| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| Targets |
HsNMT1 ( IC50 < 1 nM ); HsNMT2 ( IC50 < 1 nM ); HsNMT1 ( Kd < 210 pM )
|
|---|---|
| ln Vitro |
IMP-1088 (1-1000 nM) has an IC50 of 17 nM and inhibits the virus-induced cytopathic effect (CPE) in a dose-dependent manner. With an IC50 of 5.8 nM, IMP-1088 (125 nM) completely inhibits novel infectious viruses. In primary human bronchial epithelial cells (hBEC) infected with rhinovirus RV-A1 (MOI 5), IMP-1088 (1-1000 nM) suppresses single cycle replication and stops the formation of infectious virus for a duration of 7 hours. Even when added up to three hours after infection, IMP-1088 dramatically reduces the generation of infectious viruses[1]. In enriched samples, IMP-1088 (50 nM) considerably reduces the enrichment of several N-myristoylated proteins[1]. By preventing virus assembly in HeLa cells infected with rhinovirus RV-A16 (MOI 20) for six hours, IMP-1088 (500 nM) reduces the generation of infectious rhinovirus particles[1]. NMT activity fully recovers in 24 hours and IMP-1088 (0.24 nM-1 µM; for 24 hours + 24 hours washout) has no long-term effect on cell viability[1]. IMP-1088 effectively inhibits co-translational myristoylation of a virus-specific encoded protein (VP0), hence blocking a crucial stage in viral capsid construction. IMP-1088 does not impede the translation of rhinovirus polyprotein or the synthesis of viral RNA[1].
|
| References |
[1]. Aurélie Mousnier, et al. Fragment-derived Inhibitors of Human N-myristoyltransferase Block Capsid Assembly and Replication of the Common Cold Virus. Nat Chem. 2018 Jun;10(6):599-606.
|
| Molecular Formula |
C25H29F2N5O
|
|---|---|
| Molecular Weight |
453.53
|
| Exact Mass |
453.23
|
| Elemental Analysis |
C, 66.21; H, 6.45; F, 8.38; N, 15.44; O, 3.53
|
| CAS # |
2059148-82-0
|
| Appearance |
Liquid
|
| SMILES |
CC1=C(C(=NN1C)C)CCOC2=C(C=CC(=C2F)F)C3=CC4=C(C=C3)N(N=C4CN(C)C)C
|
| InChi Key |
SOXNKJCQBRQUMS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C25H29F2N5O/c1-15-18(16(2)31(5)28-15)11-12-33-25-19(8-9-21(26)24(25)27)17-7-10-23-20(13-17)22(14-30(3)4)29-32(23)6/h7-10,13H,11-12,14H2,1-6H3
|
| Chemical Name |
1-[5-[3,4-difluoro-2-[2-(1,3,5-trimethylpyrazol-4-yl)ethoxy]phenyl]-1-methylindazol-3-yl]-N,N-dimethylmethanamine
|
| Synonyms |
IMP1088; IMP 1088; IMP-1088
|
| 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) |
DMSO : ~100 mg/mL (~220.5 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.51 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 25.0 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: ≥ 2.5 mg/mL (5.51 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 25.0 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: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2049 mL | 11.0246 mL | 22.0493 mL | |
| 5 mM | 0.4410 mL | 2.2049 mL | 4.4099 mL | |
| 10 mM | 0.2205 mL | 1.1025 mL | 2.2049 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.
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
