Chlorpromazine HCl (Synonyms: CPZ) |
| Catalog No.GC14216 |
Chlorpromazine HCl은 경구 투여가 가능하고 혈뇌장벽을 통과할 수 있는 페노티아진계 항정신병 약물로 D2 도파민 수용체와 5-HT2A를 효과적으로 길항하고 강력한 진정 효과가 있다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 69-09-0
Sample solution is provided at 25 µL, 10mM.
Chlorpromazine HCl은 경구 투여가 가능하고 혈뇌장벽을 통과할 수 있는 페노티아진계 항정신병 약물로 D2 도파민 수용체와 5-HT2A를 효과적으로 길항하고 강력한 진정 효과가 있다.Chlorpromazine HCl은 항암 활성을 가지고 있고 증식 억제, 세포 자가포식 유도, 세포 주기 정지, 사이토크롬 c 산화효소 억제, 종양 성장 및 전이 억제, 종양 면역 탈출 억제 등을 포함한다 [3]. Chlorpromazine HCl은 hNav1.7 통로와 hERG 칼륨 통로를 차단할 수 있다 [4, 5].
체외 실험에서 U-87MG 세포를 프로 마진 HCl(10-40μM)로 24시간과 48시간 처리하면 세포 생존 능력 감소, 세포 증식, 세포 내 사이클린 A와 사이클린 B1 수준이 용량과 시간 의존적으로 감소했다[6]. 쥐 골수 세포를 1시간 동안 10μM의 Chlorpromazine HCl로 처리하면 소형 세포 외부 베스터(sEVs)의 내화를 유의미하게 억제하고 골수 유래 억제 세포(MDSCs)의 수를 크게 줄였다[7].
체내 실험에서 Chlorpromazine HCl(20mg/kg)을 U-87MG 신경교종세포 이종 이식 쥐에게 24일 동안 복강 주사했고 종양 성장을 현저히 억제하고 24일째에 종양 성장 억제율이 43.5%에 보였다[6].
References:
[1] Asano T, Tanaka K, Tada A, et al. Ameliorative effect of chlorpromazine hydrochloride on visceral hypersensitivity in rats: possible involvement of 5‐HT2A receptor[J]. British Journal of Pharmacology, 2017, 174(19): 3370-3381.
[2] Suzuki H, Gen K, Inoue Y. Comparison of the anti-dopamine D2 and anti-serotonin 5-HT2A activities of chlorpromazine, bromperidol, haloperidol and second-generation antipsychotics parent compounds and metabolites thereof[J]. Journal of Psychopharmacology, 2013, 27(4): 396-400.
[3] Kamgar-Dayhoff P, Brelidze T I. Multifaceted effect of chlorpromazine in cancer: Implications for cancer treatment[J]. Oncotarget, 2021, 12(14): 1406.
[4] Lee S J, Kim D H, Hahn S J, et al. Mechanism of inhibition by chlorpromazine of the human pain threshold sodium channel, Nav1. 7[J]. Neuroscience Letters, 2017, 639: 1-7.
[5] Thomas D, Wu K, Kathöfer S, et al. The antipsychotic drug chlorpromazine inhibits HERG potassium channels[J]. British journal of pharmacology, 2003, 139(3): 567-574.
[6] Shin S Y, Lee K S, Choi Y K, et al. The antipsychotic agent chlorpromazine induces autophagic cell death by inhibiting the Akt/mTOR pathway in human U-87MG glioma cells[J]. Carcinogenesis, 2013, 34(9): 2080-2089.
[7] Yang Z, Huo Y, Zhou S, et al. Cancer cell-intrinsic XBP1 drives immunosuppressive reprogramming of intratumoral myeloid cells by promoting cholesterol production[J]. Cell Metabolism, 2022, 34(12): 2018-2035. e8.
| 세포 실험 [1]: | |
세포 라인 | U-87MG 세포 |
제조 방법 | U-87MG 세포(2×103 세포/샘플)를 96웰 판에 배양하고 Chlorpromazine HCl의 증가하는 농도(0, 10, 20, 40μM)로 서로 다른 시간 기간(0, 24, 48시간)동안 처리했습니다. 세포 생존율과 세포 증식을 측정했습니다. |
반응 조건 | 0-40μM; 24, 48시간 동안 |
응용 분야 | Chlorpromazine HCl은 용량과 시간 의존적으로 세포 생존율과 증식을 감소시킵니다. |
| 동물 실험 [2]: | |
동물 모형 | 무흉선 누드 쥐 |
제조 방법 | U-87MG 신경 교종 세포(1×106 세포, 100μl 무혈청 DMEM)를 5~6주령 무흉선 누드 쥐의 우측 측면에 피하 주사했습니다. 종양의 평균 부피가 약 100mm³에 도달하면 매일 100μl의 PBS(대조 그룹)나 Chlorpromazine HCl(20mg/kg)을 복강 주사했습니다. 쥐는 24일째에 이산화탄소에 노출되어 안락사되었고 피부 이종 이식 종양의 크기를 비교했습니다. |
제형 | 20mg/kg; i.p. |
응용 분야 | PBS(대조 그룹) 처리와 비교하고 Chlorpromazine HClCPZ 처리는 이종 이식 종양 성장을 유의적으로 억제했고 24일째에 종양 성장 억제율은 43.5%였습니다. |
References: | |
| Cas No. | 69-09-0 | SDF | |
| Synonyms | CPZ | ||
| Chemical Name | 3-(2-chlorophenothiazin-10-yl)-N,N-dimethylpropan-1-amine;hydrochloride | ||
| Canonical SMILES | CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl.Cl | ||
| Formula | C17H19ClN2S.HCl | M.Wt | 355.33 |
| Solubility | ≥ 17.8 mg/mL in DMSO, ≥ 74.8 mg/mL in EtOH, ≥ 71.4 mg/mL in Water | Storage | Store at RT,protect from light,unstable in solution, ready to use. |
| 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8143 mL | 14.0714 mL | 28.1429 mL |
| 5 mM | 0.5629 mL | 2.8143 mL | 5.6286 mL |
| 10 mM | 0.2814 mL | 1.4071 mL | 2.8143 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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 ddH2O, 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
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
-
Related Biological Data
Cellular uptake and uptake mechanism study of PPDC.Flow cytometry profiles and quantitative analysis of endocytosis pathway.Chlorpromazine, amiloride and nystatin were used to pretreat the 4T1 cells,respectively.
Three endocytosis inhibitors, including CPZ（GLPBIO） (20 μg/ml), amiloride (10 μg/ml) and nystatin (20 μg/ml), were used to inhibit the clathrinmediated,macropinocytosis-mediated and caveolae-mediatedpathway, respectively.
Regenerative Biomaterials 10 (2023): rbad048. PMID: 37250978 IF: 6.7 -
Related Biological Data
Effect of octopamine antagonist treatment on locomotion assay in vivo. (a) The percentage of larvae that reach the target food in 30 min. (b) The time when half of the larvae reached the food.
Chlorpromazine and mianserin (GlpBio), which have significant antagonistic effects on OARs.
Archives of Insect Biochemistry and Physiology (2021): e21772. PMID: 33719088 IF: 1.691
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *