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| Targets |
Zaldaride maleate primarily targets calmodulin (CaM), a calcium-binding messenger protein that mediates numerous cellular processes, including inflammation, smooth muscle contraction, and neurotransmission. By binding to calmodulin, Zaldaride maleate inhibits its interaction with various target enzymes, such as calmodulin-stimulated cAMP phosphodiesterase (PDE). This inhibition disrupts CaM-dependent signaling pathways. Additionally, Zaldaride maleate has been shown to block voltage-gated ion channels and inhibit nAChR, suggesting it may have multiple targets.
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| ln Vitro |
In vitro, Zaldaride maleate is a potent inhibitor of calmodulin-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM. It also prevents estrogen-induced transcription activation by ER. In PC12 cells, Zaldaride maleate reversibly blocks voltage-activated Na⁺, Ca²⁺, and K⁺ currents and inhibits nicotinic acetylcholine receptors (nAChR). This broad range of activities indicates that Zaldaride maleate is a multi-functional compound that can affect various cellular processes, including ion channel function and neurotransmitter signaling.
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| ln Vivo |
In the 16, 16-dimethyl prostaglandin E2 model, zamaldaridemaleate (KW 5617, PO, 3 mg/kg) ameliorates diarrhea [4].
In vivo, Zaldaride maleate has been shown to ameliorate diarrhea in animal models. In the 16,16-dimethyl prostaglandin E2 model, oral administration of Zaldaride maleate at 3 mg/kg ameliorated diarrhea. This effect is likely due to its inhibition of calmodulin, which plays a role in intestinal fluid secretion. The compound's oral activity makes it a useful tool for studying calmodulin-mediated processes in vivo. It has also been investigated for its potential in treating other conditions, but detailed in vivo data are limited. |
| Enzyme Assay |
Non-cellular in vitro assays for Zaldaride maleate involve measuring its inhibition of calmodulin-stimulated cAMP phosphodiesterase (PDE) activity. A standard protocol uses purified calmodulin and PDE enzyme. The reaction is performed in a buffer containing cAMP, calmodulin, Ca²⁺, and varying concentrations of Zaldaride maleate. The amount of cAMP hydrolyzed is measured using a colorimetric or radiometric assay. The IC50 value is determined from the concentration-response curve.
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| Cell Assay |
Cellular assays for Zaldaride maleate are performed using cell lines such as PC12 cells. To assess its effects on ion channels, cells are treated with Zaldaride maleate, and the currents are measured using patch-clamp electrophysiology. To assess its effects on nAChR, cells are stimulated with acetylcholine or nicotine in the presence or absence of Zaldaride maleate, and the resulting currents are measured. The compound's effects on cell proliferation or signaling can also be assessed using standard biochemical assays.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat, whinnying weight 193-265 grams [4].
Doses: 3-100 mg/kg. Management: PO. Experimental Results: KW-5617 at 3 to 100 mg/kg Dramatically improved DMPGE-induced diarrhea 60 minutes before DMPGE2 challenge and Dramatically diminished bowel movements when the drug was 100 mg/kg (oral). Pretreatment with KW-5617 at 3 to 10 mg/kg (po) Dramatically delayed the onset of diarrhea, and the drug diminished or eliminated the incidence of diarrhea at 30 and 100 mg/kg (po). In vivo animal studies for Zaldaride maleate have been conducted in models of diarrhea. In the 16,16-dimethyl prostaglandin E2 model, animals are administered the prostaglandin analog to induce diarrhea. Zaldaride maleate is then administered orally at doses such as 3 mg/kg. The severity of diarrhea is assessed over a period of time. A reduction in diarrhea severity in the treated group compared to the control group indicates efficacy. |
| ADME/Pharmacokinetics |
Zaldaride maleate is a small molecule with a molecular weight of 544.60. It is orally active, indicating that it is well-absorbed after oral administration. Detailed pharmacokinetic parameters for Zaldaride maleate, such as half-life, bioavailability, and clearance, have not been fully reported in the available literature. However, its oral activity and efficacy in animal models suggest that it has sufficient bioavailability to exert its effects.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for Zaldaride maleate have not been extensively reported. As a research chemical, it is not intended for human use and is strictly for preclinical research purposes. Standard safety precautions should be followed when handling this compound, including the use of personal protective equipment. No specific toxicity data, such as LD50 values, are available in the provided literature.
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| References |
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| Additional Infomation |
See also: Zaldaride (Note moved to).
Zaldaride maleate (CGS-9343B, KW-5617) is a calmodulin inhibitor that has been studied for its potential therapeutic applications. Its ability to inhibit calmodulin-stimulated PDE activity with high potency (IC50 = 3.3 nM) makes it a valuable tool for studying calmodulin-mediated signaling pathways. The compound has also been shown to block ion channels and nAChR, suggesting it may have additional mechanisms of action. It is not a clinically approved drug and has not entered clinical trials. Its primary application is in academic and pharmaceutical research. |
| Molecular Formula |
C26H28N4O2.C4H4O4
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|---|---|
| Molecular Weight |
544.59828
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| Exact Mass |
544.232
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| CAS # |
109826-27-9
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| Related CAS # |
109826-26-8;109826-27-9;
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| PubChem CID |
6450522
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| Appearance |
White to off-white solid powder
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| Density |
1.31g/cm3
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| Boiling Point |
778ºC at 760 mmHg
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| Flash Point |
424.3ºC
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| Vapour Pressure |
1.78E-25mmHg at 25°C
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| LogP |
3.852
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
40
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| Complexity |
814
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1(C2=CC=CN2C3=CC=CC=C3CO1)CN4CCC(CC4)N5C6=CC=CC=C6NC5=O.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
NGODOSILXOFQPH-BTJKTKAUSA-N
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| InChi Code |
InChI=1S/C26H28N4O2.C4H4O4/c1-26(24-11-6-14-29(24)22-9-4-2-7-19(22)17-32-26)18-28-15-12-20(13-16-28)30-23-10-5-3-8-21(23)27-25(30)31;5-3(6)1-2-4(7)8/h2-11,14,20H,12-13,15-18H2,1H3,(H,27,31);1-2H,(H,5,6)(H,7,8)/b;2-1-
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| Chemical Name |
(Z)-but-2-enedioic acid;3-[1-[(4-methyl-6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl)methyl]piperidin-4-yl]-1H-benzimidazol-2-one
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8362 mL | 9.1811 mL | 18.3621 mL | |
| 5 mM | 0.3672 mL | 1.8362 mL | 3.6724 mL | |
| 10 mM | 0.1836 mL | 0.9181 mL | 1.8362 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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