Synonym
NS-3-008 HCl; NS-3-008 hydrochloride; NS-3-008; NS 3-008; NS3-008; NS-3008; NS 3008; NS3008;
IUPAC/Chemical Name
1-benzyl-3-hexylguanidine hydrochloride
InChi Key
UMIOAATZOCKZTH-UHFFFAOYSA-N
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
SMILES Code
N=C(NCC1=CC=CC=C1)NCCCCCC.[H]Cl
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Chronic kidney disease (CKD) is a global health problem, and novel therapies to treat CKD are urgently needed. Chronic renal inflammation in CKD was ameliorated by clock mutation. G0s2 was important for the anti-inflammatory effects of clock mutation.
Biological target:
NS-3-008 hydrochloride is an orally active transcriptional inhibitor of G0/G1 switch 2 (G0s2) with an IC50 of 2.25 μM.
In vitro activity:
This study carried out high-throughput screening of 9600 small compounds to identify novel transcriptional inhibitors of G0s2 (Figs. S4, S5). NS-3-008 inhibited the transcription of G0s2 with a half-maximal inhibitory concentration (IC50) of 2.25 μM (Fig. S6).
Reference: EBioMedicine. 2016 Nov;13:262-273. https://pubmed.ncbi.nlm.nih.gov/27745900/
In vivo activity:
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 (Fig. 7A). The phosphorylation of Stat5 and p65 protein was decreased in wild-type 5/6Nx mice treated with NS-3-008 (Fig. 7B), and SUN concentrations and renal caspase 3/7 activity decreased in 5/6Nx mice treated with NS-03-08 (Fig. 7). Finally, the F4/80-positive area and F4/80 protein levels were decreased in 5/6Nx mice treated with NS-3-008 (Fig. 7D).
Reference: EBioMedicine. 2016 Nov;13:262-273. https://pubmed.ncbi.nlm.nih.gov/27745900/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMSO |
125.0 |
463.28 |
|
| Water |
125.0 |
463.28 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
269.82
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
Matsunaga N, Ikeda E, Kakimoto K, Watanabe M, Shindo N, Tsuruta A, Ikeyama H, Hamamura K, Higashi K, Yamashita T, Kondo H, Yoshida Y, Matsuda M, Ogino T, Tokushige K, Itcho K, Furuichi Y, Nakao T, Yasuda K, Doi A, Amamoto T, Aramaki H, Tsuda M, Inoue K, Ojida A, Koyanagi S, Ohdo S. Inhibition of G0/G1 Switch 2 Ameliorates Renal Inflammation in Chronic Kidney Disease. EBioMedicine. 2016 Nov;13:262-273. doi: 10.1016/j.ebiom.2016.10.008. Epub 2016 Oct 6. PMID: 27745900; PMCID: PMC5264248.
In vitro protocol:
Matsunaga N, Ikeda E, Kakimoto K, Watanabe M, Shindo N, Tsuruta A, Ikeyama H, Hamamura K, Higashi K, Yamashita T, Kondo H, Yoshida Y, Matsuda M, Ogino T, Tokushige K, Itcho K, Furuichi Y, Nakao T, Yasuda K, Doi A, Amamoto T, Aramaki H, Tsuda M, Inoue K, Ojida A, Koyanagi S, Ohdo S. Inhibition of G0/G1 Switch 2 Ameliorates Renal Inflammation in Chronic Kidney Disease. EBioMedicine. 2016 Nov;13:262-273. doi: 10.1016/j.ebiom.2016.10.008. Epub 2016 Oct 6. PMID: 27745900; PMCID: PMC5264248.
In vivo protocol:
Matsunaga N, Ikeda E, Kakimoto K, Watanabe M, Shindo N, Tsuruta A, Ikeyama H, Hamamura K, Higashi K, Yamashita T, Kondo H, Yoshida Y, Matsuda M, Ogino T, Tokushige K, Itcho K, Furuichi Y, Nakao T, Yasuda K, Doi A, Amamoto T, Aramaki H, Tsuda M, Inoue K, Ojida A, Koyanagi S, Ohdo S. Inhibition of G0/G1 Switch 2 Ameliorates Renal Inflammation in Chronic Kidney Disease. EBioMedicine. 2016 Nov;13:262-273. doi: 10.1016/j.ebiom.2016.10.008. Epub 2016 Oct 6. PMID: 27745900; PMCID: PMC5264248.
Matsunaga N, Ikeda E, Kakimoto K, Watanabe M, Shindo N, Tsuruta A, Ikeyama H, Hamamura K, Higashi K, Yamashita T, Kondo H, Yoshida Y, Matsuda M, Ogino T, Tokushige K, Itcho K, Furuichi Y, Nakao T, Yasuda K, Doi A, Amamoto T, Aramaki H, Tsuda M, Inoue K, Ojida A, Koyanagi S, Ohdo S. Inhibition of G0/G1 Switch 2 Ameliorates Renal Inflammation in Chronic Kidney Disease. EBioMedicine. 2016 Nov;13:262-273. doi: 10.1016/j.ebiom.2016.10.008. Epub 2016 Oct 6. PMID: 27745900; PMCID: PMC5264248.
