ZLN005 |
カタログ番号GC13437
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ZLN005は過酸化物増殖剤活性化の受容体-γ共同活性因子-1α (PGC-1α)の有力で細胞特異性の転写活性剤である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 49671-76-3
Sample solution is provided at 25 µL, 10mM.
ZLN005は過酸化物増殖剤活性化の受容体-γ共同活性因子-1α (PGC-1α)の有力で細胞特異性の転写活性剤である[1]。PGC-1αは肝心な転写共同活性化因子であり、主にミトコンドリア生合成と酸化リン酸化プロセスを制御する[2]。ZLN005は通常、糖尿病、ミトコンドリア老化と敗血症などの疾患に関連する研究に使われる[3,4]。
体外で、ZLN005 (1μM)でTHP-1細胞を48時間事前処理し、更に1μg/mLのリポ多糖類(LPS)で刺激した結果、PGC-1αのmRNA発見を著しく増やし、LPS刺激で減ったミトコンドリアDNAコピー数を回復させた[5]。ZLN005 (10μM)で分化のヒト網膜色素上皮細胞ARPE-19細胞を24時間処理し、ミトコンドリアスーパーオキシドの産生を著しく減らした[6]。
体内で、盲腸結紮と穿刺(CLP)が誘導した敗血症のC57BL/6マウスに、ZLN005 (12mg/kg/日；3日間)を腹腔内注射した結果、6日間の生存率を著しく改善した（0%から30%に）[5]。周術期神経認知障害（PND）マウスモデルで、手術の3日前から手術の1日後まで、ZLN005 (7.5mg/kg/日)を毎日腹腔内注射した結果、術後24時間の時点で、海馬体と脳皮質における炎症促進サイトカインIL-6とIL-1βのレベルを著しく減らし、神経炎症を改善した[7]。肝虚血再灌流障害（IRI）手術の3日前、ZLN005 (12mg/kg/日)をC57BL/6マウスに3日間腹腔内注射して事前処理した結果、ALT、ASTとLDHの血清レベルを著しく減らし、肝臓組織壊死の面積を減らした[8]。
References:
[1] ZHANG W, XIONG H, PANG J, et al. PGC-1α overexpression promotes mitochondrial biogenesis to protect auditory cells against cisplatin-induced cytotoxicity[J]. Journal of Bio-X Research, 2019, 2(2): 81-86.
[2] LIU Y, BAI H, GUO F, et al. PGC-1α activator ZLN005 promotes maturation of cardiomyocytes derived from human embryonic stem cells[J]. Aging (Albany NY), 2020, 12(8): 7411.
[3] ZHAI M, HU H, ZHENG Y, et al. PGC1α: An emerging therapeutic target for chemotherapy-induced peripheral neuropathy[J]. Therapeutic Advances in Neurological Disorders, 2023, 16: 17562864231163361.
[4] QIAN L, ZHU Y, DENG C, et al. Peroxisome proliferator-activated receptor gamma coactivator-1 (PGC-1) family in physiological and pathophysiological process and diseases[J]. Signal Transduction and Targeted Therapy, 2024, 9(1): 50.
[5] SUZUKI Y, KAMI D, TAYA T, et al. ZLN005 improves the survival of polymicrobial sepsis by increasing the bacterial killing via inducing lysosomal acidification and biogenesis in phagocytes[J]. Frontiers in Immunology, 2023, 14: 1089905.
[6] SATISH S, PHILIPOSE H, ROSALES M A B, et al. Pharmaceutical induction of PGC-1α promotes retinal pigment epithelial cell metabolism and protects against oxidative damage[J]. Oxidative Medicine and Cellular Longevity, 2018, 2018(1): 9248640.
[7] WU X, DING S, WANG G, et al. ZLN005 reduces neuroinflammation and improves mitochondrial function in mice with perioperative neurocognitive disorders[J]. Journal of Inflammation Research, 2024, 17: 8135-8146.
[8] TOHME C, HAYKAL T, YANG R, et al. ZLN005, a PGC-1α Activator, Protects the Liver against Ischemia–Reperfusion Injury and the Progression of Hepatic Metastases[J]. Cells, 2024, 13(17): 1448.
| 細胞実験[1]: | |
細胞株 | THP-1細胞（ヒト単球性白血病細胞株） |
準備方法 | 10nMのホルボール12-ミリスチン酸13-アセタートを含有する成長培地で、5 × 105個の細胞/ウェルの密度で、細胞を12ウェルの細胞培養プレートに播種した。48時間後、培地の上清を注意深く除去し、プレートの底に接着した細胞が剥がれることを避けた。48時間後、1μg/mlのLPSを添加し、細胞を各時点で採取し、実験に使った。 |
反応条件 | 1μM；48時間 |
アプリケーション | ZLN005 (1μM)でTHP-1細胞を48時間事前処理し、更に1μg/mLのリポ多糖類(LPS)で刺激した結果、PGC-1αのmRNA発見を著しく増やし、LPS刺激で減ったミトコンドリアDNAコピー数を回復させた。 |
| 動物実験 [1]: | |
動物モデル | CLP誘発の敗血症C57BL/6マウス |
準備方法 | ZLN005ストック溶液は、10mMの濃度に調整したDMSOで調製した。0日目から2日目まで、ZLN005 (12mg/kg)をマウスに注射した。CLP後の6日目まで、マウスの生存率を持続的に検査した。 |
投与形態 | 12mg/kg/日；3日間；腹腔内注射 |
アプリケーション | CLP誘発の敗血症のC57BL/6マウスで、ZLN005 (12mg/kg/日；3日間)を腹腔内注射した結果、6日間の生存率を0%から30%までに改善した。 |
References: | |
| Cas No. | 49671-76-3 | SDF | |
| Chemical Name | 2-(4-tert-butylphenyl)-1H-benzimidazole | ||
| Canonical SMILES | CC(C)(C)C1=CC=C(C=C1)C2=NC3=CC=CC=C3N2 | ||
| Formula | C17H18N2 | M.Wt | 250.34 |
| 溶解度 | ≥ 23.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.9946 mL | 19.9728 mL | 39.9457 mL |
| 5 mM | 798.9 μL | 3.9946 mL | 7.9891 mL |
| 10 mM | 399.5 μL | 1.9973 mL | 3.9946 mL |
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)