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NS-3-008 is a novel and orally bioactive transcriptional inhibitor of G0/G1 switch 2 (G0s2). NS-3-008 can be used for chronic kidney disease. NS-3-008 inhibited the transcription of G0s2 with a half-maximal inhibitory concentration (IC50) of 2.25 μM. Moreover, treatment of wild-type 5/6Nx mice with NS-3-008 (5 mg/kg, P.O.) resulted in decreased levels of G0s2 and Ccl2 mRNA in the kidneys.
| ln Vitro |
Hsd17b4 is bound by NS-3-008; overexpression of Hsd17b4 causes G0s2 mRNA expression, but Hsd17b4 knockdown decreases G0s2 mRNA levels. One way to counteract the inhibitory impact of NS-3-008 is to delete the Stat5 binding site in the G0s2 promoter or knock down Hsd17b4. Stat5's nuclear phosphorylation is decreased by NS-3-008 [1].
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| ln Vivo |
G0s2 and Ccl2 mRNA levels in the kidney of wild-type 5/6Nx mice were reduced after 4 weeks of oral NS-3-008 (5 mg/kg) therapy. Phosphorylation of the proteins Stat5 and p65, as well as SUN concentration and renal caspase 3/7 activity, were all decreased in 5/6Nx animals given NS-03-08 treatment. The F4/80-positive region and F4/80 protein levels were decreased in 5/6Nx mice given NS-3-008 treatment [1].
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| References |
[1]. Matsunaga N, et al. Inhibition of G0/G1 Switch 2 Ameliorates Renal Inflammation in Chronic Kidney Disease. EBioMedicine. 2016 Nov;13:262-273.
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| Molecular Formula |
C14H24CLN3
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|---|---|
| Molecular Weight |
269.813462257385
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| Exact Mass |
269.165
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| Elemental Analysis |
C, 62.32 H, 8.97 Cl, 13.14 N, 15.57
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| CAS # |
1172854-54-4
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| Related CAS # |
1172854-54-4;1172854-54-4 (HCl);
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| PubChem CID |
45053078
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
18
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| Complexity |
208
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UMIOAATZOCKZTH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H23N3.ClH/c1-2-3-4-8-11-16-14(15)17-12-13-9-6-5-7-10-13/h5-7,9-10H,2-4,8,11-12H2,1H3,(H3,15,16,17)1H
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| Chemical Name |
1-benzyl-3-hexylguanidine hydrochloride
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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 : ~125 mg/mL (~463.29 mM)
H2O : ~125 mg/mL (~463.29 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.71 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 (7.71 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 (7.71 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: 10 mg/mL (37.06 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 | 3.7063 mL | 18.5316 mL | 37.0631 mL | |
| 5 mM | 0.7413 mL | 3.7063 mL | 7.4126 mL | |
| 10 mM | 0.3706 mL | 1.8532 mL | 3.7063 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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