| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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G150 (G-150) is a novel, potent and selective inhibitor of h-cGAS (human cyclic GMP-AMP synthase) which inhibits dsDNA-triggered interferon expression with an IC50 of 10.2 nM.
| ln Vitro |
G150 (0.1-100 μM; 1 hour) has an impact on primary human macrophages and human THP1 cells' production of CXCL10 and IFNB1 [1]. THP1 cells and primary human macrophages' dsDNA sensing is impacted by G150 (5–10 μM; 1 hour) [1]. G150 (0.1-100 μM; 1 hour) has an impact on THP1-Dual cell activation of the NF-κB pathway [1].
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|---|---|
| Cell Assay |
RT-PCR[1]
Cell Types: human THP1 cells and primary human macrophages Tested Concentrations: 0.1-100 μM Incubation Duration: 1 hour Experimental Results: Dose-dependent inhibition of IFNB1 and interferon-stimulated genes Monitoring CXCL10 expression, IC50 is 1.96 respectively and 7.57 μM in human THP1 cells, and inhibited the expression of IFNB1 and CXCL10 in primary human macrophages with IC50 of 0.62 and 0.87 μM, respectively. RT-PCR[1] Cell Types: human THP1 cells and primary human macrophages Tested Concentrations: 5 and 10 μM Incubation Duration: 1 hour Experimental Results: 10 μM in THP1 cells and 5 μM in primary cells , inhibits dsDNA sensing in human macrophages. RT-PCR[1] Cell Types: THP1-Dual cells Tested Concentrations: 0.1-100 μM Incubation Duration: 1 hour Experimental Results: Inhibits SEAP activity and luciferase activity in THP1-Dual cells, IC50 is 0.90 and 1.79 μM respectively. |
| References |
| Molecular Formula |
C18H16CL2N4O2
|
|---|---|
| Molecular Weight |
391.2512
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| Exact Mass |
390.065
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| CAS # |
2369751-30-2
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| PubChem CID |
138393372
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| Appearance |
White to off-white solid powder
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| Density |
1.545±0.06 g/cm3(Predicted)
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| Boiling Point |
694.0±55.0 °C(Predicted)
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| Flash Point |
373.5±31.5 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.736
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| LogP |
2.73
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
26
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| Complexity |
539
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
VVUOUIPXYFIWLE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16Cl2N4O2/c19-12-5-10(9-1-2-14(21)22-6-9)16-11-7-24(15(26)8-25)4-3-13(11)23-18(16)17(12)20/h1-2,5-6,23,25H,3-4,7-8H2,(H2,21,22)
|
| Chemical Name |
1-[9-(6-aminopyridin-3-yl)-6,7-dichloro-1,3,4,5-tetrahydropyrido[4,3-b]indol-2-yl]-2-hydroxyethanone
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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 : ~125 mg/mL (~319.49 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.32 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 (5.32 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 (5.32 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 | 2.5559 mL | 12.7796 mL | 25.5591 mL | |
| 5 mM | 0.5112 mL | 2.5559 mL | 5.1118 mL | |
| 10 mM | 0.2556 mL | 1.2780 mL | 2.5559 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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