| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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Description: JTE-607 HCl, the hydrochloride of JTE607, is a potent inhibitor of inflammatory cytokine production with the potential for the treatment of systemic inflammatory response. It induces apoptosis accompanied by an increase in p21waf1/cip1 in acute myelogenous leukemia cells. JTE-607 inhibits the production of TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively.
| ln Vitro |
JTE-607, with an IC50 of 11, 5.9, 8.8, 7.3, and 9.1 nM, respectively, suppresses the production of inflammatory cytokines by LPS-stimulated human PBMC, including TNF-α, IL-1β, IL-6, IL-8, and IL-10. JTE-607 also has an inhibitory effect on these cytokines' mRNA expression [1]. With an IC 50 of roughly 10 nM, JTE-607 suppresses the release of inflammatory cytokines by LPS-stimulated human PBMC [1]. JTE607 has an IC50 of 59, 780, 1600, and 19000 nM, respectively, which suppresses the production of TNF-α in mouse and rat PBMC and LPS-stimulated IL-8 in monkey and rabbit PBMC [1]. Moreover, JTE607 suppresses IL-1RA and granulocyte-macrophage colony-stimulating factor, with IC50 values of 5.4±0.4 nM and 2.4±0.8 nM, respectively[1]. In monkey, rabbit, mouse, and rat, JTE-607 suppresses cytokine production with IC50 values of 59±26, 780±120, 1600±650, and 19000±3200 nM, respectively[1].
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| ln Vivo |
After an LPS exposure in C, JTE-607 (0.3–10 mg/kg, iv) dose-dependently lowers mortality. mice susceptible to parvum, while lowering TNF-α in mouse plasma [1].
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| Cell Assay |
RT-PCR[1]
Cell Types: human peripheral blood mononuclear cells (PBMCs) Tested Concentrations: 100 nM Incubation Duration: 20 hrs (hours) Experimental Results: decreased the increase in the level of mRNAs of TNF-α, IL-1b, IL-6 and IL -8. |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (5 to 6 weeks old) are sensitized by injecting Corynebacterium parvum[1]
Doses: 0.3, 1, 3, 10 mg/kg Route of Administration: Administered intravenously (iv)10 min before the LPS challenge. Experimental Results: demonstrated dose dependent inhibition of the mortality at 0.3 to 10 mg/kg and significant effect at 3 and 10 mg/kg. |
| References | |
| Additional Infomation |
JTE-607 dihydrochloride is the dihydrochloride salt of JTE-607. It is a cytokine inhibitor which suppresses the production of proinflammatory cytokines such as interleukin (IL-1beta), IL-6, IL-8, granulocyte macrophage colony stimulating factor (GM-CSF), and tumor necrosis factor (TNF-alpha). It acts as a pro-drug which is cleaved by carboxylesterase 1 (CES1) to its active free acid form, which then binds to cleavage and polyadenylation specificity factor 3 (CPSF3). It has a role as an anti-inflammatory agent, an antineoplastic agent, an apoptosis inducer, a prodrug, a cardioprotective agent and a CPSF3 inhibitor. It contains a JTE-607(2+).
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| Molecular Formula |
C22H29CL4N3O3
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|---|---|
| Molecular Weight |
525.292
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| Exact Mass |
595.117
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| Elemental Analysis |
C, 50.27; H, 5.57; Cl, 23.74; N, 7.03; O, 13.39
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| CAS # |
188791-09-5
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| Related CAS # |
188791-71-1;188791-09-5 (HCl);
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| PubChem CID |
9938544
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| Appearance |
White to off-white solid powder
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| LogP |
5.284
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
37
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| Complexity |
674
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| Defined Atom Stereocenter Count |
1
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| SMILES |
ClC1=C(C(C(N([H])[C@]([H])(C(=O)OC([H])([H])C([H])([H])[H])C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])=O)=C([H])C(=C1OC([H])([H])C([H])([H])N1C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H])Cl)O[H].Cl[H].Cl[H]
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| InChi Key |
JUJAUEQJEWIWCQ-FJSYBICCSA-N
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| InChi Code |
InChI=1S/C25H31Cl2N3O5.2ClH/c1-3-34-25(33)20(15-17-7-5-4-6-8-17)28-24(32)18-16-19(26)23(21(27)22(18)31)35-14-13-30-11-9-29(2)10-12-30/h4-8,16,20,31H,3,9-15H2,1-2H3,(H,28,32)2*1H/t20-/m0../s1
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| Chemical Name |
N-[3,5-Dichloro-2-hydroxy-4-[2-(4-methyl-1-piperazinyl)ethoxy]benzoyl]-L-phenylalanine ethyl ester dihydrochloride
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| Synonyms |
TO-207; TO 207; TO207; JTE-607; JTE 607; JTE 607; JTE-607 HCl; JTE-607 dihydrochloride.
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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) |
DMSO : ~250 mg/mL (~418.51 mM)
H2O : ~20 mg/mL (~33.48 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.48 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 (3.48 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 (3.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (167.40 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9037 mL | 9.5186 mL | 19.0371 mL | |
| 5 mM | 0.3807 mL | 1.9037 mL | 3.8074 mL | |
| 10 mM | 0.1904 mL | 0.9519 mL | 1.9037 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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