Cipemastat
Based on 1 Customer Validation
Cipemastat is a potent, competitive inhibitor of human collagenases 1, 2 and 3 with Kis of 3.0, 4.4 and 3.4 nM, respectively.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.20%
- CAS 番号: 190648-49-8
- 分子式: C22H36N4O5
- 分子量:436.55
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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collagenases 1 3.0 nM (Ki) |
collagenases 2 4.4 nM (Ki) |
collagenases 3 3.4 nM (Ki) |
stromelysins 1 527 nM (Ki) |
gelatinase A 154 nM (Ki) |
gelatinase B 59.1 nM (Ki) |
Cipemastat (Ro 32-3555) is a potent, competitive inhibitor of human matrix metalloproteinases. Cipemastat is selective for collagenase 1, 2 and 3 relative to related matrix metalloproteinases. Cipemastat is also a potent inhibitor of rat collagenase (IC50=44.7±3.4 nM (n=4)). In vitro cartilage degradation ± inhibited IL-1a induced cartilage degradation in vitro in a concentration-dependent manner with an IC50=60 nM. The inhibition is not mediated by a cytotoxic action on explant chondrocytes. Cipemastat, at all concentrations tested, fail to modify glucose utilization when compared to explants cultured in the presence of IL-La alone[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 190648-49-8
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性状 Solid
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分子量 436.55
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分子式 C22H36N4O5
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Color Off-white to light yellow
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SMILES
O=C(N1C[C@H](C(NO)=O)[C@H](C(N2CCCCC2)=O)CC3CCCC3)C(C)(C)N(C)C1=O
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別名
Ro 32-3555
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (229.07 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (5.73 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 (5.73 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.
プロトコル
Rats[1]
Cipemastat (Ro 32-3555) is formulated in 5% succinylated gelatin and the volume administered to rats is 10 mL/kg, p.o. Female, AHH/R strain rats are used. Rats are anaesthetized in an isoflurane-closed system, and an intra-articular injection of 20 mL of the P. acnes/Freund's incomplete adjuvant emulsion made into the right hind knee. Twenty-eight days later the injection is repeated with the same volume and concentration of antigen to induce the monoarthritis. Animals are orally dosed once daily with either 5% succinylated gelatin as the control vehicle or Cipemastat (50 mg/kg) starting on day 1 after challenge injection. Groups of eight female AHH/R rats are used in these experiments. The animals are dosed twice daily with either 50, 25 or 10 mg/kg Cipemastat, dexamethasone (0.1 mg/kg, s.c. once/day) or vehicle control (10 mL/kg, p.o., b.i.d.). The arthritis is induced by injection into the right hind paws with 0.1 mL of a 5 mg/mL homogenized suspension of Mycobacterium tuberculosis in liquid paraffin. The volume of both the right and left hind paws is measured by water plethysmography by immersing the paw up to the hair line of the ankle. Paw volumes are determined every two or three days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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データシート (280 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 2.2907 mL | 11.4534 mL | 22.9069 mL | 57.2672 mL |
| 5 mM | 0.4581 mL | 2.2907 mL | 4.5814 mL | 11.4534 mL | |
| 10 mM | 0.2291 mL | 1.1453 mL | 2.2907 mL | 5.7267 mL | |
| 15 mM | 0.1527 mL | 0.7636 mL | 1.5271 mL | 3.8178 mL | |
| 20 mM | 0.1145 mL | 0.5727 mL | 1.1453 mL | 2.8634 mL | |
| 25 mM | 0.0916 mL | 0.4581 mL | 0.9163 mL | 2.2907 mL | |
| 30 mM | 0.0764 mL | 0.3818 mL | 0.7636 mL | 1.9089 mL | |
| 40 mM | 0.0573 mL | 0.2863 mL | 0.5727 mL | 1.4317 mL | |
| 50 mM | 0.0458 mL | 0.2291 mL | 0.4581 mL | 1.1453 mL | |
| 60 mM | 0.0382 mL | 0.1909 mL | 0.3818 mL | 0.9545 mL | |
| 80 mM | 0.0286 mL | 0.1432 mL | 0.2863 mL | 0.7158 mL | |
| 100 mM | 0.0229 mL | 0.1145 mL | 0.2291 mL | 0.5727 mL |
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