| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
H1C receptor.
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|---|---|
| ln Vitro |
Tesmilifene may affect how 12(S)HETE affects cancer cells, which could have an indirect effect on how susceptible cellular DNA is to chemotherapy[1].
Tesmilifene fumarate is an H1C receptor antagonist that potentiates a wide range of cytotoxic agents. It offers some protection of normal cells. As a potentiator of chemotherapy, it may enhance the efficacy of cytotoxic drugs while reducing their toxicity to normal tissues. |
| ln Vivo |
Tesmilifene (DPPE, 20 μg (icv in 5 μL) and 20 mg/kg (sc)) increased the amount of seizures brought on by both convulsants[2].
In vivo, Tesmilifene fumarate has been investigated for its potential in cancer therapy as an adjunct to chemotherapy. Its ability to potentiate cytotoxics and protect normal cells suggests it may improve the therapeutic index of anticancer drugs. |
| Enzyme Assay |
In vitro receptor binding assays for tesmilifene fumarate are performed to evaluate its affinity for the H1C receptor. Radioligand binding studies using membrane preparations from cells expressing the H1C receptor are conducted. The compound's ability to displace a specific radiolabeled ligand is measured to calculate its binding affinity.
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| Cell Assay |
In vitro cell-based assays are conducted using cancer cell lines to evaluate the effects of tesmilifene fumarate on cytotoxicity. The compound is tested in combination with various cytotoxic agents, and cell viability is measured to assess its potentiating effects. Its protective effects on normal cells are also evaluated in parallel assays.
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| Animal Protocol |
Animal/Disease Models: Male BKTO mice (25-45 g)[2].
Doses: 20 mg/kg (sc) and 20 μg (icv in 5 μL). Route of Administration: SC and icv. Experimental Results: Potentiated seizures induced by both convulsants. In vivo animal studies are conducted in tumor xenograft models to evaluate the effects of tesmilifene fumarate on tumor growth and chemotherapy efficacy. The compound is administered in combination with cytotoxic agents, and its effects on tumor size, survival, and toxicity are assessed. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for tesmilifene fumarate. As a research compound, its ADME properties would be characterized in standard preclinical studies.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for tesmilifene fumarate. As an H1C receptor antagonist, its toxicity profile is expected to be related to its mechanism of action. Standard safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
Tesmilifene fumarate (DPPE fumarate) is an H1C receptor antagonist that potentiates a wide range of cytotoxic agents and offers protection of normal cells. It has been investigated as a potentiator of chemotherapy in cancer research. The compound is not approved for human therapeutic use and is strictly for research purposes.
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| Molecular Formula |
C23H29NO5
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|---|---|
| Molecular Weight |
399.48
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| Exact Mass |
399.204
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| CAS # |
1185241-83-1
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| PubChem CID |
45073473
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
29
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| Complexity |
369
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(CC)CCOC1=CC=C(C=C1)CC2=CC=CC=C2.C(=C/C(=O)O)\C(=O)O
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| InChi Key |
ZOOMDYHTGZSGDD-WLHGVMLRSA-N
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| InChi Code |
InChI=1S/C19H25NO.C4H4O4/c1-3-20(4-2)14-15-21-19-12-10-18(11-13-19)16-17-8-6-5-7-9-17;5-3(6)1-2-4(7)8/h5-13H,3-4,14-16H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1+
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| Chemical Name |
2-(4-benzylphenoxy)-N,N-diethylethanamine;(E)-but-2-enedioic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 250 mg/mL (625.81 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5033 mL | 12.5163 mL | 25.0325 mL | |
| 5 mM | 0.5007 mL | 2.5033 mL | 5.0065 mL | |
| 10 mM | 0.2503 mL | 1.2516 mL | 2.5033 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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