| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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W-9 hydrochloride is a novel and potent Calmodulin antagonist.
| Targets |
Calmodulin antagonist; binds to calmodulin and inhibits Ca²⁺/calmodulin-regulated enzyme activities [1]
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|---|---|
| ln Vitro |
W-7 inhibited proliferation of Chinese hamster ovary K1 (CHO-K1) cells with 50% inhibition of cell proliferation at 32 µM. In contrast, its analogue W-5 (chlorine-deficient) required 200 µM for 50% inhibition, correlating with its weaker calmodulin binding affinity. The inhibitory effect of W-7 up to 50 µM was reversible as assessed by colony formation assay [1]
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| Enzyme Assay |
Calmodulin-deficient, Ca²⁺-dependent cyclic nucleotide phosphodiesterase was purified from bovine brain. Calmodulin was purified from bovine brain and assayed by measuring the activation of the calmodulin-deficient phosphodiesterase. One unit of calmodulin was defined as the amount needed for 50% maximal activation.
Myosin light chain kinase was purified from chicken gizzard, and its activity was measured. The displacement of [³H]W-7 from purified calmodulin in the presence of Ca²⁺ by W-7 or W-5 was investigated using an equilibrium binding technique on a Sephadex G-50 gel filtration column [1] |
| Cell Assay |
CHO-K1 cells were cultured in medium supplemented with fetal bovine serum and antibiotics. For proliferation assays, cells were plated in dishes and treated with various concentrations of W-7 or W-5 for 2 days, after which cells were trypsinized and counted.
For colony formation assay, cells in exponential growth were treated with various concentrations of W-7 for 2 days, then cultured in fresh medium for 5 days to allow colony formation. Colonies were stained and counted. For synchronization studies, cells were synchronized by mechanical shaking during mitosis, then released into the cell cycle in the presence of 25 µM W-7 or 2.5 mM thymidine for 12 hours. DNA synthesis was assessed by [³H]thymidine incorporation into acid-insoluble fractions [1] |
| References | |
| Additional Infomation |
W-7 is a putative calmodulin antagonist that can penetrate the cell membrane and is mainly distributed in the cytoplasm, as confirmed by tritium-labeled W-7 autoradiography. It selectively inhibits the G₁/S phase of the cell cycle, similar to the effect of excess thymidine. W-7 and its derivatives are considered useful tools for studying calmodulin and cell biology [1].
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| Molecular Formula |
C16H22CL2N2O2S
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|---|---|
| Molecular Weight |
377.324
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| Exact Mass |
376.078
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| Elemental Analysis |
C, 50.93; H, 5.88; Cl, 18.79; N, 7.42; O, 8.48; S, 8.50
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| CAS # |
69762-85-2
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| Related CAS # |
W-7 hydrochloride;61714-27-0
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| PubChem CID |
44118677
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| Appearance |
White to off-white solid powder
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| Boiling Point |
518.8ºC at 760 mmHg
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| Melting Point |
221-223ºC
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| Flash Point |
267.6ºC
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| LogP |
6.264
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
23
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| Complexity |
424
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| Defined Atom Stereocenter Count |
0
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| SMILES |
0
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| InChi Key |
FGWDLQXTCSKXSK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H21ClN2O2S.ClH/c17-16-7-5-6-13-12-14(8-9-15(13)16)22(20,21)19-11-4-2-1-3-10-18;/h5-9,12,19H,1-4,10-11,18H2;1H
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| Chemical Name |
N-(6-aminohexyl)-5-chloronaphthalene-2-sulfonamide;hydrochloride
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| Synonyms |
W-9 HCl; W-9 hydrochloride
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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 (~662.55 mM)
H2O : ~20.83 mg/mL (~55.20 mM) |
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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 | 2.6503 mL | 13.2514 mL | 26.5027 mL | |
| 5 mM | 0.5301 mL | 2.6503 mL | 5.3005 mL | |
| 10 mM | 0.2650 mL | 1.3251 mL | 2.6503 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00440648 | COMPLETED | Drug: sevelamer carbonate, sevelamer hydrochloride Drug: sevelamer hydrochloride, sevelamer carbonate |
Chronic Kidney Disease | Genzyme, a Sanofi Company | 2005-03 | Phase 2 |
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