| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
mPGES-1 level is considerably inhibited by dipoglanstat (IC50: approximately 1 nM)[3]. The up-regulation of P-gp and mPGES-1 levels on glutamate-mediated in isolated brain capillaries is inhibited by vipoglanstat [3]. Vipoglanstat inhibits the migration of inflammatory cells in human peripheral blood as well as the release of inflammatory mediators[3].
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|---|---|
| ln Vivo |
With reductions in neutrophil influx, protein content, TNF-ɑ, IL-1β, and PGE2 levels in bronchoalveolar lavage (BAL), myeloperoxidase activity, expression of mPGES-1, cyclooxygenase (COX)-2, and intracellular adhesion molecule in lung tissue, dipoglanstat (30 mg/kg; ip) can lessen LPS-induced lung injury[2]. Lung injury score, mPGES-1 and inducible nitric oxide synthase lung expression, and sepsis-induced BAL inflammatory cell recruitment are all markedly reduced by dipoglanstat (30 mg/kg; po; 2 h, 8 h, and 22 h)[2]. Mice with acute sepsis who receive dipoglanstat (30 mg/kg; po; QD) also have significantly longer survival times[2].
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| Animal Protocol |
Animal/Disease Models: LPS-induced acute lung injury models [2]
Doses: 30 mg/kg Route of Administration: 30 mg/kg, ip Experimental Results: Preserved lung architecture and decreased immune cell influx into the lungs of LPS‑challenged mice. Animal/Disease Models: CLP-induced sepsis models[2] Doses: 30 mg/kg Route of Administration: 30 mg/kg, po, 2 hrs, 8 hrs and 22 hrs; 30 mg/kg, po, QD Experimental Results: Attenuated CLP‑induced lung injury and prolonging survival. |
| References |
| Molecular Formula |
C30H34CL2F5N5O3
|
|---|---|
| Molecular Weight |
678.520682811737
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| Exact Mass |
677.195
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| CAS # |
1360622-01-0
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| PubChem CID |
56649447
|
| Appearance |
White to off-white solid powder
|
| LogP |
7.8
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
10
|
| Heavy Atom Count |
45
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| Complexity |
1010
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(NC2=C(Cl)C=CC(CNC(=O)C(C)(C)C)=C2Cl)N(C)C2=CC(OCC(F)F)=C(C(N[C@@H]3CC[C@@H](C(F)(F)F)CC3)=O)C=C2N=1
|
| InChi Key |
PFORUFFGGNOLPJ-FITNRVMRSA-N
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| InChi Code |
InChI=1S/C30H34Cl2F5N5O3/c1-29(2,3)27(44)38-13-15-5-10-19(31)25(24(15)32)41-28-40-20-11-18(22(45-14-23(33)34)12-21(20)42(28)4)26(43)39-17-8-6-16(7-9-17)30(35,36)37/h5,10-12,16-17,23H,6-9,13-14H2,1-4H3,(H,38,44)(H,39,43)(H,40,41)/t16?,17-
|
| Chemical Name |
2-{2,6-dichloro-3-[(2,2- dimethylpropanamido)methyl]anilino}-6-(2,2- difluoroethoxy)-1-methyl-N-[trans-4- (trifluoromethyl)cyclohexyl]-1H-benzimidazole-5- carboxamide
|
| Synonyms |
Vipoglanstat BI-1029539 GS-248 BI 1029539 GS248 BI1029539 GS 248
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~150 mg/mL (~221.07 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.75 mg/mL (5.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 37.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4738 mL | 7.3690 mL | 14.7380 mL | |
| 5 mM | 0.2948 mL | 1.4738 mL | 2.9476 mL | |
| 10 mM | 0.1474 mL | 0.7369 mL | 1.4738 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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