-white
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SMILES
O=C(N)C1=CC=C(C2=NN=C(C(C)(OC3=C(F)C=C(Cl)C=C3F)C)N2C)C(F)=C1
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Synonyms
ASP3662
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (235.40 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)
In Vivo:
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: ≥ 5 mg/mL (11.77 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (11.77 mM); Suspended solution
This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
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.
순도&문서
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Data Sheet (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Buttgereit F, et al. Effects of clofutriben, a selective 11β-hydroxysteroid dehydrogenase type 1 inhibitor, on the efficacy and toxicity of prednisolone in patients with polymyalgia rheumatica: a single-blind controlled trial with sequential cohorts. Ann Rheum Dis. 2025 Nov 11:S0003-4967(25)04454-1. [Content Brief]
[2]. Kiso T, et al. Analgesic effects of ASP3662, a novel 11β-hydroxysteroid dehydrogenase 1 inhibitor, in rat models of neuropathic and dysfunctional pain. Br J Pharmacol. 2018;175(19):3784-3796. [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 |
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| DMSO | 1 mM | 2.3540 mL | 11.7702 mL | 23.5405 mL | 58.8512 mL |
| 5 mM | 0.4708 mL | 2.3540 mL | 4.7081 mL | 11.7702 mL | |
| 10 mM | 0.2354 mL | 1.1770 mL | 2.3540 mL | 5.8851 mL | |
| 15 mM | 0.1569 mL | 0.7847 mL | 1.5694 mL | 3.9234 mL | |
| 20 mM | 0.1177 mL | 0.5885 mL | 1.1770 mL | 2.9426 mL | |
| 25 mM | 0.0942 mL | 0.4708 mL | 0.9416 mL | 2.3540 mL | |
| 30 mM | 0.0785 mL | 0.3923 mL | 0.7847 mL | 1.9617 mL | |
| 40 mM | 0.0589 mL | 0.2943 mL | 0.5885 mL | 1.4713 mL | |
| 50 mM | 0.0471 mL | 0.2354 mL | 0.4708 mL | 1.1770 mL | |
| 60 mM | 0.0392 mL | 0.1962 mL | 0.3923 mL | 0.9809 mL | |
| 80 mM | 0.0294 mL | 0.1471 mL | 0.2943 mL | 0.7356 mL | |
| 100 mM | 0.0235 mL | 0.1177 mL | 0.2354 mL | 0.5885 mL |
Clofutriben Related Classifications
HY-120496 Related Classifications
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