Cimetidine
Based on 6 publication(s) in Google Scholar
Cimetidine (SKF-92334) is an orally active, inverse and BBB-permeable histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine has anti-cancer and anti-inflammatory activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.69%
- No. CAS: 51481-61-9
- Fòrmula: C10H16N6S
- Peso molecular:252.34
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Cimetidine
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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Cell Migration/Invasion Assay
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WB
Ver todos los productos específicos de isoformas Histamine Receptor
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Actividad biológica
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H2 Receptor |
Histamine Receptor 0.6 μM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1 μM
Compound: Cimetidine
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Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells
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[PMID: 26988801] |
| CHO | IC50 |
1 μM
Compound: Cimetidine
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Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
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[PMID: 27876250] |
| CHO | IC50 |
1 x 10-6 M
Compound: Cimetidine
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Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
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[PMID: 27876250] |
| HEK293 | IC50 |
1.2 μM
Compound: cimetidine
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Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
149 μM
Compound: Cimetidine
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Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of YM155 after 1 min
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of YM155 after 1 min
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[PMID: 28230985] |
| HRPE | IC50 |
1.5 mM
Compound: Cimetidine
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TP_TRANSPORTER: inhibition of TEA uptake in Octn1-HRPE cells
TP_TRANSPORTER: inhibition of TEA uptake in Octn1-HRPE cells
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[PMID: 10825452] |
| LLC-PK1 | IC50 |
>50 μM
Compound: Cimetidine
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Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
>50 μM
Compound: Cimetidine
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Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
>50 μM
Compound: Cimetidine
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Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
>50 μM
Compound: Cimetidine
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TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
>50 μM
Compound: Cimetidine
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TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells
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[PMID: 12699389] |
| LLC-PK1 | IC50 |
>50 μM
Compound: Cimetidine
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TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells
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[PMID: 12699389] |
| S2 | IC50 |
>2000 μM
Compound: Cimetidine
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TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in rOAT1-expressing S2 cells
TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in rOAT1-expressing S2 cells
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[PMID: 14978359] |
| S2 | IC50 |
166 μM
Compound: Cimetidine
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TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in rOAT3-expressing S2 cells
TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in rOAT3-expressing S2 cells
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[PMID: 14978359] |
| S2 | IC50 |
492 μM
Compound: Cimetidine
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TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in hOAT1-expressing S2 cells
TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in hOAT1-expressing S2 cells
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[PMID: 14978359] |
| S2 | IC50 |
92.4 μM
Compound: Cimetidine
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TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT3-expressing S2 cells
TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT3-expressing S2 cells
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[PMID: 14978359] |
| S2 | IC50 |
>2000 μM
Compound: Cimetidine
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TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT4-expressing S2 cells
TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT4-expressing S2 cells
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[PMID: 14978359] |
Cimetidine (SKF-92334), a partial agonist for H2R, has a pharmacological profile different from ranitidine and famotidine, possibly contributing to its antitumor activity on gastrointestinal cancers [1]. Cimetidine had no effect on the uptake and cytotoxicity of cisplatin in ovarian cancer cells with high OCT2 mRNA levels (IGROV-1 cells)[3].
Cimetidine showed no effect on proliferation, survival, migration and invasion of 3LL cells. Cimetidine reversed MDSC-mediated T-cell suppression, and improved IFN-γ production[4].
Cimetidine-mediated down-regulation of NCAM involved suppression of the nuclear translocation of NF-kappaB, a transcriptional activator of NCAM gene expression[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cimetidine exerts a beneficial effect on periodontal disease in rats, decreasing the RANKL/OPG ratio in gingival connective tissue and reducing alveolar bone resorption[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 51481-61-9
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Appearance Solid
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Peso molecular 252.34
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Fòrmula C10H16N6S
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Color White to off-white
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SMILES
CC1=C(CSCC/N=C(NC)/NC#N)NC=N1
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Synonyms
SKF-92334
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Biochim Biophys Acta Mol Basis Dis
Both carvedilol and cimetidine alleviate cisplatin-induced nephrotoxicity via downregulating OCT2. [Abstract]2025 Jun;1871(5):167754. PMID: 40044066 -
Exp Neurol
Inhibition of histamine receptor 3 alleviates sevoflurane-induced hypomyelination and neurobehavioral deficits. [Abstract]2025 Mar:385:115086. PMID: 39637962 -
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Ann Transl Med
Cimetidine promotes STUB1-mediated degradation of tumoral FOXP3 by activating PI3K-Akt pathway in gastric cancer. [Abstract]2020 Oct;8(20):1304. PMID: 33209884
Cimetidine purchased from MedChemExpress. Usage Cited in: Ann Transl Med. 2020 Oct;8(20):1304. [Abstract]
Our study showed that Cimetidine disrupted the proliferative capacity of GC cells by CCK8.
Cimetidine purchased from MedChemExpress. Usage Cited in: Ann Transl Med. 2020 Oct;8(20):1304. [Abstract]
Our study showed that Cimetidine (4 mM, 24 h) disrupted the proliferative capacity of GC cells byplate clone assay.
Cimetidine purchased from MedChemExpress. Usage Cited in: Ann Transl Med. 2020 Oct;8(20):1304. [Abstract]
Wound healing showed that Cimetidine (4 mM, 24 h) significantly reduced the number of migrated GC cells.
Cimetidine purchased from MedChemExpress. Usage Cited in: Ann Transl Med. 2020 Oct;8(20):1304. [Abstract]
Transwell assay showed that Cimetidine (4 mM, 24 h) significantly reduced the number of migrated GC cells.
Cimetidine purchased from MedChemExpress. Usage Cited in: Ann Transl Med. 2020 Oct;8(20):1304. [Abstract]
CCK8 assay revealed that the IC50 of Cimetidine (0-10 mM) inhibiting the viability of GC cells was increased with the decrease of FOXP3 level in these GC cells.
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Chemosphere
Mass-balance-model-based evaluation of sewage treatment plant contribution to residual pharmaceuticals in environmental waters. [Abstract]2019 Jun:225:378-387. PMID: 30884299
Solvente y solubilidad
DMSO : 60 mg/mL (237.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 2 mg/mL (7.93 mM; Need ultrasonic)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: 3 mg/mL (11.89 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 3 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: ≥ 3 mg/mL (11.89 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 3.12 mg/mL (12.36 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. M J Smit, et al. Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors. Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6802-7. [Content Brief]
[2]. Takahashi, H.K., et al., Cimetidine induces interleukin-18 production through H2-agonist activity in monocytes. Mol Pharmacol, 2006. 70(2): p. 450-3. [Content Brief]
[3]. Sprowl, J.A., et al., Conjunctive therapy of cisplatin with the OCT2 inhibitor cimetidine: influence on antitumor efficacy and systemic clearance. Clin Pharmacol Ther, 2013. 94(5): p. 585-92. [Content Brief]
[4]. Zheng, Y., et al., Cimetidine suppresses lung tumor growth in mice through proapoptosis of myeloid-derived suppressor cells. Mol Immunol, 2013. 54(1): p. 74-83. [Content Brief]
[5]. Fukuda, M., K. Kusama, and H. Sakashita, Cimetidine inhibits salivary gland tumor cell adhesion to neural cells and induces apoptosis by blocking NCAM expression. BMC Cancer, 2008. 8: p. 376. [Content Brief]
[6]. Longhini, R., et al., Cimetidine Reduces the Alveolar Bone Loss in Induced Periodontitis in Rat Molars. J Periodontol, 2013. [Content Brief]
[7]. Hough LB, et al. Cimetidine penetrates brain and inhibits non-opiate footshock-induced analgesia. Pharmacol Biochem Behav. 1986 May;24(5):1257-61. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.9629 mL | 19.8145 mL | 39.6291 mL | 99.0727 mL |
| 5 mM | 0.7926 mL | 3.9629 mL | 7.9258 mL | 19.8145 mL | |
| DMSO | 10 mM | 0.3963 mL | 1.9815 mL | 3.9629 mL | 9.9073 mL |
| 15 mM | 0.2642 mL | 1.3210 mL | 2.6419 mL | 6.6048 mL | |
| 20 mM | 0.1981 mL | 0.9907 mL | 1.9815 mL | 4.9536 mL | |
| 25 mM | 0.1585 mL | 0.7926 mL | 1.5852 mL | 3.9629 mL | |
| 30 mM | 0.1321 mL | 0.6605 mL | 1.3210 mL | 3.3024 mL | |
| 40 mM | 0.0991 mL | 0.4954 mL | 0.9907 mL | 2.4768 mL | |
| 50 mM | 0.0793 mL | 0.3963 mL | 0.7926 mL | 1.9815 mL | |
| 60 mM | 0.0660 mL | 0.3302 mL | 0.6605 mL | 1.6512 mL | |
| 80 mM | 0.0495 mL | 0.2477 mL | 0.4954 mL | 1.2384 mL | |
| 100 mM | 0.0396 mL | 0.1981 mL | 0.3963 mL | 0.9907 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Cimetidine Related Classifications
HY-14289 Related Classifications
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