TTK21
Based on 1 Customer Validation
TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of neurogenesis and long-term memory.CSP-TTK21 can ameliorate Aβ-impaired long-term potentiation (LTP). CSP-TTK21 may enhance the transcription of genes that promote synaptic health and cognitive function. CSP-TTK21 is orally effective and leads to improvements in motor functions, histone acetylation dynamics in a spinal injury rat model.
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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: 99.39%
- CAS 番号: 709676-56-2
- 分子式: C17H15ClF3NO2
- 分子量:357.75
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
- 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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CBP/p300 |
TTK21 (50-275 μM) is able to concentration-dependently activate CBP and p300 acetyltransferases and increase histone acetylation. Effectively activates CBP/p300 activity and increases the acetylation of histone H3 and H4. 100 μM TTK21 can promote the self-acetylation of p300[1].
TTK21 (50-275 μM; 6-24 h) in Hela cells, can't effectively penetrate the cell membrane to enter the cell by itself. However, when combined with carbon nanosphere CSP, it is able to enter SH-SY5Y neuronal cells and significantly increase the acetylation level of histone H3, indicating that the CSP-TTK21 complex has the ability to penetrate the cell membrane[1].
CSP-TTK21 (0.36 µg/ml; 1 h) can restor protein synthesis-dependent long-term potentiation (LTP) damage caused by Aβ (1-42) multimerst[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Rat hippocampal CA1 area slices
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Concentration:CSP-TTK21 0.36 µg/ml
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Incubation Time:1 h
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Result:CSP-TTK21 upregulated certain genes whose expression was decreased under Aβ(1–42) treatment, such as genes involved in the Wnt signaling pathway. CSP-TTK21 also potentially downregulated genes associated with inflammation, helping to reduce the neuroinflammatory response caused by Aβ(1–42).
CSP-TTK21 (20 mg/kg; p.o; single dose) enhances long-term potentiation comparably to intraperitoneal injection, suggesting effective memory enhancement in Wild-type mice[3].
CSP-TTK21 (10 mg/kg; p.o; weekly) promotes motor recovery after spinal cord injury in rats, and enhances the expression of regeneration-associated genes in the prefrontal cortex and cerebellum following spinal cord injury[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B57BL/6J male [1]
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Dosage:CSP-TTK21; 20 mg/kg; single dose
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Administration:i.p.
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Result:Increased histone acetylation significantly in the hippocampus and frontal cortex. CSP-TTK21 crossed the blood-brain barrier and was primarily detected in the brain, liver, and spleen. It promoted differentiation of newly generated neurons in the dentate gyrus.
Mice with CSP-TTK21 displayed a persistent memory of the platform location in a Morris water maze task for a longer period compared to controls, demonstrating enhanced long-term memory.
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Animal Model:Wild-type mice [3]
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Dosage:CSP-TTK21; 20 mg/kg; single dose
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Administration:p.o.
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Result:The administered compound crossed the blood-brain barrier, induced histone acetylation specifically H4K12ac and H3K14ac marks in the hippocampus, and did not alter basal synaptic transmission. It was found to enhance long-term potentiation comparably to intraperitoneal injection, suggesting effective memory enhancement through oral delivery.
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Animal Model:rats with spinal cord injury[3]
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Dosage:CSP-TTK21; 10 mg/kg; weekly
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Administration:p.o.
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Result:Rats with CSP-TTK21 showed significant improvement in locomotion and rearing activity compared to controls. Histone acetylation was notably increased in the spinal cord, suggesting enhanced gene expression linked to regeneration and functional recovery. Enhanced histone acetylation levels (H4K12ac, H3K27ac, H3K9ac) were observed in the prefrontal cortex and cerebellum of rats with CSP-TTK21, indicating active epigenetic modifications that support neuronal regeneration and functional recovery.
化学情報
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CAS 番号 709676-56-2
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性状 Solid
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分子量 357.75
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分子式 C17H15ClF3NO2
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Color White to off-white
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SMILES
ClC1=CC=C(C=C1C(F)(F)F)NC(C2=CC=CC=C2OCCC)=O
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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 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (279.52 mM; ultrasonic and warming and heat to 60°C; 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.
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.
純度とドキュメンテーション
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データシート (281 KB)
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SDS (393 KB)
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- Français - FR (393 KB)
- Deutsch - DE (393 KB)
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- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Chatterjee S, et al. A novel activator of CBP/p300 acetyltransferases promotes neurogenesis and extends memory duration in adult mice. J Neurosci. 2013;33(26):10698-10712. [Content Brief]
[2]. Singh A et al. Glucose derived carbon nanosphere (CSP) conjugated TTK21, an activator of the histone acetyltransferases CBP/p300, ameliorates amyloid-beta 1-42 induced deficits in plasticity and associativity in hippocampal CA1 pyramidal neurons. Aging Cell. 2022 Sep;21(9):e13675. [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 | 2.7952 mL | 13.9762 mL | 27.9525 mL | 69.8812 mL |
| 5 mM | 0.5590 mL | 2.7952 mL | 5.5905 mL | 13.9762 mL | |
| 10 mM | 0.2795 mL | 1.3976 mL | 2.7952 mL | 6.9881 mL | |
| 15 mM | 0.1863 mL | 0.9317 mL | 1.8635 mL | 4.6587 mL | |
| 20 mM | 0.1398 mL | 0.6988 mL | 1.3976 mL | 3.4941 mL | |
| 25 mM | 0.1118 mL | 0.5590 mL | 1.1181 mL | 2.7952 mL | |
| 30 mM | 0.0932 mL | 0.4659 mL | 0.9317 mL | 2.3294 mL | |
| 40 mM | 0.0699 mL | 0.3494 mL | 0.6988 mL | 1.7470 mL | |
| 50 mM | 0.0559 mL | 0.2795 mL | 0.5590 mL | 1.3976 mL | |
| 60 mM | 0.0466 mL | 0.2329 mL | 0.4659 mL | 1.1647 mL | |
| 80 mM | 0.0349 mL | 0.1747 mL | 0.3494 mL | 0.8735 mL | |
| 100 mM | 0.0280 mL | 0.1398 mL | 0.2795 mL | 0.6988 mL |
TTK21 関連分類
HY-116673 関連分類
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