| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
VCAM-1 and its ligands' ability to adhere is inhibited by K-7174 (10 μM; 1 h) [1]. With an IC50 value of 14 μM, K-7174 (1-30 μM; 1 h) dose-dependently suppresses VCAM-1 expression [1]. With an IC50 value of 9 μM, K-7174 (1-30 μM; 1 h) dose-dependently suppresses TNFα's activation of VCAM-1 mRNA [1]. In Hep3B cells, K-7174 (10–20 μM; 24 hours) recovers Epo synthesis in a dose-dependent way [2]. K-7174 reduces GATA binding activity at 2.5–30 μM for a 24-hour period [2]. K-7174 (0-25 μM; 72 hours) causes apoptosis and suppresses the proliferation of MM cells [3].
|
|---|---|
| ln Vivo |
K-7174 (30 mg/kg; intraperitoneally once daily for 9 days) reverses hemoglobin concentration and reticulocyte count declines caused by TNF-α or IL-1β [2]. Tumor growth is inhibited in vivo by K-7174 (75 mg/kg; intraperitoneally given once daily for 14 days) [3]. In vivo tumor growth is inhibited more effectively by K-7174 (50 mg/kg; po, once daily for 14 days) than by intraperitoneal injection [3].
|
| Cell Assay |
Cell Viability Assay[3]
Cell Types: KMS12-BM, U266 and RPMI8226 Cell line Tested Concentrations: 0-25 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibition of MM cell growth. Apoptosis analysis [3] Cell Types: KMS12-BM, U266 and RPMI8226 Cell line Tested Concentrations: 10 μM Incubation Duration: 48 h Experimental Results: As the percentage of annexin-V positive cells increased, the apoptosis of MM cells increased Dramatically. |
| Animal Protocol |
Animal/Disease Models: ICR mice injected with IL-β or TNF-α [2]
Doses: 30 mg/kg Route of Administration: intraperitoneal (ip) injection; 30 mg/kg, one time/day for 9 days Experimental Results: Erythropoietin (Epo ) yield, reticulocyte count, and hemoglobin (Hb) concentration increased Animal/Disease Models: NOD/SCID (severe combined immunodeficient) mouse with murine xenografts [3] Doses: 75 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 14 Experimental Results: The tumor volume was Dramatically diminished, but the body weight was Dramatically diminished after 10 days. Animal/Disease Models: NOD/SCID (severe combined immunodeficient) mouse with murine xenografts [3] Doses: 50 mg/kg Route of Administration: po (oral gavage); one time/day for 14 days Experimental Results: Demonstrated anti-myeloma activity. Oral administration has proven to be more effective than intraperitoneal (ip) injection. |
| References |
|
| Molecular Formula |
C33H48N2O6
|
|---|---|
| Molecular Weight |
568.74402
|
| Exact Mass |
568.351
|
| CAS # |
191089-59-5
|
| Related CAS # |
K-7174 dihydrochloride;191089-60-8
|
| PubChem CID |
9874191
|
| Appearance |
Colorless to light yellow oil
|
| LogP |
5.908
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
16
|
| Heavy Atom Count |
41
|
| Complexity |
663
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=C(OC)C(OC)=CC(/C=C/CCCN2CCN(CCC/C=C/C3=CC(OC)=C(OC)C(OC)=C3)CCC2)=C1
|
| InChi Key |
JXXCDAKRSXICGM-AOEKMSOUSA-N
|
| InChi Code |
InChI=1S/C33H48N2O6/c1-36-28-22-26(23-29(37-2)32(28)40-5)14-9-7-11-16-34-18-13-19-35(21-20-34)17-12-8-10-15-27-24-30(38-3)33(41-6)31(25-27)39-4/h9-10,14-15,22-25H,7-8,11-13,16-21H2,1-6H3/b14-9+,15-10+
|
| Chemical Name |
1,4-bis[(E)-5-(3,4,5-trimethoxyphenyl)pent-4-enyl]-1,4-diazepane
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 1.7583 mL | 8.7914 mL | 17.5827 mL | |
| 5 mM | 0.3517 mL | 1.7583 mL | 3.5165 mL | |
| 10 mM | 0.1758 mL | 0.8791 mL | 1.7583 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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