NS-3-008 HCl
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MedKoo CAT#: 555784

CAS#: 1172854-54-4 (HCl)

Description: NS-3-008 is an orally active 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.


Chemical Structure

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NS-3-008 HCl
CAS# 1172854-54-4 (HCl)

Theoretical Analysis

MedKoo Cat#: 555784
Name: NS-3-008 HCl
CAS#: 1172854-54-4 (HCl)
Chemical Formula: C14H24ClN3
Exact Mass: 0.00
Molecular Weight: 269.817
Elemental Analysis: C, 62.32; H, 8.97; Cl, 13.14; N, 15.57

Price and Availability

Size Price Availability Quantity
10mg USD -2 2 Weeks
25mg USD -2 2 Weeks
5g USD -2 2 Weeks
50mg USD 450 2 Weeks
100mg USD 750 2 Weeks
200mg USD 1250 2 Weeks
500mg USD 1950 2 Weeks
1g USD 2950 2 Weeks
2g USD 5450 2 Weeks
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Related CAS #: 1172854-54-4 (free base)   1172854-54-4 (HCl)    

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

Appearance: Solid powder

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.

Product Data:
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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 125.0 463.28
Water 125.0 463.28

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.

Recalculate based on batch purity %
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.

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https://www.thelancet.com/journals/ebiom/article/PIIS2352-3964(16)30463-7/fulltext